Acetylcholine is an essential neurotransmitter found throughout the nervous system. Its action on postsynaptic receptors is regulated through hydrolysis by various carboxylesterases, especially cholinesterases (ChEs)....Acetylcholine is an essential neurotransmitter found throughout the nervous system. Its action on postsynaptic receptors is regulated through hydrolysis by various carboxylesterases, especially cholinesterases (ChEs). The acute toxicity of organophosphate (OP) compounds is directly linked to their action as inhibitors of ChE. One widely used assay for evaluating ChE activity is a spectrophotometric method developed by Ellman et al. When the enzyme source is from tissues or, in particular, blood, hemoglobin displays a spectrophotometric peak at the same wave-length used to analyze cholinergic activity. This creates a substantial background that interferes with the Ellman’s assay and must be overcome in order to accurately monitor cholinesterase activity. Herein, we directly compare blood processing methods: classical method (1.67 ± 0.30 U/mL) and HemogloBindTM treatment (1.51 ± 0.17 U/mL), and clearly demonstrate that pretreatment of blood samples with HemoglobindTM is both a sufficient and rapid sample preparation method for the assessment of ChE activity using the Ellman’s method.展开更多
AIM To examine whether nizatidine stimulatesduodenal HCO<sub>3</sub><sup>-</sup> secretion in rats by inhibitingAChE activity.METHODS Under pentobarbital anesthesia,aproximal duodenal loop was ...AIM To examine whether nizatidine stimulatesduodenal HCO<sub>3</sub><sup>-</sup> secretion in rats by inhibitingAChE activity.METHODS Under pentobarbital anesthesia,aproximal duodenal loop was perfused withsaline,and the HCO<sub>3</sub> secretion was measuredat pH 7.0 using a pH-stat method and by adding10mM HCI.Nizatidine,neostigmine,carbacholor famotidine was administered i.v.as a singleinjection.RESULTS Intravenous administration ofnizatidine（3-30 mg/kg）dose-dependentlyincreased duodenal HCO<sub>3</sub><sup>-</sup> secretion,and theeffect at 10mg/kg was equivalent to thatobtained by carbachol at 0.01 mg/kg.Thisnizatidine action was observed at the same doserange that inhibited acid secretion and enhancedgastric motility,mimicked by i.v.injection ofneostigmine（0.03 mg/kg）,and significantlyattenuated by bilateral vagotomy and prior s.c.administration of atropine but not byindomethacin,a cyclooxygenase inhibitor,orN<sup>G</sup>-nitro-L-arginine methyl ester,a NO synthaseinhibitor.The HCO<sub>3</sub><sup>-</sup> secretory response toacetylcholine（0.001 mg/kg）was significantlypotentiated by the concurrent administration ofnizatidine（3mg/kg,i.v.）.The IC<sub>50</sub>of nizatidine for AChE of rat erythrocytes was1.4×10<sup>-6</sup>M,about 12 times higher than that ofneostigmine.Neither famotidine(】10<sup>-3</sup>M,30mg/kg,i.v.)nor cisapride(】 10<sup>-3</sup>M,3mg/kg,i.v.)had any influence on AChEactivity or duodenal HCO<sub>3</sub><sup>-</sup> secretion.Duodenaldamage induced by acid perfusion（100 mM HCIfor 4 h）in the presence of indomethacin wassignificantly prevented by nizatidine andneostigmine,at the doses that increased theHCO<sub>3</sub><sup>-</sup> secretion.CONCLUSION Nizatidine stimulates duodenalHCO<sub>3</sub><sup>-</sup> secretion,in both vagal-dependent andatropine-sensitive manners,and the action isassociated with the anti-AChE activity of thisagent.展开更多
Objective:To explore cholinesterase inhibitory and antioxidant effect of six coniferous trees(Abies bornmulleriana,Picea pungens,Juniperus communis,Cedrus libani,Taxus baccata,and Cupressus sempervirens var.horizantal...Objective:To explore cholinesterase inhibitory and antioxidant effect of six coniferous trees(Abies bornmulleriana,Picea pungens,Juniperus communis,Cedrus libani,Taxus baccata,and Cupressus sempervirens var.horizantalis).Methods:Acetone(Ace),ethyl acetate(EtOAc),and ethanol(EtOH)extracts prepared from the needles and shoots of the six coniferous trees were screened for their acetylcholinesterase(AChE)and butyrylcholinesterasc(BChE)inhibitory activity at 100μg/mL.Antioxidant activity of the extracts was tested using 2,2-diphenyl-1-picrylhydrazyl(DPPH)and N,N-dimethyl-p-phenylendiamine(DMPD)radical scavenging,nietal-chelation capacity,ferric-(FRAP)and phosphomolibdenum-reducing antioxidant power(PRAP)assays.All of the assays were performed in ELISA microplate reader.Total phenol and flavonoid amounts in the extracts were determined spectrophotometrically.Results:Among thirty-six extracts in total,the shoot-Ace extract of Cupressus sempervirens var.horizantalis exerted the highest inhibition against AChE[(54.84±2.51)%],while the needle-Ace extract of Cedrus libani was the most effective in inhibiting BChE[(67.54±0.30)%].The highest DPPH radical scavenging effect,FRAP and PRAP was observed in the shoot-Ace and EtOAc extracts from Taxus baccata.whereas all the extracts showed a variable degree of scavenging effect against DPMD radical.The shoot-EtOAc extract of Cedrus libani had the highest metalchelation capacity[(58.04±0.70)%].The shoot extracts of Taxus baccata were determined to have the richest total phenol content,which may contribute to its marked antioxidant activity.Conclusions:The conifer species screened in this study may contain cholinesterase-inhibiting and antioxidant properties,which might be useful against Alzheimer's disease.展开更多
Objective:To investigate the effect of Cannabis sativa resin and/or tramadol,two commonly drugs of abuse on acetylcholinesterase and butyrylcholinesterase activities as a possible cholinergic biomarkers of neurotoxici...Objective:To investigate the effect of Cannabis sativa resin and/or tramadol,two commonly drugs of abuse on acetylcholinesterase and butyrylcholinesterase activities as a possible cholinergic biomarkers of neurotoxicity induced by these agents.Methods:rats were treated with cannabis resin(5,10 or 20 mg/kg)(equivalent to the active constituent A'-tetrahydrocannabinol),tramadol(5,10 and 20 mg/kg) or tramadol(10 mg/kg)combined with cannabis resin(5,10 and 20 mg/kg) subcutaneously daily for 6 weeks.Acetylcholinesterase(AChE) and butyrylcholinesterase(BChE) activities were measured in brain and serum.We also measured the activity of paraoxonase-1(PONl) in serum of rats treated with these agents.Results:(i) AChE activity in brain increased after 10-20 mg/kg cannabis resin(by 16.3%-36.5%).AChE activity in brain did not change after treatment with 5-20 mg/kg tramadol.The administration of both cannabis resin(5,10 or 20 mg/kg) and tramadol(10 mg/kg) resulted in decreased brain AChE activity by 14.1%,12.9%and 13.6%,respectively;(ii) BChE activity in serum was markedly and dose-dependenlly inhibited by cannabis resin(by 60.9%-76.9%).BChE activity also decreased by 17.6%-36.5%by 10-20mg/kg tramadol and by 57.2%-63.9%by the cannabis resin/tramadol combined treatment;(iii)Cannabis resin at dose of 20 mg/kg increased serum PONl activity by 25.7%.In contrast,tramadol given at 5,10 and 20 mg/kg resulted in a dose-dependent decrease in serum PON1 activity by 19%,36.7%,and 46.1%,respectively.Meanwhile,treatment with cannabis resin plus tramadol resulted in 40.2%,35.8%,30.7%inhibition of PONl activity compared to the saline group.Conclusions:these data suggest that cannabis resin exerts different effects on AChE and BChE activities which could contribute to the memory problems and the decline in cognitive function in chronic users.展开更多
Two novel naphthol derivatives(1 and 2) were synthesized and characterized via IR,~1H NMR,and HRMS.The structure of compound 2 was verified by single-crystal X-ray crystallography.It crystallizes in monoclinic,space g...Two novel naphthol derivatives(1 and 2) were synthesized and characterized via IR,~1H NMR,and HRMS.The structure of compound 2 was verified by single-crystal X-ray crystallography.It crystallizes in monoclinic,space group C2/c with a = 21.6725(9),b = 6.0127(3),c = 25.5405(14) ?,β = 94.716(5)o,V = 3316.9(3) ?~3,Z = 8,F(000) = 1384,D_c = 1.511 Mg/m^3,M_r = 377.22 and μ = 2.487 mm^(-1).In addition,their cholinesterase inhibitory activities in vitro toward Electrophorus electricus acetylcholinesterase(eel ACh E) and horse serum butyrylcholinesterase(eq BCh E) were further determined.The results showed that compound 1 as a new acetylcholinesterase(ACh E) inhibitor displayed higher ACh E inhibitory activity(IC_(50) = 1.4 μM),which could be considered for Alzheimer's disease therapeutics.展开更多
Introduction: Dementia is frequently associated with Parkinson’s disease, especially in later stages. Efficacy of cholinesterase inhibitors (ChI) in Alzheimer’s dementia is well established. However, treatment with ...Introduction: Dementia is frequently associated with Parkinson’s disease, especially in later stages. Efficacy of cholinesterase inhibitors (ChI) in Alzheimer’s dementia is well established. However, treatment with ChI in Parkinson’s disease dementia (PDD) remains controversial. The objective of this systematic review and meta-analysis was to assess the effects of ChI in PDD. Methods: A comprehensive literature search was performed in MEDLINE, EMBASE and Cochrane library up to March 2014 using the descriptors “Parkinson’s disease”, “dementia in Parkinson’s disease”, “cognition”, “acetylcholinesterase inhibitors”, “cholinesterase inhibitors”, “anticholinesterase agents”, “rivastigmine”, “donepezil” and “galantamine” (Pubmed search strategy). All randomized, doubleblinded, placebo-controlled trials that met the eligibility criteria and assessed the effects of ChI in PDD were considered for analysis. There were no restrictions regarding paper language. Summary effect-sizes were presented as standardized mean differences (SMD) and the pooled analysis was performed with a fixed-effects model. Outcomes considered for analysis were the Mini Mental Status Exam (MMSE) score and the cognition scale for evaluation of dementia ADAS-Cog. The degree of heterogeneity between included studies was assessed through the I2 test. Results: After a comprehensive search, 175 references were retrieved. From these, five randomized trials involving 946PDD subjects were included in the review. Four studies used donepezil and only one study used rivastigmine. The pooled analysis of five studies that assessed the effects of ChI in MMSE total score showed a SMD of 0.24 (CI 95% 0.11 - 0.38). Three studies considered the effects of ChI on Adas-Cog and the pooled results showed a SMD of 0.21 (CI 95% 0.07 - 0.35). There was no significant heterogeneity between the studies. Conclusions: The results of this systematic review and meta- analysis suggest that ChI improves cognitive impairment in PDD subjects. Despite statistically significant, the translation of these results into relevant clinical improvement should be taken with caution, as the studies did not address what would be considered a clinically significant result.展开更多
Cholinergic dysfunction is common to Alzheimer’s dementia and Schizophrenia. The objective of this study is to undertake a systematic review and meta-analysis of the literature on the cognitive and clinical effects o...Cholinergic dysfunction is common to Alzheimer’s dementia and Schizophrenia. The objective of this study is to undertake a systematic review and meta-analysis of the literature on the cognitive and clinical effects of cholinesterase inhibitors administered to patients with schizophrenia and co-morbid Alzheimer’s disease dementia. A literature search of the MEDLINE, CINAHL, PubMed, PsycINFO, EMBASE, AMED, BNI, HMIC and Health Business Elite databases has been performed (up to January 2013) to investigate the use of cholinesterase inhibitors in patients with schizophrenia and dementia. The terms “schizophrenia”, “dementia”, “rivastigmine”, “donepezil”, “galantamine” and “cognitive deficit” have been searched, with a restriction for English language. Five published studies including 1 RCT have been included for the qualitative review. Treatments include Donepezil 5 mg and 10 mg as well as Rivastigmine 9 mg. The numbers of participants vary from 2 incase report to20 inthe RCT. Only 1 study qualifies for meta-analysis. There is a very limited evidence on the efficacy and safety of using acetylcholinesterase inhibitors in the management of dementia co-morbid with schizophrenia. The only randomised controlled study shows lack of evidence in terms of efficacy in using cholinesterase inhibitors in the management of dementia with schizophrenia. Future research projects will have to look at an adequate sample size to explore treatment on various cognitive and noncognitive domains and the sample should be selected by using definitive and internationally acceptable diagnostic criteria.展开更多
<strong>Objective:</strong> To evaluate early prediction value of IPS<span> </span><span><span style="font-family:Verdana;">combined with SchE and D-dimer detection for in...<strong>Objective:</strong> To evaluate early prediction value of IPS<span> </span><span><span style="font-family:Verdana;">combined with SchE and D-dimer detection for infection and survival in critically ill patients. </span><b><span style="font-family:Verdana;">Methods:</span></b></span><b><span> </span></b><span style="font-family:Verdana;">199 critically ill patients admitted to the emergency intensive care unit (EICU) of our hospital from December 2018 to December 2019 were retrospectively analyzed, including 110 infection patients (infection group) and 89 non-infection</span><span> </span><span style="font-family:Verdana;">patients (non-infection group).</span><span> </span><span><span style="font-family:Verdana;">According to the survival, the infection group was divided into death group (68 cases) and survival group (42 cases). The IPS, APACHE II, SOFA and SchE, D-dimer expression levels were detected and compared;Univariate and logistic regression analysis were used to evaluate the independent prognostic factors. </span><b><span style="font-family:Verdana;">Results: </span></b><span style="font-family:Verdana;">The IPS and APACHE II of patients in the infected group were higher than those in the non-infected group, the level of SchE was lower than that in the non-infected group, and the level of D-dimer was higher than that in the non-infected group (</span><i><span style="font-family:Verdana;">P</span></i></span><i><span> </span></i><span style="font-family:Verdana;"><</span><span> </span><span style="font-family:Verdana;">0.001). IPS, SOFA, APACHE</span><span style="font-family:Verdana;"> II</span><span style="font-family:Verdana;">, SchE, D-dimer, invasive mechanical ventilation, septic shock, and ICU length</span><span style="font-family:Verdana;"> of stay had significant influence on the prognosis of critically ill patients</span><span> </span><span><span style="font-family:Verdana;">(</span><i><span style="font-family:Verdana;">P</span></i></span><i><span> </span></i><span style="font-family:Verdana;"><</span><span> </span><span><span style="font-family:Verdana;">0.001). Logistic regression analysis showed that IPS (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 2.821, </span><span><span style="font-family:Verdana;">95%</span><i><span style="font-family:Verdana;"> CI</span></i></span><span style="font-family:Verdana;"> 1.501</span></span><span style="font-family:Verdana;"> - </span><span><span style="font-family:Verdana;">5.227), SOFA (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 5.078, </span><span><span style="font-family:Verdana;">95% </span><i><span style="font-family:Verdana;">CI</span></i></span><span style="font-family:Verdana;"> 3.327 </span></span><span style="font-family:Verdana;">-</span><span><span style="font-family:Verdana;"> 7.690), APACHE II (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 14.308, </span><span><span style="font-family:Verdana;">95% </span><i><span style="font-family:Verdana;">CI</span></i></span><span style="font-family:Verdana;"> 8.901 </span></span><span style="font-family:Verdana;">-</span><span><span style="font-family:Verdana;"> 21.893), SchE (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 0.223, </span><span><span style="font-family:Verdana;">95%</span><i><span style="font-family:Verdana;"> CI</span></i></span><span style="font-family:Verdana;"> 0.165 </span></span><span style="font-family:Verdana;">-</span><span style="font-family:Verdana;"> 0.291), D-dimer</span><span style="font-family:Verdana;"> (</span><i><span style="font-family:Verdana;">OR</span></i><i><span> </span></i><span style="font-family:Verdana;">=</span><span> </span><span style="font-family:Verdana;">2.10</span><span style="font-family:Verdana;">, </span><span style="font-family:Verdana;">95%</span><i><span> </span></i><i><span style="font-family:Verdana;">CI</span></i><i><span> </span></i><span style="font-family:Verdana;">1.55</span><span style="font-family:Verdana;"> - </span><span style="font-family:Verdana;">2.85</span><span style="font-family:Verdana;">)</span><span><span style="font-family:Verdana;">, septic shock (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 9.948,</span></span><span> </span><span style="font-family:Verdana;">95%</span><span> </span><i><span style="font-family:Verdana;">CI</span></i><span style="font-family:Verdana;"> 7.012</span><span style="font-family:Verdana;"> - </span><span style="font-family:Verdana;">17.012)</span><span> </span><span style="font-family:Verdana;">were independent factors affecting the prognosis of critically ill patients with infection</span><span style="font-family:Verdana;"> (</span><i><span style="font-family:Verdana;">P</span></i><span> </span><span style="font-family:Verdana;"><</span><span> </span><span style="font-family:Verdana;">0.001</span><span style="font-family:Verdana;">)</span><span style="font-family:Verdana;">.</span><span> </span><b><span style="font-family:Verdana;">Conclusion:</span></b><b><span> </span></b><span style="font-family:Verdana;">IPS and D-dimer expression level in infected patients were increased and SchE decreased significantly compared with those in non-infected patients, and they significantly correlated with</span><span> </span><span style="font-family:Verdana;">disease severity of infected</span><span> </span><span style="font-family:Verdana;">patients</span><span> </span><span style="font-family:Verdana;">and could be early prediction</span><span> </span><span style="font-family:Verdana;">for prognosis.</span>展开更多
Objective: To study the changes of serum pancreatic stone protein (PSP) and cholinesterase (ChE) contents in children with sepsis and their correlation with systemic inflammatory response and target organ damage. Meth...Objective: To study the changes of serum pancreatic stone protein (PSP) and cholinesterase (ChE) contents in children with sepsis and their correlation with systemic inflammatory response and target organ damage. Methods: A total of 64 children with sepsis who were treated in the hospital between January 2015 and January 2017 were selected as observation group, and 50 healthy children who received vaccination in the hospital during the same period were selected as normal control group. The contents of PSP, ChE, inflammatory factors as well as liver and kidney function indexes in the two groups were detected. Pearson test was used to assess the correlation of serum PSP and ChE contents with systemic inflammatory response and target organ damage in children with sepsis. Results: Serum PSP content of observation group was higher than that of control group while ChE content was lower than that of control group;serum inflammatory factors PCT, CRP, IL-1, IL-6 and IL-10 contents of observation group were higher than those of normal control group;liver function indexes TBIL, ALT and AST contents were higher than those of normal control group;kidney function indexes Scr and BUN contents were higher than those of normal control group. Pearson test showed that the serum PSP and ChE contents in children with sepsis were directly correlated with the systemic inflammatory response as well as liver and renal function injury. Conclusion: Serum PSP content significantly increases while ChE content significantly decreases in children with sepsis and the specific change is directly correlated with the overall disease severity.展开更多
Objective:To investigate effects of hemoperfusion and hemofiltration combination on treating patients with acute organophosphours pesticide poisoning (AOPP) and influence of it on cholinesterase, dopamine and inflamma...Objective:To investigate effects of hemoperfusion and hemofiltration combination on treating patients with acute organophosphours pesticide poisoning (AOPP) and influence of it on cholinesterase, dopamine and inflammatory factors.Methods:A total of 82 cases of AOPP patients treated in our hospital from Sep 2012 to Jul 2016 were selected as subjects. They were randomly divided to be the observation group and the control group, 41 cases for each. For patients in observation group, combined therapy of hemoperfusion (HP) and hemofiltration (HF) were provided. For patients in control group, combined therapy of HP and hemodialysis (HD) were provided. Effects on the two groups of patients were compared. Meanwhile, cholinesterase, dopamine and inflammatory factors levels in different times before and after treatment were compared.Results:Consciousness improvement times and hospitalization times in observation group were significantly lower than in control group. No significant difference showed on fatality rates between the two groups. Before treatment, no significant difference showed on CHE and DE levels between two groups of patients;6 h and 12 h after treatment, CHE average levels in two groups were significantly higher than before treatment in the same group, and levels in observation group at the same phase were significantly higher than in control group;6 h and 12 h after treatment, DA levels in observation group were significantly lower than the same group before treatment, and significantly lower than control group, while 12 h after treatment, DA levels in control group were significantly lower than the same group before treatment. Before treatment, no significant difference showed on serum TGF-β1, TNF-α, IL-6, IL-8 between two groups of patients. After treatment, each index levels in two groups were significantly lower than the same group before treatment, and levels in observation group at the same phase were significantly lower than control group. Conclusion:Effects of blood purification therapy on treating AOPP were worth approving, but effects of HP and HF combined therapy were more significant. In addition, improvement of HP+HF on CHE, DA and inflammatory factors were better than HP+HD.展开更多
A novel Acetazolamide condensed 1,4-dihydropyridines was set up by treating of N-(5-acetamido-1,3,4-thiadiazol-2-ylsulfonyl)-3-oxobutanamide with an aryl aldehyde and 25-30%alkali with sight amount of barium nitrate a...A novel Acetazolamide condensed 1,4-dihydropyridines was set up by treating of N-(5-acetamido-1,3,4-thiadiazol-2-ylsulfonyl)-3-oxobutanamide with an aryl aldehyde and 25-30%alkali with sight amount of barium nitrate as a catalyst.Confirmation of the synthetic structure of the titled compounds(4-16)was substantiated by thin-layer chromatography(TLC),IR,^(1)H NMR,^(13)C NMR,Mass spectra(MS)and elemental analysis(C,H,and N)were finished.The titled compounds were assessed for anticholinesterase activity against acetylcholinesterase and butyl cholinesterase enzymes.The titled compound produced weak,moderate,or high anticholinesterase activity.Particularly,compound 8 demonstrated the best anticholinesterase activity of all the 1,4-dihydropyridines,with an IC_(50) estimation of 0.08μM and 2.9μM.展开更多
Due to their significant value in both economy and ecology,Daphnia had long been employed to investigate in vivo response of cholinesterase(ChE) in anticholinesterase exposures,whereas the type constitution and proper...Due to their significant value in both economy and ecology,Daphnia had long been employed to investigate in vivo response of cholinesterase(ChE) in anticholinesterase exposures,whereas the type constitution and property of the enzyme remained unclear.A type of ChE was purified from Daphnia magna using a three-step procedure,i.e.,Triton X-100 extraction,ammonium sulfate precipitation,and diethylaminoethyl(DEAE)-Sepharose Fast-Flow chromatography.According to sodium dodecyl sulfate polyacrylamide gel electrophoresis(SDS-PAGE),molecular mass of the purified ChE was estimated to be 84 kDa.Based on substrate studies,the purified enzyme preferred butyrylthiocholine iodide(BTCh) [with maximum velocity(Vmax)/Michaelis constant(Km)=8.428 L/(min·mg protein)] to acetylthiocholine iodide(ATCh) [with V max /Km =5.346 L/(min·mg protein)] as its substrate.Activity of the purified enzyme was suppressed by high concentrations of either ATCh or BTCh.Inhibitor studies showed that the purified enzyme was more sensitive towards inhibition by tetraisopropylpyrophosphoramide(iso-OMPA) than by 1,5-bis(4-allyldimethylammoniumphenyl) pentan-3-one dibromide(BW284C51).Result of the study suggested that the purified ChE was more like a type of pseudocholinesterase,and it also suggested that Daphnia magna contained multiple types of ChE in their bodies.展开更多
Background:Hand,foot,and mouth disease(HFMD)caused by enterovirus 71(EV71)is a potentially life-threatening infectious disease that commonly occurs in children.Diagnosis of HFMD caused by EV71 largely depends on clini...Background:Hand,foot,and mouth disease(HFMD)caused by enterovirus 71(EV71)is a potentially life-threatening infectious disease that commonly occurs in children.Diagnosis of HFMD caused by EV71 largely depends on clinical manifestations and rare serological biomarkers used to identify children suffering from HFMD.Serum cholinesterase(SChE)activity has frequently been reported as a potential biomarker for solid central nervous system tumors,chronic heart failure,and liver cirrhosis.However,its potential value in the diagnosis of neurotropic virus infections,such as HFMD caused by EV71,remains to be determined.Findings:In our study,220 children hospitalized with HFMD caused by EV71,34 inpatients infected with coxsackievirus A16(CVA16),and 43 undefined enterovirus-infected HFMD inpatients were recruited at the Anhui Provincial Children’s Hospital between January 2011 and December 2012.SChE activity was measured.The non-parametric Mann–Whitney U test showed that SChE activity in children diagnosed with HFMD caused by EV71 was significantly higher than in healthy controls(p<0.001),as well as in children with upper respiratory tract infections(p=0.011),bronchopneumonia(p<0.001),septicemia(p<0.001),amygdalitis(p<0.001),and appendicitis(p<0.001).In addition,higher SChE activity was observed in male inpatients with HFMD caused by EV71(47.7%positivity)compared to female inpatients(26.1%positivity)(chi-square test,p=0.002).In our study,no significant differences in SChE levels were observed among different ages(up to 120 months)(r=-0.112,p>0.05).An important finding was that SChE activity declined in the recovery phase of HFMD caused by EV71 compared to the acute phase(p<0.001).Conclusions:Elevated SChE activity was observed in patients with severe HFMD caused by EV71.Therefore,SChE might be a potential assistant biomarker for the diagnosis of HFMD caused by EV71 in children.展开更多
Objective:To screen the antioxidant,cholinesterase and tyrosinase enzymatic inhibition activities of the leaves and heartwood of Calophyllum symingtonianum(C.symingtonianum),and the bark of Calophyllum depressinervosu...Objective:To screen the antioxidant,cholinesterase and tyrosinase enzymatic inhibition activities of the leaves and heartwood of Calophyllum symingtonianum(C.symingtonianum),and the bark of Calophyllum depressinervosum(C.depressinervosum).Methods:Samples of leaves and heartwood of C.symingtonianum and bark of C.depressinervosum were tested for their total phenolic content and in vitro antioxidant assay by 2,2-diphenyl-1-picrylhydrazyl radical scavenging and β-carotene bleaching.Cholinesterase inhibition by Ellman’s method and tyrosinase inhibition using L-3,4-dihydroxyphenylalanine as a substrate were also tested.Results:All methanol extracts were found to exhibit strong 2,2-diphenyl-1-picrylhydrazyl radical scavenging effects.Extracts from the heartwood of C.symingtonianum gave a low IC50(5.17±0.04)μg/mL followed by bark of C.depressinervosum[(7.30±0.14)μg/mL]and C.symingtonianum leaves[(15.70±1.43)μg/mL].The methanol extract of C.depressinervosum bark showed 95.08%inhibition ofβ-carotene bleaching.All extracts showed moderate inhibition towards tyrosinase activity with an IC50 of more than 100μg/mL.The methanol extract of C.depressinervosum stem bark showed the highest inhibition(78.46%)against butyrylcholinesterase.Conclusions:These results showed that both Calophyllum species are potential sources of antioxidant and cholinesterase inhibitors.Further study is needed for the isolation and characterization of the active metabolites responsible for both activities.展开更多
Objective: To assess and compare the clinical efficacy and safety of cognitive enhancers(donepezil, galantamine, rivastigmine, and memantine) on cognition, behavior, function, and global status in patients with vascul...Objective: To assess and compare the clinical efficacy and safety of cognitive enhancers(donepezil, galantamine, rivastigmine, and memantine) on cognition, behavior, function, and global status in patients with vascular cognitive impairment.Data sources: The initial literature search was performed with PubMed, EMBASE, the Cochrane Methodology Register, the Cochrane Central Register of Controlled Trials, and Cumulative Index to Nursing & Allied Health(CINAHL) from inception to January 2018 for studies regarding donepezil, galantamine, rivastigmine, and memantine for treatment of vascular cognitive impairment.Data selection: Randomized controlled trials on donepezil, galantamine, rivastigmine, and memantine as monotherapy in the treatment of vascular cognitive impairment were included. A Bayesian network meta-analysis was conducted. Outcome measures: Efficacy was assessed by changes in scores of the Alzheimer's Disease Assessment Scale, cognitive subscale, Mini-Mental State Examination, Neuropsychiatric Inventory scores and Clinician's Interview-Based Impression of Change Scale Plus Caregiver's Input, Activities of Daily Living, the Clinical Dementia Rating scale. Safety was evaluated by mortality, total adverse events(TAEs), serious adverse events(SAEs), nausea, vomiting. diarrhea, or cerebrovascular accidents(CVAs). Results: After screening 1717 citations, 12 randomized controlled trials were included. Donepezil and rivastigmine(mean difference(e) = –0.77, 95% confidence interval(CI): 0.25–1.32; MD = 1.05, 95% CI: 0.18–1.79) were significantly more effective than placebo in reducing Mini-Mental State Examination scores. Donepezil, galantamine, and memantine(MD = –1.30, 95% CI: –2.27 to –0.42; MD = –1.67, 95% CI: –3.36 to –0.06; MD = –2.27, 95% CI: –3.91 to –0.53) showed superior benefits on the Alzheimer's Disease Assessment Scale–cognitive scores compared with placebo. Memantine(MD = 2.71, 95% CI: 1.05–7.29) improved global status(Clinician's Interview-Based Impression of Change Scale Plus Caregiver's Input) more than the placebo. Safety results revealed that donepezil 10 mg(odds ratio(OR) = 3.04, 95% CI: 1.86–5.41) contributed to higer risk of adverse events than placebo. Galantamine(OR = 5.64, 95% CI: 1.31–26.71) increased the risk of nausea. Rivastigmine(OR = 16.80, 95% CI: 1.78–319.26) increased the risk of vomiting. No agents displayed a significant risk of serious adverse events, mortality, cerebrovascular accidents, or diarrhea.Conclusion: We found significant efficacy of donepezil, galantamine, and memantine on cognition. Memantine can provide significant efficacy in global status. They are all safe and well tolerated.展开更多
BACKGROUND: Paraoxonase 1(PON1) is an ester hydro- lase in serum and in the liver. Studies have suggested that PON1 measurement to the current battery of tests may im- prove the evaluation of chronic liver diseases. T...BACKGROUND: Paraoxonase 1(PON1) is an ester hydro- lase in serum and in the liver. Studies have suggested that PON1 measurement to the current battery of tests may im- prove the evaluation of chronic liver diseases. The aim of this study was to investigate the clinical significance of mo- nitoring the level of serum PON1 activity in liver transplan- tation patients. METHODS: A series of biochemical indexes were moni- tored in preoperative, operative and postoperative serum samples of 17 liver-transplanted patients. The change of se- rum PON1 level and its relations with other biochemical in- dexes were analyzed. RESULTS: PON1 was distributed normally in the healthy population and its reference value ranged from 45.5 to 265.8 U/mL. The PON1 level of all patients was lower than that of control group significantly (P<0.001); the level be- gan to elevate continuously 5 minutes after opening of the portal vein and was higher than that 90 minutes after open- ing of the portal vein ( P <0.05). Two days after operation it was still higher than the normal. The levels of serum ALT and AST elevated more significantly after opening of the portal vein than before operation and they were higher than the normal values till 2 days after the operation. CONCLUSIONS: The level of PON1 in serum may be taken as one of the effective indexes to assess whether the implant is alive and to monitor liver function of the patient together with other tests.展开更多
BACKGROUND:The aim of the present study is to describe the clinical correlates of hypotension and its associated outcomes in patients with acute organophosphorus poisoning(AOPP).METHODS:In this retrospective cohort st...BACKGROUND:The aim of the present study is to describe the clinical correlates of hypotension and its associated outcomes in patients with acute organophosphorus poisoning(AOPP).METHODS:In this retrospective cohort study,we analyzed data pertaining to 871 patients with AOPP who were treated at two hospitals.Data from hypotensive and non-hypotensive patients were compared to identify clinical correlates of hypotension.We also evaluated the association between clinical parameters(including hypotension)and in-hospital mortality.RESULTS:The incidence of hypotension in AOPP patients was 16.4%.Hypotensive patients showed signifi cantly higher in-hospital mortality(1.1%vs.39.9%,P<0.001).Advanced age(odds ratio[OR]1.25,95%confi dence interval[CI]1.08–1.44),history of diabetes(OR 2.65,95%CI 1.14–5.96),and increased white blood cell count(OR 1.06,95%CI 1.03–1.09),plasma cholinesterase(OR 0.91,95%CI 0.84–0.94),plasma albumin(OR 0.88,95%CI 0.85–0.92),serum amylase(OR 1.01,95%CI 1.01–1.02),and blood pH(OR 0.64,95%CI 0.54–0.75)were signifi cantly associated with hypotension.After adjusting for potential confounders,hypotension was associated with increased in-hospital mortality(hazard ratio 8.77–37.06,depending on the controlled variables).CONCLUSIONS:Hypotension is a common complication of AOPP and is associated with increased in-hospital mortality.Advanced age,history of diabetes,and changes in laboratory parameters were associated with hypotension in AOPP patients.展开更多
Objective:To evaluate the effect of different doses of lead acetate(1/20,1/40 and 1/60 of LD_(50))on body weight gain,blood picture,plasma prolein profile and the function of liver,kidney and thyroid gland.Methods:Mal...Objective:To evaluate the effect of different doses of lead acetate(1/20,1/40 and 1/60 of LD_(50))on body weight gain,blood picture,plasma prolein profile and the function of liver,kidney and thyroid gland.Methods:Male albino rats were divided into four groups,the first group represented the health control animals,while the second,third and fourth groups were ingested orally with sub lethal doses of load acetate(1/20,1/40 and 1/60)of the oral LD_(50),respectively.One dose was ingested every two days during the experimental period(14 weeks)including the adaptation time.Blood was collected and used for all analysis.Results:The results showed that,the ingestion of Pb^(2+)induced significant stimulation in glutamic-pyruvic transaminase(ALT)and glutamic-oxalacetic transaminease(AST)activity.Also,total soluble protein and albumin contents of plasma were significantly decreased,while the content of globulin was changed by the Pb^(2+)treatments.The cholinesteiase activity was inhibited,but the activities of alkaline and acid phosphates and lactate dehydrogenase were stimulated,while plasma glucose level was elevated as a result of lead acetate intoxication.In case of blood picture,Pb^(2+)ingestion reduced the contents of hemoglobin and RBCs count of intoxicated rat's blood and the plasma levels of T3,T4 and blood WBCs count were decreased.Conclusions:It can be concluded that lead acetate has harmful effect on experimental male albino rats.Therefore,the present work advises people to prevent exposure to the lead compound to avoid injurious hazard risk.展开更多
A novel quartz crystal microbalance (QCM) biosensor for the determination of organophosphorus pesticide,such as dichlorvos (DDVP),has been fabricated with poly (3,4-ethylenedioxythiophene)/Poly (4-styrenesulfonate) (P...A novel quartz crystal microbalance (QCM) biosensor for the determination of organophosphorus pesticide,such as dichlorvos (DDVP),has been fabricated with poly (3,4-ethylenedioxythiophene)/Poly (4-styrenesulfonate) (PEDOT/PSS) and cholinesterase butyl (BuChE).It is found that PEDOT/PSS coated sensor exhibits the highest sensitivity for DDVP among PEDOT,polyvinyl pyrrolidone,polyvinyl alcohol and polyacrylic acid sensor series.The conditions to prepare PEDOT/PSS coated sensor are optimized.The sensitivity of the PEDOT/PSS hiosensor with BuChE is higher than the others without BuChE The determination of dichlorvos in the range from 400μg/g to 2400μg/g used PEDOT/PSS with BuChE coated hiosensor was obtained.展开更多
文摘Acetylcholine is an essential neurotransmitter found throughout the nervous system. Its action on postsynaptic receptors is regulated through hydrolysis by various carboxylesterases, especially cholinesterases (ChEs). The acute toxicity of organophosphate (OP) compounds is directly linked to their action as inhibitors of ChE. One widely used assay for evaluating ChE activity is a spectrophotometric method developed by Ellman et al. When the enzyme source is from tissues or, in particular, blood, hemoglobin displays a spectrophotometric peak at the same wave-length used to analyze cholinergic activity. This creates a substantial background that interferes with the Ellman’s assay and must be overcome in order to accurately monitor cholinesterase activity. Herein, we directly compare blood processing methods: classical method (1.67 ± 0.30 U/mL) and HemogloBindTM treatment (1.51 ± 0.17 U/mL), and clearly demonstrate that pretreatment of blood samples with HemoglobindTM is both a sufficient and rapid sample preparation method for the assessment of ChE activity using the Ellman’s method.
文摘AIM To examine whether nizatidine stimulatesduodenal HCO<sub>3</sub><sup>-</sup> secretion in rats by inhibitingAChE activity.METHODS Under pentobarbital anesthesia,aproximal duodenal loop was perfused withsaline,and the HCO<sub>3</sub> secretion was measuredat pH 7.0 using a pH-stat method and by adding10mM HCI.Nizatidine,neostigmine,carbacholor famotidine was administered i.v.as a singleinjection.RESULTS Intravenous administration ofnizatidine（3-30 mg/kg）dose-dependentlyincreased duodenal HCO<sub>3</sub><sup>-</sup> secretion,and theeffect at 10mg/kg was equivalent to thatobtained by carbachol at 0.01 mg/kg.Thisnizatidine action was observed at the same doserange that inhibited acid secretion and enhancedgastric motility,mimicked by i.v.injection ofneostigmine（0.03 mg/kg）,and significantlyattenuated by bilateral vagotomy and prior s.c.administration of atropine but not byindomethacin,a cyclooxygenase inhibitor,orN<sup>G</sup>-nitro-L-arginine methyl ester,a NO synthaseinhibitor.The HCO<sub>3</sub><sup>-</sup> secretory response toacetylcholine（0.001 mg/kg）was significantlypotentiated by the concurrent administration ofnizatidine（3mg/kg,i.v.）.The IC<sub>50</sub>of nizatidine for AChE of rat erythrocytes was1.4×10<sup>-6</sup>M,about 12 times higher than that ofneostigmine.Neither famotidine(】10<sup>-3</sup>M,30mg/kg,i.v.)nor cisapride(】 10<sup>-3</sup>M,3mg/kg,i.v.)had any influence on AChEactivity or duodenal HCO<sub>3</sub><sup>-</sup> secretion.Duodenaldamage induced by acid perfusion（100 mM HCIfor 4 h）in the presence of indomethacin wassignificantly prevented by nizatidine andneostigmine,at the doses that increased theHCO<sub>3</sub><sup>-</sup> secretion.CONCLUSION Nizatidine stimulates duodenalHCO<sub>3</sub><sup>-</sup> secretion,in both vagal-dependent andatropine-sensitive manners,and the action isassociated with the anti-AChE activity of thisagent.
基金the Scientific and Technological Research Council of Turkey(TUBITAK)for the scholarship provided her for Ph.D.program
文摘Objective:To explore cholinesterase inhibitory and antioxidant effect of six coniferous trees(Abies bornmulleriana,Picea pungens,Juniperus communis,Cedrus libani,Taxus baccata,and Cupressus sempervirens var.horizantalis).Methods:Acetone(Ace),ethyl acetate(EtOAc),and ethanol(EtOH)extracts prepared from the needles and shoots of the six coniferous trees were screened for their acetylcholinesterase(AChE)and butyrylcholinesterasc(BChE)inhibitory activity at 100μg/mL.Antioxidant activity of the extracts was tested using 2,2-diphenyl-1-picrylhydrazyl(DPPH)and N,N-dimethyl-p-phenylendiamine(DMPD)radical scavenging,nietal-chelation capacity,ferric-(FRAP)and phosphomolibdenum-reducing antioxidant power(PRAP)assays.All of the assays were performed in ELISA microplate reader.Total phenol and flavonoid amounts in the extracts were determined spectrophotometrically.Results:Among thirty-six extracts in total,the shoot-Ace extract of Cupressus sempervirens var.horizantalis exerted the highest inhibition against AChE[(54.84±2.51)%],while the needle-Ace extract of Cedrus libani was the most effective in inhibiting BChE[(67.54±0.30)%].The highest DPPH radical scavenging effect,FRAP and PRAP was observed in the shoot-Ace and EtOAc extracts from Taxus baccata.whereas all the extracts showed a variable degree of scavenging effect against DPMD radical.The shoot-EtOAc extract of Cedrus libani had the highest metalchelation capacity[(58.04±0.70)%].The shoot extracts of Taxus baccata were determined to have the richest total phenol content,which may contribute to its marked antioxidant activity.Conclusions:The conifer species screened in this study may contain cholinesterase-inhibiting and antioxidant properties,which might be useful against Alzheimer's disease.
文摘Objective:To investigate the effect of Cannabis sativa resin and/or tramadol,two commonly drugs of abuse on acetylcholinesterase and butyrylcholinesterase activities as a possible cholinergic biomarkers of neurotoxicity induced by these agents.Methods:rats were treated with cannabis resin(5,10 or 20 mg/kg)(equivalent to the active constituent A'-tetrahydrocannabinol),tramadol(5,10 and 20 mg/kg) or tramadol(10 mg/kg)combined with cannabis resin(5,10 and 20 mg/kg) subcutaneously daily for 6 weeks.Acetylcholinesterase(AChE) and butyrylcholinesterase(BChE) activities were measured in brain and serum.We also measured the activity of paraoxonase-1(PONl) in serum of rats treated with these agents.Results:(i) AChE activity in brain increased after 10-20 mg/kg cannabis resin(by 16.3%-36.5%).AChE activity in brain did not change after treatment with 5-20 mg/kg tramadol.The administration of both cannabis resin(5,10 or 20 mg/kg) and tramadol(10 mg/kg) resulted in decreased brain AChE activity by 14.1%,12.9%and 13.6%,respectively;(ii) BChE activity in serum was markedly and dose-dependenlly inhibited by cannabis resin(by 60.9%-76.9%).BChE activity also decreased by 17.6%-36.5%by 10-20mg/kg tramadol and by 57.2%-63.9%by the cannabis resin/tramadol combined treatment;(iii)Cannabis resin at dose of 20 mg/kg increased serum PONl activity by 25.7%.In contrast,tramadol given at 5,10 and 20 mg/kg resulted in a dose-dependent decrease in serum PON1 activity by 19%,36.7%,and 46.1%,respectively.Meanwhile,treatment with cannabis resin plus tramadol resulted in 40.2%,35.8%,30.7%inhibition of PONl activity compared to the saline group.Conclusions:these data suggest that cannabis resin exerts different effects on AChE and BChE activities which could contribute to the memory problems and the decline in cognitive function in chronic users.
文摘Two novel naphthol derivatives(1 and 2) were synthesized and characterized via IR,~1H NMR,and HRMS.The structure of compound 2 was verified by single-crystal X-ray crystallography.It crystallizes in monoclinic,space group C2/c with a = 21.6725(9),b = 6.0127(3),c = 25.5405(14) ?,β = 94.716(5)o,V = 3316.9(3) ?~3,Z = 8,F(000) = 1384,D_c = 1.511 Mg/m^3,M_r = 377.22 and μ = 2.487 mm^(-1).In addition,their cholinesterase inhibitory activities in vitro toward Electrophorus electricus acetylcholinesterase(eel ACh E) and horse serum butyrylcholinesterase(eq BCh E) were further determined.The results showed that compound 1 as a new acetylcholinesterase(ACh E) inhibitor displayed higher ACh E inhibitory activity(IC_(50) = 1.4 μM),which could be considered for Alzheimer's disease therapeutics.
文摘Introduction: Dementia is frequently associated with Parkinson’s disease, especially in later stages. Efficacy of cholinesterase inhibitors (ChI) in Alzheimer’s dementia is well established. However, treatment with ChI in Parkinson’s disease dementia (PDD) remains controversial. The objective of this systematic review and meta-analysis was to assess the effects of ChI in PDD. Methods: A comprehensive literature search was performed in MEDLINE, EMBASE and Cochrane library up to March 2014 using the descriptors “Parkinson’s disease”, “dementia in Parkinson’s disease”, “cognition”, “acetylcholinesterase inhibitors”, “cholinesterase inhibitors”, “anticholinesterase agents”, “rivastigmine”, “donepezil” and “galantamine” (Pubmed search strategy). All randomized, doubleblinded, placebo-controlled trials that met the eligibility criteria and assessed the effects of ChI in PDD were considered for analysis. There were no restrictions regarding paper language. Summary effect-sizes were presented as standardized mean differences (SMD) and the pooled analysis was performed with a fixed-effects model. Outcomes considered for analysis were the Mini Mental Status Exam (MMSE) score and the cognition scale for evaluation of dementia ADAS-Cog. The degree of heterogeneity between included studies was assessed through the I2 test. Results: After a comprehensive search, 175 references were retrieved. From these, five randomized trials involving 946PDD subjects were included in the review. Four studies used donepezil and only one study used rivastigmine. The pooled analysis of five studies that assessed the effects of ChI in MMSE total score showed a SMD of 0.24 (CI 95% 0.11 - 0.38). Three studies considered the effects of ChI on Adas-Cog and the pooled results showed a SMD of 0.21 (CI 95% 0.07 - 0.35). There was no significant heterogeneity between the studies. Conclusions: The results of this systematic review and meta- analysis suggest that ChI improves cognitive impairment in PDD subjects. Despite statistically significant, the translation of these results into relevant clinical improvement should be taken with caution, as the studies did not address what would be considered a clinically significant result.
文摘Cholinergic dysfunction is common to Alzheimer’s dementia and Schizophrenia. The objective of this study is to undertake a systematic review and meta-analysis of the literature on the cognitive and clinical effects of cholinesterase inhibitors administered to patients with schizophrenia and co-morbid Alzheimer’s disease dementia. A literature search of the MEDLINE, CINAHL, PubMed, PsycINFO, EMBASE, AMED, BNI, HMIC and Health Business Elite databases has been performed (up to January 2013) to investigate the use of cholinesterase inhibitors in patients with schizophrenia and dementia. The terms “schizophrenia”, “dementia”, “rivastigmine”, “donepezil”, “galantamine” and “cognitive deficit” have been searched, with a restriction for English language. Five published studies including 1 RCT have been included for the qualitative review. Treatments include Donepezil 5 mg and 10 mg as well as Rivastigmine 9 mg. The numbers of participants vary from 2 incase report to20 inthe RCT. Only 1 study qualifies for meta-analysis. There is a very limited evidence on the efficacy and safety of using acetylcholinesterase inhibitors in the management of dementia co-morbid with schizophrenia. The only randomised controlled study shows lack of evidence in terms of efficacy in using cholinesterase inhibitors in the management of dementia with schizophrenia. Future research projects will have to look at an adequate sample size to explore treatment on various cognitive and noncognitive domains and the sample should be selected by using definitive and internationally acceptable diagnostic criteria.
文摘<strong>Objective:</strong> To evaluate early prediction value of IPS<span> </span><span><span style="font-family:Verdana;">combined with SchE and D-dimer detection for infection and survival in critically ill patients. </span><b><span style="font-family:Verdana;">Methods:</span></b></span><b><span> </span></b><span style="font-family:Verdana;">199 critically ill patients admitted to the emergency intensive care unit (EICU) of our hospital from December 2018 to December 2019 were retrospectively analyzed, including 110 infection patients (infection group) and 89 non-infection</span><span> </span><span style="font-family:Verdana;">patients (non-infection group).</span><span> </span><span><span style="font-family:Verdana;">According to the survival, the infection group was divided into death group (68 cases) and survival group (42 cases). The IPS, APACHE II, SOFA and SchE, D-dimer expression levels were detected and compared;Univariate and logistic regression analysis were used to evaluate the independent prognostic factors. </span><b><span style="font-family:Verdana;">Results: </span></b><span style="font-family:Verdana;">The IPS and APACHE II of patients in the infected group were higher than those in the non-infected group, the level of SchE was lower than that in the non-infected group, and the level of D-dimer was higher than that in the non-infected group (</span><i><span style="font-family:Verdana;">P</span></i></span><i><span> </span></i><span style="font-family:Verdana;"><</span><span> </span><span style="font-family:Verdana;">0.001). IPS, SOFA, APACHE</span><span style="font-family:Verdana;"> II</span><span style="font-family:Verdana;">, SchE, D-dimer, invasive mechanical ventilation, septic shock, and ICU length</span><span style="font-family:Verdana;"> of stay had significant influence on the prognosis of critically ill patients</span><span> </span><span><span style="font-family:Verdana;">(</span><i><span style="font-family:Verdana;">P</span></i></span><i><span> </span></i><span style="font-family:Verdana;"><</span><span> </span><span><span style="font-family:Verdana;">0.001). Logistic regression analysis showed that IPS (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 2.821, </span><span><span style="font-family:Verdana;">95%</span><i><span style="font-family:Verdana;"> CI</span></i></span><span style="font-family:Verdana;"> 1.501</span></span><span style="font-family:Verdana;"> - </span><span><span style="font-family:Verdana;">5.227), SOFA (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 5.078, </span><span><span style="font-family:Verdana;">95% </span><i><span style="font-family:Verdana;">CI</span></i></span><span style="font-family:Verdana;"> 3.327 </span></span><span style="font-family:Verdana;">-</span><span><span style="font-family:Verdana;"> 7.690), APACHE II (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 14.308, </span><span><span style="font-family:Verdana;">95% </span><i><span style="font-family:Verdana;">CI</span></i></span><span style="font-family:Verdana;"> 8.901 </span></span><span style="font-family:Verdana;">-</span><span><span style="font-family:Verdana;"> 21.893), SchE (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 0.223, </span><span><span style="font-family:Verdana;">95%</span><i><span style="font-family:Verdana;"> CI</span></i></span><span style="font-family:Verdana;"> 0.165 </span></span><span style="font-family:Verdana;">-</span><span style="font-family:Verdana;"> 0.291), D-dimer</span><span style="font-family:Verdana;"> (</span><i><span style="font-family:Verdana;">OR</span></i><i><span> </span></i><span style="font-family:Verdana;">=</span><span> </span><span style="font-family:Verdana;">2.10</span><span style="font-family:Verdana;">, </span><span style="font-family:Verdana;">95%</span><i><span> </span></i><i><span style="font-family:Verdana;">CI</span></i><i><span> </span></i><span style="font-family:Verdana;">1.55</span><span style="font-family:Verdana;"> - </span><span style="font-family:Verdana;">2.85</span><span style="font-family:Verdana;">)</span><span><span style="font-family:Verdana;">, septic shock (</span><i><span style="font-family:Verdana;">OR</span></i><span style="font-family:Verdana;"> = 9.948,</span></span><span> </span><span style="font-family:Verdana;">95%</span><span> </span><i><span style="font-family:Verdana;">CI</span></i><span style="font-family:Verdana;"> 7.012</span><span style="font-family:Verdana;"> - </span><span style="font-family:Verdana;">17.012)</span><span> </span><span style="font-family:Verdana;">were independent factors affecting the prognosis of critically ill patients with infection</span><span style="font-family:Verdana;"> (</span><i><span style="font-family:Verdana;">P</span></i><span> </span><span style="font-family:Verdana;"><</span><span> </span><span style="font-family:Verdana;">0.001</span><span style="font-family:Verdana;">)</span><span style="font-family:Verdana;">.</span><span> </span><b><span style="font-family:Verdana;">Conclusion:</span></b><b><span> </span></b><span style="font-family:Verdana;">IPS and D-dimer expression level in infected patients were increased and SchE decreased significantly compared with those in non-infected patients, and they significantly correlated with</span><span> </span><span style="font-family:Verdana;">disease severity of infected</span><span> </span><span style="font-family:Verdana;">patients</span><span> </span><span style="font-family:Verdana;">and could be early prediction</span><span> </span><span style="font-family:Verdana;">for prognosis.</span>
文摘Objective: To study the changes of serum pancreatic stone protein (PSP) and cholinesterase (ChE) contents in children with sepsis and their correlation with systemic inflammatory response and target organ damage. Methods: A total of 64 children with sepsis who were treated in the hospital between January 2015 and January 2017 were selected as observation group, and 50 healthy children who received vaccination in the hospital during the same period were selected as normal control group. The contents of PSP, ChE, inflammatory factors as well as liver and kidney function indexes in the two groups were detected. Pearson test was used to assess the correlation of serum PSP and ChE contents with systemic inflammatory response and target organ damage in children with sepsis. Results: Serum PSP content of observation group was higher than that of control group while ChE content was lower than that of control group;serum inflammatory factors PCT, CRP, IL-1, IL-6 and IL-10 contents of observation group were higher than those of normal control group;liver function indexes TBIL, ALT and AST contents were higher than those of normal control group;kidney function indexes Scr and BUN contents were higher than those of normal control group. Pearson test showed that the serum PSP and ChE contents in children with sepsis were directly correlated with the systemic inflammatory response as well as liver and renal function injury. Conclusion: Serum PSP content significantly increases while ChE content significantly decreases in children with sepsis and the specific change is directly correlated with the overall disease severity.
文摘Objective:To investigate effects of hemoperfusion and hemofiltration combination on treating patients with acute organophosphours pesticide poisoning (AOPP) and influence of it on cholinesterase, dopamine and inflammatory factors.Methods:A total of 82 cases of AOPP patients treated in our hospital from Sep 2012 to Jul 2016 were selected as subjects. They were randomly divided to be the observation group and the control group, 41 cases for each. For patients in observation group, combined therapy of hemoperfusion (HP) and hemofiltration (HF) were provided. For patients in control group, combined therapy of HP and hemodialysis (HD) were provided. Effects on the two groups of patients were compared. Meanwhile, cholinesterase, dopamine and inflammatory factors levels in different times before and after treatment were compared.Results:Consciousness improvement times and hospitalization times in observation group were significantly lower than in control group. No significant difference showed on fatality rates between the two groups. Before treatment, no significant difference showed on CHE and DE levels between two groups of patients;6 h and 12 h after treatment, CHE average levels in two groups were significantly higher than before treatment in the same group, and levels in observation group at the same phase were significantly higher than in control group;6 h and 12 h after treatment, DA levels in observation group were significantly lower than the same group before treatment, and significantly lower than control group, while 12 h after treatment, DA levels in control group were significantly lower than the same group before treatment. Before treatment, no significant difference showed on serum TGF-β1, TNF-α, IL-6, IL-8 between two groups of patients. After treatment, each index levels in two groups were significantly lower than the same group before treatment, and levels in observation group at the same phase were significantly lower than control group. Conclusion:Effects of blood purification therapy on treating AOPP were worth approving, but effects of HP and HF combined therapy were more significant. In addition, improvement of HP+HF on CHE, DA and inflammatory factors were better than HP+HD.
文摘A novel Acetazolamide condensed 1,4-dihydropyridines was set up by treating of N-(5-acetamido-1,3,4-thiadiazol-2-ylsulfonyl)-3-oxobutanamide with an aryl aldehyde and 25-30%alkali with sight amount of barium nitrate as a catalyst.Confirmation of the synthetic structure of the titled compounds(4-16)was substantiated by thin-layer chromatography(TLC),IR,^(1)H NMR,^(13)C NMR,Mass spectra(MS)and elemental analysis(C,H,and N)were finished.The titled compounds were assessed for anticholinesterase activity against acetylcholinesterase and butyl cholinesterase enzymes.The titled compound produced weak,moderate,or high anticholinesterase activity.Particularly,compound 8 demonstrated the best anticholinesterase activity of all the 1,4-dihydropyridines,with an IC_(50) estimation of 0.08μM and 2.9μM.
基金Project supported by the Zhejiang Provincial Natural Science Foundation of China(No.LY12B07008)the Department of Education of Zhejiang Province,China(No.20070138)
文摘Due to their significant value in both economy and ecology,Daphnia had long been employed to investigate in vivo response of cholinesterase(ChE) in anticholinesterase exposures,whereas the type constitution and property of the enzyme remained unclear.A type of ChE was purified from Daphnia magna using a three-step procedure,i.e.,Triton X-100 extraction,ammonium sulfate precipitation,and diethylaminoethyl(DEAE)-Sepharose Fast-Flow chromatography.According to sodium dodecyl sulfate polyacrylamide gel electrophoresis(SDS-PAGE),molecular mass of the purified ChE was estimated to be 84 kDa.Based on substrate studies,the purified enzyme preferred butyrylthiocholine iodide(BTCh) [with maximum velocity(Vmax)/Michaelis constant(Km)=8.428 L/(min·mg protein)] to acetylthiocholine iodide(ATCh) [with V max /Km =5.346 L/(min·mg protein)] as its substrate.Activity of the purified enzyme was suppressed by high concentrations of either ATCh or BTCh.Inhibitor studies showed that the purified enzyme was more sensitive towards inhibition by tetraisopropylpyrophosphoramide(iso-OMPA) than by 1,5-bis(4-allyldimethylammoniumphenyl) pentan-3-one dibromide(BW284C51).Result of the study suggested that the purified ChE was more like a type of pseudocholinesterase,and it also suggested that Daphnia magna contained multiple types of ChE in their bodies.
基金supported by the National Natural Science Foundation of China(No:81271826).
文摘Background:Hand,foot,and mouth disease(HFMD)caused by enterovirus 71(EV71)is a potentially life-threatening infectious disease that commonly occurs in children.Diagnosis of HFMD caused by EV71 largely depends on clinical manifestations and rare serological biomarkers used to identify children suffering from HFMD.Serum cholinesterase(SChE)activity has frequently been reported as a potential biomarker for solid central nervous system tumors,chronic heart failure,and liver cirrhosis.However,its potential value in the diagnosis of neurotropic virus infections,such as HFMD caused by EV71,remains to be determined.Findings:In our study,220 children hospitalized with HFMD caused by EV71,34 inpatients infected with coxsackievirus A16(CVA16),and 43 undefined enterovirus-infected HFMD inpatients were recruited at the Anhui Provincial Children’s Hospital between January 2011 and December 2012.SChE activity was measured.The non-parametric Mann–Whitney U test showed that SChE activity in children diagnosed with HFMD caused by EV71 was significantly higher than in healthy controls(p<0.001),as well as in children with upper respiratory tract infections(p=0.011),bronchopneumonia(p<0.001),septicemia(p<0.001),amygdalitis(p<0.001),and appendicitis(p<0.001).In addition,higher SChE activity was observed in male inpatients with HFMD caused by EV71(47.7%positivity)compared to female inpatients(26.1%positivity)(chi-square test,p=0.002).In our study,no significant differences in SChE levels were observed among different ages(up to 120 months)(r=-0.112,p>0.05).An important finding was that SChE activity declined in the recovery phase of HFMD caused by EV71 compared to the acute phase(p<0.001).Conclusions:Elevated SChE activity was observed in patients with severe HFMD caused by EV71.Therefore,SChE might be a potential assistant biomarker for the diagnosis of HFMD caused by EV71 in children.
基金Supported by the Ministry of Higher Education Malaysia(Grant No.GUP2526.06H34).
文摘Objective:To screen the antioxidant,cholinesterase and tyrosinase enzymatic inhibition activities of the leaves and heartwood of Calophyllum symingtonianum(C.symingtonianum),and the bark of Calophyllum depressinervosum(C.depressinervosum).Methods:Samples of leaves and heartwood of C.symingtonianum and bark of C.depressinervosum were tested for their total phenolic content and in vitro antioxidant assay by 2,2-diphenyl-1-picrylhydrazyl radical scavenging and β-carotene bleaching.Cholinesterase inhibition by Ellman’s method and tyrosinase inhibition using L-3,4-dihydroxyphenylalanine as a substrate were also tested.Results:All methanol extracts were found to exhibit strong 2,2-diphenyl-1-picrylhydrazyl radical scavenging effects.Extracts from the heartwood of C.symingtonianum gave a low IC50(5.17±0.04)μg/mL followed by bark of C.depressinervosum[(7.30±0.14)μg/mL]and C.symingtonianum leaves[(15.70±1.43)μg/mL].The methanol extract of C.depressinervosum bark showed 95.08%inhibition ofβ-carotene bleaching.All extracts showed moderate inhibition towards tyrosinase activity with an IC50 of more than 100μg/mL.The methanol extract of C.depressinervosum stem bark showed the highest inhibition(78.46%)against butyrylcholinesterase.Conclusions:These results showed that both Calophyllum species are potential sources of antioxidant and cholinesterase inhibitors.Further study is needed for the isolation and characterization of the active metabolites responsible for both activities.
基金supported by the Natural Science Foundation of Liaoning Province of China,No.20170541036(to HYL)
文摘Objective: To assess and compare the clinical efficacy and safety of cognitive enhancers(donepezil, galantamine, rivastigmine, and memantine) on cognition, behavior, function, and global status in patients with vascular cognitive impairment.Data sources: The initial literature search was performed with PubMed, EMBASE, the Cochrane Methodology Register, the Cochrane Central Register of Controlled Trials, and Cumulative Index to Nursing & Allied Health(CINAHL) from inception to January 2018 for studies regarding donepezil, galantamine, rivastigmine, and memantine for treatment of vascular cognitive impairment.Data selection: Randomized controlled trials on donepezil, galantamine, rivastigmine, and memantine as monotherapy in the treatment of vascular cognitive impairment were included. A Bayesian network meta-analysis was conducted. Outcome measures: Efficacy was assessed by changes in scores of the Alzheimer's Disease Assessment Scale, cognitive subscale, Mini-Mental State Examination, Neuropsychiatric Inventory scores and Clinician's Interview-Based Impression of Change Scale Plus Caregiver's Input, Activities of Daily Living, the Clinical Dementia Rating scale. Safety was evaluated by mortality, total adverse events(TAEs), serious adverse events(SAEs), nausea, vomiting. diarrhea, or cerebrovascular accidents(CVAs). Results: After screening 1717 citations, 12 randomized controlled trials were included. Donepezil and rivastigmine(mean difference(e) = –0.77, 95% confidence interval(CI): 0.25–1.32; MD = 1.05, 95% CI: 0.18–1.79) were significantly more effective than placebo in reducing Mini-Mental State Examination scores. Donepezil, galantamine, and memantine(MD = –1.30, 95% CI: –2.27 to –0.42; MD = –1.67, 95% CI: –3.36 to –0.06; MD = –2.27, 95% CI: –3.91 to –0.53) showed superior benefits on the Alzheimer's Disease Assessment Scale–cognitive scores compared with placebo. Memantine(MD = 2.71, 95% CI: 1.05–7.29) improved global status(Clinician's Interview-Based Impression of Change Scale Plus Caregiver's Input) more than the placebo. Safety results revealed that donepezil 10 mg(odds ratio(OR) = 3.04, 95% CI: 1.86–5.41) contributed to higer risk of adverse events than placebo. Galantamine(OR = 5.64, 95% CI: 1.31–26.71) increased the risk of nausea. Rivastigmine(OR = 16.80, 95% CI: 1.78–319.26) increased the risk of vomiting. No agents displayed a significant risk of serious adverse events, mortality, cerebrovascular accidents, or diarrhea.Conclusion: We found significant efficacy of donepezil, galantamine, and memantine on cognition. Memantine can provide significant efficacy in global status. They are all safe and well tolerated.
文摘BACKGROUND: Paraoxonase 1(PON1) is an ester hydro- lase in serum and in the liver. Studies have suggested that PON1 measurement to the current battery of tests may im- prove the evaluation of chronic liver diseases. The aim of this study was to investigate the clinical significance of mo- nitoring the level of serum PON1 activity in liver transplan- tation patients. METHODS: A series of biochemical indexes were moni- tored in preoperative, operative and postoperative serum samples of 17 liver-transplanted patients. The change of se- rum PON1 level and its relations with other biochemical in- dexes were analyzed. RESULTS: PON1 was distributed normally in the healthy population and its reference value ranged from 45.5 to 265.8 U/mL. The PON1 level of all patients was lower than that of control group significantly (P<0.001); the level be- gan to elevate continuously 5 minutes after opening of the portal vein and was higher than that 90 minutes after open- ing of the portal vein ( P <0.05). Two days after operation it was still higher than the normal. The levels of serum ALT and AST elevated more significantly after opening of the portal vein than before operation and they were higher than the normal values till 2 days after the operation. CONCLUSIONS: The level of PON1 in serum may be taken as one of the effective indexes to assess whether the implant is alive and to monitor liver function of the patient together with other tests.
基金approved by the Medical Ethics Committee of the First Hospital of Jilin University(approval number:2018-146).
文摘BACKGROUND:The aim of the present study is to describe the clinical correlates of hypotension and its associated outcomes in patients with acute organophosphorus poisoning(AOPP).METHODS:In this retrospective cohort study,we analyzed data pertaining to 871 patients with AOPP who were treated at two hospitals.Data from hypotensive and non-hypotensive patients were compared to identify clinical correlates of hypotension.We also evaluated the association between clinical parameters(including hypotension)and in-hospital mortality.RESULTS:The incidence of hypotension in AOPP patients was 16.4%.Hypotensive patients showed signifi cantly higher in-hospital mortality(1.1%vs.39.9%,P<0.001).Advanced age(odds ratio[OR]1.25,95%confi dence interval[CI]1.08–1.44),history of diabetes(OR 2.65,95%CI 1.14–5.96),and increased white blood cell count(OR 1.06,95%CI 1.03–1.09),plasma cholinesterase(OR 0.91,95%CI 0.84–0.94),plasma albumin(OR 0.88,95%CI 0.85–0.92),serum amylase(OR 1.01,95%CI 1.01–1.02),and blood pH(OR 0.64,95%CI 0.54–0.75)were signifi cantly associated with hypotension.After adjusting for potential confounders,hypotension was associated with increased in-hospital mortality(hazard ratio 8.77–37.06,depending on the controlled variables).CONCLUSIONS:Hypotension is a common complication of AOPP and is associated with increased in-hospital mortality.Advanced age,history of diabetes,and changes in laboratory parameters were associated with hypotension in AOPP patients.
基金Supported by Management of Agriculture,Cario University
文摘Objective:To evaluate the effect of different doses of lead acetate(1/20,1/40 and 1/60 of LD_(50))on body weight gain,blood picture,plasma prolein profile and the function of liver,kidney and thyroid gland.Methods:Male albino rats were divided into four groups,the first group represented the health control animals,while the second,third and fourth groups were ingested orally with sub lethal doses of load acetate(1/20,1/40 and 1/60)of the oral LD_(50),respectively.One dose was ingested every two days during the experimental period(14 weeks)including the adaptation time.Blood was collected and used for all analysis.Results:The results showed that,the ingestion of Pb^(2+)induced significant stimulation in glutamic-pyruvic transaminase(ALT)and glutamic-oxalacetic transaminease(AST)activity.Also,total soluble protein and albumin contents of plasma were significantly decreased,while the content of globulin was changed by the Pb^(2+)treatments.The cholinesteiase activity was inhibited,but the activities of alkaline and acid phosphates and lactate dehydrogenase were stimulated,while plasma glucose level was elevated as a result of lead acetate intoxication.In case of blood picture,Pb^(2+)ingestion reduced the contents of hemoglobin and RBCs count of intoxicated rat's blood and the plasma levels of T3,T4 and blood WBCs count were decreased.Conclusions:It can be concluded that lead acetate has harmful effect on experimental male albino rats.Therefore,the present work advises people to prevent exposure to the lead compound to avoid injurious hazard risk.
文摘A novel quartz crystal microbalance (QCM) biosensor for the determination of organophosphorus pesticide,such as dichlorvos (DDVP),has been fabricated with poly (3,4-ethylenedioxythiophene)/Poly (4-styrenesulfonate) (PEDOT/PSS) and cholinesterase butyl (BuChE).It is found that PEDOT/PSS coated sensor exhibits the highest sensitivity for DDVP among PEDOT,polyvinyl pyrrolidone,polyvinyl alcohol and polyacrylic acid sensor series.The conditions to prepare PEDOT/PSS coated sensor are optimized.The sensitivity of the PEDOT/PSS hiosensor with BuChE is higher than the others without BuChE The determination of dichlorvos in the range from 400μg/g to 2400μg/g used PEDOT/PSS with BuChE coated hiosensor was obtained.
