Objective:To observe the analgesic effect of combined spinal and epidural anesthesia on older patients undergoing hip fracture surgery.Method:One hundred and twenty elderly hip fracture surgery patients treated in our...Objective:To observe the analgesic effect of combined spinal and epidural anesthesia on older patients undergoing hip fracture surgery.Method:One hundred and twenty elderly hip fracture surgery patients treated in our hospital from January 2021 to December 2022 were selected and randomly divided into two groups,with 60 cases in the experimental group and 60 in the control group.The experimental group was given combined spinal-epidural anesthesia intervention measures,while the control group was given epidural anesthesia intervention measures.The analgesic effect,tumor necrosis factor-alpha(TNF-α),C-reactive protein(CRP)levels,and other observation indicators were analyzed after anesthesia intervention.Result:After the intervention,the analgesic effect and the evaluation results of the subjects in the experimental group were better than those in the control group(P<0.05);the obtained values of TNF-αand CRP levels in the experimental group were higher than those of the control group(P<0.05).Conclusion:The combined spinal-epidural anesthesia intervention demonstrated positive outcomes.The analgesic effect of patients during surgery and their inflammatory factor levels improved,which makes this intervention worthy of clinical application and promotion.展开更多
Background:Peanut shells are a commonly discarded byproduct of peanut processing.However,recent studies have shown that they contain bioactive compounds that have potential health benefits.Specifically,water extract f...Background:Peanut shells are a commonly discarded byproduct of peanut processing.However,recent studies have shown that they contain bioactive compounds that have potential health benefits.Specifically,water extract from peanut shells has been identified as a promising source of these compounds.Therefore,investigating the effects of water extract from peanut shells on coagulation and analgesia in mice could have significant implications for human health.Methods:(1)Analgesic experiments:The analgesic effect of the aqueous extract of peanut shells was observed by the hot plate method in mice.The aspirin group was used as a positive control group for analgesic experiments.(2)Coagulation experiment:the coagulation effect of the aqueous extract of peanut shells was observed by the capillary method and slide method.Yunnan Baiyao group was the positive control group of the coagulation test.Results:(1)The analgesic effect of peanut shell water extract on mice was prolonged with the increase in dose.The low,medium,and high dose groups of peanut shell could improve the pain domain of mice induced by the hot plate method in a certain period(P<0.05);with the increase of peanut shell water extract dose,liver weight coefficient increased(P<0.05).(2)Peanut shell water extract coagulated mice,and the high-dose group of peanut shells was the most significant.Within the scope of this study,the higher the concentration,the better the coagulation effect(P<0.05).Compared with distilled water group,the liver weight coefficients of the Yunnan Baiyao group,low,middle,and high dose groups of peanut shells were significantly increased(P<0.05).Conclusion:(1)The aqueous extract of peanut shells has a specific analgesic effect on mice.(2)The aqueous extract of peanut shells promotes coagulation,and the pro-coagulant effect is more significant with increasing dose and the liver weight coefficient increases.展开更多
Background:To study the anti-inflammatory,analgesic,fatigue resistant and antihypoxia effects of ethanol extract and water extract of pine pollen.Methods:Two different extracts of pine pollen were prepared into there ...Background:To study the anti-inflammatory,analgesic,fatigue resistant and antihypoxia effects of ethanol extract and water extract of pine pollen.Methods:Two different extracts of pine pollen were prepared into there different concentrations,that is 1.5 mg·mL^-1,4.5 mg·mL^-1 and 7.5 mg·mL^-1 respectively.The extract were studied by xylene-induced ear swelling,acetic acid distortion test and hot plate test.The antihypoxia and antifatigue effects were explored by weight-bearing swimming experiment,routine pressure hypoxia tolerance experiment and liver weight coefficient comparison.Results:Through the study of the four pharmacological effects of ethanol extract and water extract,we found that the anti-inflammatory,analgesic,antithyposia and antifatigue effects of ethanol extract were better than that of water extract.Moreover,the experimental effects significantly improved with the increase of the concentration,and the effect of alcohol increased dose group was accurate(P<0.05).Conclusion:Pine pollen has excellent effects of anti-inflammatory,analgesic,antihypoxia and anti-fatigue.Besides,with the increase of drug concentration,effects tend to be more obvious with positive correlation.展开更多
Objective:To systematically evaluate the clinical efficacy and analgesic effect of acupuncture and moxibustion in the treatment of herpes zoster by comparing western medicine.Methods:Randomized controlled trials on ac...Objective:To systematically evaluate the clinical efficacy and analgesic effect of acupuncture and moxibustion in the treatment of herpes zoster by comparing western medicine.Methods:Randomized controlled trials on acupuncture and western medicine for herpes zoster were searched from CNKI,Wanfang Database,VIP,CMB,PubMed,Embase and Cochrane library databases,and the retrieval time was from January 2010 to July 2020.RevMan5.3 software was used for Meta analysis.Results:A total of 30 randomized controlled studies were included,involving a total of 4292 patients.Subgroup analysis was conducted according to different intervention measures in the experimental group.The results showed that:(1)The total effective rate of the subgroup analysis showed that the combined effect of acupuncture treatment alone RR=1.10,95%CI[1.05,1.15],P<0.0001.Results:RR=1.16,95%CI[0.86,1.57],P=0.33.It suggests that the therapeutic effect of acupuncture and moxibustion on herpes zoster is superior to that of western medicine,but acupuncture and western medicine treatment cannot improve the clinical efficacy of western medicine.However,due to the unstable meta-analysis of acupuncture and western medicine treatment in the subgroup,the results need to be treated with caution and further clinical verification is still needed.(2)VAS score improvement analysis showed that the combined effect of acupuncture alone RR=2.20,95%CI[1.53,2.87],P<0.00001.RR=1.12,95%CI[0.39,1.85],P=0.002,suggesting that acupuncture is significantly better than western medicine in improving the pain of shingles,and western medicine combined with acupuncture can improve the analgesic effect.(3)The subgroup analysis of sequelae incidence showed that the combined effect amount of acupuncture alone on sequelae incidence at 30 days was RR=0.34,95%CI[0.25,0.48],P<0.00001,and the combined effect amount of acupuncture combined with western medicine was RR=0.18,95%CI[0.05,0.69],P=0.01.Incidence of sequelae at 60 days RR=0.38,95%CI[0.23,0.62],P=0.0001;The incidence of post-herpetic neuralgia treated with acupuncture alone at 90 days RR=0.39,95%CI[0.20,0.74],P=0.004,suggesting that the incidence of post-herpetic neuralgia treated with acupuncture is significantly lower than that treated with western medicine,and western medicine combined with acupuncture can reduce the incidence of post-herpetic neuralgia.(4)The time analysis of the onset of pain relief showed that the combined effect of acupuncture alone RR=-2.32,95%CI[-2.48,-2.17],P<0.00001.RR=-2.39,95%CI[-2.70,-2.09],P<0.00001,suggesting that the onset time of acupuncture and moxibustion was shorter than that of western medicine,and western medicine combined with acupuncture and moxibustion could accelerate the onset time of analgesia.(5)The time analysis of pain relief showed that the combined effect of acupuncture alone RR=-10.80,95%CI[-12.49,-9.01],P<0.00001.RR=-5.98,95%CI[-11.55,-0.41],P=0.04,suggesting that acupuncture treatment of herpes zoster can significantly reduce the pain time,combined with western medicine can shorten the pain time.Conclusion:Acupuncture and moxibustion treatment of herpes zoster in the total effective rate,pain relief and the incidence of post-neurosis is significantly better than western medicine;Acupuncture and moxibustion combined with western medicine can improve the analgesic effect and reduce the incidence of post-neurosis.In view of the low overall quality of the literature included in this study,further clinical validation is needed for this conclusion.展开更多
Objective To investigate analgesic effect of i ntra -articular low -dose tramadol a fter arthroscopic knee surgery.Methods60patients undergoing arthroscopic k nee surgery under lumbar anesthesia were randomly divided ...Objective To investigate analgesic effect of i ntra -articular low -dose tramadol a fter arthroscopic knee surgery.Methods60patients undergoing arthroscopic k nee surgery under lumbar anesthesia were randomly divided into intra -ar ticular injection of tramadol(TJ group),mulscle injection of tramadol(TM)and saline control group.Vision analog scoring was conducted under exte nsion of knee joint 8h and24h after drugs administration.Follow -up was done to observe unwanted e ffects 48h after surgery.Results Score of TJ group was significantly lower than those of other groups(P <0.05).No unwanted effects were found.Conclusion Intra -articular tramadol in low -dose could relieve operative pain.展开更多
[Objectives]To observe the clinical analgesic effect of Qianghuo Chushi Decoction(QHCSD)on patients with fasciitis,and explore its possible molecular mechanism based on network pharmacology.[Methods]120 enrolled patie...[Objectives]To observe the clinical analgesic effect of Qianghuo Chushi Decoction(QHCSD)on patients with fasciitis,and explore its possible molecular mechanism based on network pharmacology.[Methods]120 enrolled patients were randomly divided into experimental group and control group,and were separately treated with QHCSD formula granules and Diclofenac Sodium Enteric-coated Tablets for 4 weeks.The patient’s pain visual analogue scale(VAS)was used as the curative effect indicator.The molecular action mechanism of QHCSD was predicted based on network pharmacology,the active components of QHCSD were screened using TCMSP database,potential targets were predicted by PharmMapper server,compound-target network and protein interaction network were constructed,and GO-based enrichment analysis and KEGG-based biological pathway enrichment analysis were performed.[Results]After treatment,the pain scores in each group were significantly lower than those before treatment(P<0.01),the score of the experimental group was significantly lower than that of the control group(P<0.01),and the total effective rate of the experimental group was 83.33%,which was significantly higher than that of the control group(78.33%,P<0.05).Based on 108 active components in QHCSD,a compound-target network was constructed.The PPI network contained 155 nodes and 527 interaction relationships,and key nodes included FOS,ESR1,NCOA1,RELA,EGFR,MAPK8,IL-6,etc.The GO pathway mainly involved steroid hormone and its receptor activity,RNA polymerase II transcriptional regulator binding,nuclear receptor activity,protein heterodimerization activity and other pathways.KEGG metabolic pathways included PI3 K-Akt signaling pathway,Kaposi’s sarcoma-associated herpesvirus(KSHV)infection and other pathways.[Conclusions]QHCSD has a significant analgesic effect on fasciitis,and the PI3 K-Akt signaling pathway may be the key pathway for its analgesic effect.展开更多
Objective:This study investigates the in vivo anti-inflammatory and analgesic pharmacological effects of white peony root and mucuna pruriens and their combinations.Methods:In this study,the corresponding solutions we...Objective:This study investigates the in vivo anti-inflammatory and analgesic pharmacological effects of white peony root and mucuna pruriens and their combinations.Methods:In this study,the corresponding solutions were administered in groups,and after 14 days of gavage,xylene-induced ear swelling test,acetic acid torsion test and hot plate pain test were performed.Results:It was found that both Paeonia lactiflora root and Kapok had anti-inflammatory and analgesic effects(P<0.05),with the 2:1 group having the best experimental effect(P<0.05).Conclusion:Paeonia lactiflora root and Kapok and its combination have good anti-inflammatory and analgesic effects in vivo,and the 2:1 group showed significant anti-inflammatory and analgesic effects compared with other groups.展开更多
The present study was designed to isolate and characterize the analgesic compounds of Artemisa sacrorum Ledeb. The Et OAc crude extracts from the aerial parts of Artemisa sacrorum Ledeb were separated by chromatograph...The present study was designed to isolate and characterize the analgesic compounds of Artemisa sacrorum Ledeb. The Et OAc crude extracts from the aerial parts of Artemisa sacrorum Ledeb were separated by chromatography and the structures of new compounds were elucidated based on spectral analyses. Analgesic activities of the isolated compounds were assessed in rats with hot plate test and paw pressure assay. Two new flavone C-glycosides, named as Sacroroside A and B(Compounds 1 and 2) were isolated from the Et OAc crude extract of the aerial parts of Artemisa sacrorum Ledeb. They showed significant analgesic effects. In conclusion, Compounds 1 and 2 are new natural products, which show significant analgesic effects in a dose-dependent manner.展开更多
Objective:To analyze the effect of pantoprazole and omeprazole in the treatment of patients with gastric ulcer.Methods:The treatment effect,recurrence rate,helicobacter pylori negative conversion rate,adverse reaction...Objective:To analyze the effect of pantoprazole and omeprazole in the treatment of patients with gastric ulcer.Methods:The treatment effect,recurrence rate,helicobacter pylori negative conversion rate,adverse reaction status and pain relief time of the two groups were compared.Results:The total effective rate of the experimental group(97.78%,44/45)was higher than that of the control group(84.44%,38/45),P<0.05;The recurrence rate(4.44%,2/45)and Helicobacter pylori negative conversion rate(95.56%,43/45)of the experimental group were significantly higher than those of the control group(P<0.05);The incidence of adverse reactions in the experimental group(11.11%,5/45)was lower than that in the control group(15.56%,7/45)(P>0.05);The pain relief time of the experimental group was(2.24±1.16)d,which was shorter than that of the control group(P<0.05).Conclusion:In the process of clinical treatment of gastric ulcer,pantoprazole has significant curative effect and low recurrence rate,which can eradicate Helicobacter pylori as soon as possible,shorten the pain time and make the treatment safer.展开更多
BACKGROUND During anesthesia administration for cataract surgery,low pH of proparacaine may induce pain or complications such as corneal damage and poor wound healing,with the use of additional drops intraoperatively ...BACKGROUND During anesthesia administration for cataract surgery,low pH of proparacaine may induce pain or complications such as corneal damage and poor wound healing,with the use of additional drops intraoperatively increasing the risk of complications.Accordingly,there is a clinical need for adjuncts to local anesthesia needs to improve the efficiency of anesthesia and reduce the required amount of intraoperative proparacaine.AIM To identify a method of anesthesia for geriatric cataract phacoemulsification that provides more efficient analgesia and improves clinical efficacy.METHODS A total of 130 geriatric patients with cataracts who attended Hebei Eye Hospital from December 2020 to December 2022 were included in the present study.Patients were divided into the proparacaine surface anesthesia(SA)group(65 cases)and the compound acupuncture-medicine anesthesia group(CAMA group,65 cases).Patients in the CAMA group were provided acupuncture analgesia in addition to SA.Preoperative anxiety[Self-Rating Anxiety Scale(SAS)score and state anxiety inventory(SAI)score],intraoperative stress,vital signs,analgesia,and cooperation,as well as postoperative adverse events,were compared between groups.RESULTS More marked reductions in anxiety were observed among patients in the CAMA group,with corresponding reductions in SAS and SAI scores.During the operation,no change in the secretion of E,NE,or Cor group compared to the preoperative period was observed in the CAMA,which was markedly lower than that in the SA group.Heart rate,blood pressure,and respiratory rate were more stable intraoperatively in the CAMA group.In addition,the incidence of intraoperative pain and the number of additional doses of anesthesia required in the CAMA group were markedly lower than in the SA group.Accordingly,patients in the CAMA group were able to avoid eye movements and eyelid closing leading to greater cooperation with surgeons during surgery.Furthermore,marked reductions in intraoperative adverse effects were observed in the CAMA group,indicating greater overall safety.CONCLUSION Proparacaine SA combined with acupuncture as an analgesic provides improved analgesia with greater safety compared to surface anesthesia with proparacaine during geriatric cataract phacoemulsification.展开更多
BACKGROUND Laparoscopic surgery has become a common surgical approach for the clinical treatment of intra-abdominal lesions in recent years.We hypothesized that lumbar block with postoperative patient-controlled intra...BACKGROUND Laparoscopic surgery has become a common surgical approach for the clinical treatment of intra-abdominal lesions in recent years.We hypothesized that lumbar block with postoperative patient-controlled intravenous analgesia(PCIA)by butorphanol after gynecological surgery under general anesthesia would be more effective than PCIA by butorphanol alone.AIM To investigate the effect of lumbar block with PCIA by butorphanol after gynecological surgery under general anesthesia.METHODS This study assessed 120 women scheduled for laparoscopic surgery at our hospital between May 2017 and May 2020.They were divided using a random number table into a research group(those who received quadratus lumborum block combined with PCIA analgesia by butorphanol)and a control group(those who received only PCIA analgesia by butorphanol),with 60 patients in each group.Demographic factors,visual analog scale scores for pain,serum inflammatory markers,PCIA compressions,Ramsay scores,and adverse events were compared between groups using a t-test,analysis of variance,orχ2 test,as appropriate.RESULTS There were no significant differences in demographic factors between groups(all P>0.05).The visual analog scale scores of the research group in the resting state 12 h and 24 h postoperatively were significantly lower than those of the control group(P<0.05).Two hours after surgery,there were no significant differences in the levels of serum tumor necrosis factor-α,interleukin(IL)-6,or IL-8 between groups(P>0.05).The serum tumor necrosis factor-αlevels of the research group 24 h postoperatively were significantly lower than those of the control group(P<0.05).The levels of serum IL-6 and IL-8 in the study group 24 h and 48 h postoperatively were significantly lower than those in the control group(P<0.05).CONCLUSION Lumbar block with PCIA with butorphanol after gynecological surgery under general anesthesia significantly improves the analgesic effect and reduces the degree of inflammation,instances of PCIA compression,and adverse reactions.展开更多
Eight new C_(19)-diterpenoid alkaloid arabinosides, named aconicarmichosides E–L(1–8), were isolated from an aqueous extract of the lateral roots of Aconitum carmichaelii(Fu Zi). Their structures were determined by ...Eight new C_(19)-diterpenoid alkaloid arabinosides, named aconicarmichosides E–L(1–8), were isolated from an aqueous extract of the lateral roots of Aconitum carmichaelii(Fu Zi). Their structures were determined by spectroscopic and chemical methods including 2D NMR experiments and acid hydrolysis. Compounds 1–8, together with the previously reported four neoline 14-O-arabinosides from the same plant, represent the only examples of glycosidic diterpenoid alkaloids so far. At a dose of 1.0 mg/kg(i.p.), as compared with the black control, compounds 1, 2, and 4–6 exhibited analgesic effects with 465.6% inhibitions against acetic acid-induced writhing of mice. Structure–activity relationship was also discussed.展开更多
Quantitative evaluation of analgesic efficacy improves understanding of the antinociceptive mechanisms of new analgesics and provides important guidance for their development.Lappaconitine(LA),a potent analgesic drug ...Quantitative evaluation of analgesic efficacy improves understanding of the antinociceptive mechanisms of new analgesics and provides important guidance for their development.Lappaconitine(LA),a potent analgesic drug extracted from the root of natural Aconitum species,has been clinically used for years because of its effective analgesic and non-addictive properties.However,being limited to ethological experiments,previous studies have mainly investigated the analgesic effect of LA at the behavioral level,and the associated antinociceptive mechanisms are still unclear.In this study,electrocorticogram(ECoG)technology was used to investigate the analgesic effects of two homologous derivatives of LA,Lappaconitine hydrobromide(LAH)and Lappaconitine trifluoroacetate(LAF),on Sprague-Dawley rats subjected to nociceptive laser stimuli,and to further explore their antinociceptive mechanisms.We found that both LAH and LAF were effective in reducing pain,as manifested in the remarkable reduction of nocifensive behaviors and laser-evoked potentials(LEPs)amplitudes(N2 and P2 waves,and gamma-band oscillations),and significantly prolonged latencies of the LEP-N2/P2.These changes in LEPs reflect the similar antinociceptive mechanism of LAF and LAH,i.e.,inhibition of the fast signaling pathways.In addition,there were no changes in the auditory-evoked potential(AEP-N1 component)before and after LAF or LAH treatment,suggesting that neither drug had a central anesthetic effect.Importantly,compared with LAH,LAF was superior in its effects on the magnitudes of gamma-band oscillations and the resting-state spectra,which may be associated with their differences in the octanol/water partition coefficient,degree of dissociation,toxicity,and glycine receptor regulation.Altogether,jointly applying nociceptive laser stimuli and ECoG recordings in rats,we provide solid neural evidence for the analgesic efficacy and antinociceptive mechanisms of derivatives of LA.展开更多
Objective:To investigate the effect of preemptive analgesia withflurbiprofen axetil injection on the analgesic effect,inflammatory response,stress response and immune response in patients undergoing thoracoscopic lobe...Objective:To investigate the effect of preemptive analgesia withflurbiprofen axetil injection on the analgesic effect,inflammatory response,stress response and immune response in patients undergoing thoracoscopic lobectomy.Methods:92 patients with early non-small cell lung cancer who underwent thoracoscopic lobectomy from January 2016 to March 2018 in our hospital were divided into observation group and control group according to the method of random digital table,46 cases in each group.The control group was given routine perioperative analgesia,the observation group was given advanced analgesia mode,and the visual simulation scoring method(visual)was used to observe the patients in the two groups at 4,12,24 and 48 h after operation The results showed that the level of inflammation factor,stress response factor and immune response were significantly higher than that of before operation(T0),when anesthesia woke up(T1),12 hours after operation(T2),24 h after operation(T3)and 48 h after operation(T4).Results:(1)The VAS score of the observation group was significantly lower than that of the control group(P<0.05)at 4,12,24 and 48 h after operation;(2)The levels of IL-6,IL-10,SP-A and TNF-αin the two groups were significantly lower than that of the control group(P<0.05)The level of factor-α,TNF-α)was higher than that of to time point,and showed an upward trend;the level of IL-6,IL-10,TNF-α,SP-A decreased gradually at T3,T4 time points,the level of IL-6,TNF-α,SP-A in T1,T2,T3,T4 time points in the observation group was lower than that of the control group,and the level of IL-10 was higher than that of the control group(P<0.05);(3)Compared with T0 time point,the epinephrine(EPIPH)at T1,T2,T3,T4 time points in the two groups The levels of rine,e,noradrenaline,NE and cortisol in the observation group increased first and then decreased;the levels of E,NE and cor in the observation group were lower than those in the control group at T1,T2,T3 and T4 time points(P<0.05);and(4)Compared with T0 time point,the serum IgG,IgM and IgA levels in the two groups decreased gradually at T1,T2,T3 and T4 time points,but the observation group The levels of IgG,IgM and IgA in serum of group A were higher than those of group B(P<0.05).Conclusion:Preemptive analgesia with flurbiprofen axetil injection can significantly improve the postoperative pain,reduce the level of ;inflammation,reduce the stress response and increase the level of immune response.展开更多
The uterine tetanic contraction and uterine artery blood flow reduction are possible reasons for primary dysmenorrhea(PD). In the present study, we aimed to evaluate the uterine relaxant effect and the influence on ut...The uterine tetanic contraction and uterine artery blood flow reduction are possible reasons for primary dysmenorrhea(PD). In the present study, we aimed to evaluate the uterine relaxant effect and the influence on uterine artery blood velocity of Ge-Gen Decoction(GGD), a well-known Chinese herbal formula. In female ICR mice, uterine contraction was induced by oxytocin exposure following estradiol benzoate pretreatment, and the uterine artery blood velocity was detected by Doppler ultrasound. Histopathological examination of the uterine tissue samples were performed by H&E staining. Ex vivo studies demonstrated that oxytocin, posterior pituitary, or acetylcholine induced contractions in isolated mouse uterus. GGD inhibited both spontaneous and stimulated contractions. In vivo study demonstrated that GGD significantly reduced oxytocin-induced writhing responses with a maximal inhibition of 87%. Further study demonstrated that GGD normalized oxytocin-induced abnormalities of prostaglandins F_2 alpha(PGF_(2α)) and Ca^(2+) in mice. In addition, injection of oxytocin induced a decrease in uterine artery blood flow velocity. Pretreatment with GGD reversed the oxytocin response on blood flow velocity. Histopathological examination showed pretreatment with GGD alleviated inflammation and edema in the uterus when compared with the model group. Both ex vivo and in vivo results indicated that GGD possessed a significant spasmolytic effect on uterine tetanic contraction as well as improvement on uterine artery blood velocity which may involve PGF_(2α) and Ca^(2+) signaling, suggesting that GGD may have a clinic potential in PD therapy.展开更多
Three new C20-diterpenoid alkaloids with a sulfonic acid unit,named aconicarmisulfonines B and C(1 and 2)and chuanfusulfonine A(3),respectively,were isolated from the Aconitum carmichaelii lateral roots("fu zi&qu...Three new C20-diterpenoid alkaloids with a sulfonic acid unit,named aconicarmisulfonines B and C(1 and 2)and chuanfusulfonine A(3),respectively,were isolated from the Aconitum carmichaelii lateral roots("fu zi"in Chinese).Structures of 1-3 were determined by spectroscopic data analysis.Intriguing chemical properties and reactions were observed for the C20-diterpenoid alkaloids:(a)specific selective nucleophilic addition of the carbonyl(C-12)in 1 with CD3 OD;(b)interconversion between 1 and 2 in D2 O;(c)stereo-and/or regioselective deuterations of H-11αin 1-3 and both H-11αand H-11βin aconicarmisulfonine A(4);(d)TMSP-2,2,3,3-d4 promoted cleavage of the C-12-C-13 bond of 4 in D2 O;(e)dehydrogenation of 4 in pyridine-d5,and(f)Na2 SO3-assisted dehydrogenation and N-deethylation of songorine(5,a putative precursor of 1-4).Biogenetically,1 and 2 are correlated with 4,for which the same novel carbon skeleton is proposed to be derived from semipinacol rearrangements via migrations of C-13-C-16 and C-15-C-16 bonds of the napelline-type skeleton,respectively.Meanwhile,3 is a highly possible precursor or a concurrent product in the biosynthetic pathways of 1,2,and 4.In the acetic acid-induced mice writhing assay,at 1.0 mg/kg(i.p.),compounds 1,2,5,5 a,and 5 b exhibited analgesic effects against mice writhing.展开更多
基金Weifang Municipal Science and Technology Bureau(Medical)Project“Effects and Mechanisms of Oxycodone and Alfentanil on IgFs in Mouse Ovarian Granulosa Cells”(2021YX035)。
文摘Objective:To observe the analgesic effect of combined spinal and epidural anesthesia on older patients undergoing hip fracture surgery.Method:One hundred and twenty elderly hip fracture surgery patients treated in our hospital from January 2021 to December 2022 were selected and randomly divided into two groups,with 60 cases in the experimental group and 60 in the control group.The experimental group was given combined spinal-epidural anesthesia intervention measures,while the control group was given epidural anesthesia intervention measures.The analgesic effect,tumor necrosis factor-alpha(TNF-α),C-reactive protein(CRP)levels,and other observation indicators were analyzed after anesthesia intervention.Result:After the intervention,the analgesic effect and the evaluation results of the subjects in the experimental group were better than those in the control group(P<0.05);the obtained values of TNF-αand CRP levels in the experimental group were higher than those of the control group(P<0.05).Conclusion:The combined spinal-epidural anesthesia intervention demonstrated positive outcomes.The analgesic effect of patients during surgery and their inflammatory factor levels improved,which makes this intervention worthy of clinical application and promotion.
基金supported by several organizations,including the National Natural Science Foundation of China(No.81360684)the State Administration of Traditional Chinese Medicine(2012 No.32)+1 种基金the Guangxi Key Discipline of Pharmaceutical Chemistry(2017 No.22)the National-level training program for college students’innovation and entrepreneurship(No.201810599013).
文摘Background:Peanut shells are a commonly discarded byproduct of peanut processing.However,recent studies have shown that they contain bioactive compounds that have potential health benefits.Specifically,water extract from peanut shells has been identified as a promising source of these compounds.Therefore,investigating the effects of water extract from peanut shells on coagulation and analgesia in mice could have significant implications for human health.Methods:(1)Analgesic experiments:The analgesic effect of the aqueous extract of peanut shells was observed by the hot plate method in mice.The aspirin group was used as a positive control group for analgesic experiments.(2)Coagulation experiment:the coagulation effect of the aqueous extract of peanut shells was observed by the capillary method and slide method.Yunnan Baiyao group was the positive control group of the coagulation test.Results:(1)The analgesic effect of peanut shell water extract on mice was prolonged with the increase in dose.The low,medium,and high dose groups of peanut shell could improve the pain domain of mice induced by the hot plate method in a certain period(P<0.05);with the increase of peanut shell water extract dose,liver weight coefficient increased(P<0.05).(2)Peanut shell water extract coagulated mice,and the high-dose group of peanut shells was the most significant.Within the scope of this study,the higher the concentration,the better the coagulation effect(P<0.05).Compared with distilled water group,the liver weight coefficients of the Yunnan Baiyao group,low,middle,and high dose groups of peanut shells were significantly increased(P<0.05).Conclusion:(1)The aqueous extract of peanut shells has a specific analgesic effect on mice.(2)The aqueous extract of peanut shells promotes coagulation,and the pro-coagulant effect is more significant with increasing dose and the liver weight coefficient increases.
基金The National Natural Science Foundation of China(No.81360684)Guangxi Key Research and Development Plan Project(Gui Ke AB18221095)+2 种基金China National and Regional University Students Innovation and Entrepreneurship Training Scheme Funding(No.201910599012)High-level Talent Research Projects From Youjiang Medical University For Nationalities(No.01002018079)China National and Autonomous Region Innovation Planning Project for University Students in 2020(2020010599030).
文摘Background:To study the anti-inflammatory,analgesic,fatigue resistant and antihypoxia effects of ethanol extract and water extract of pine pollen.Methods:Two different extracts of pine pollen were prepared into there different concentrations,that is 1.5 mg·mL^-1,4.5 mg·mL^-1 and 7.5 mg·mL^-1 respectively.The extract were studied by xylene-induced ear swelling,acetic acid distortion test and hot plate test.The antihypoxia and antifatigue effects were explored by weight-bearing swimming experiment,routine pressure hypoxia tolerance experiment and liver weight coefficient comparison.Results:Through the study of the four pharmacological effects of ethanol extract and water extract,we found that the anti-inflammatory,analgesic,antithyposia and antifatigue effects of ethanol extract were better than that of water extract.Moreover,the experimental effects significantly improved with the increase of the concentration,and the effect of alcohol increased dose group was accurate(P<0.05).Conclusion:Pine pollen has excellent effects of anti-inflammatory,analgesic,antihypoxia and anti-fatigue.Besides,with the increase of drug concentration,effects tend to be more obvious with positive correlation.
基金Construction Project of Advantageous Disciplines in Jiangsu Universities,Open Project of the Third Phase of Advantageous Disciplines in Traditional Chinese Medicine of Nanjing University of Chinese Medicine(No.ZYX03KF035)2019 Hospital-Level Project of Jiangsu Hospital of Traditional Chinese Medicine(No.Y19024)the Sixth Batch of National Old Chinese Medicine experts Academic Experience Successor Project[National Education and Development of Traditional Chinese Medicine(2017)No.29]。
文摘Objective:To systematically evaluate the clinical efficacy and analgesic effect of acupuncture and moxibustion in the treatment of herpes zoster by comparing western medicine.Methods:Randomized controlled trials on acupuncture and western medicine for herpes zoster were searched from CNKI,Wanfang Database,VIP,CMB,PubMed,Embase and Cochrane library databases,and the retrieval time was from January 2010 to July 2020.RevMan5.3 software was used for Meta analysis.Results:A total of 30 randomized controlled studies were included,involving a total of 4292 patients.Subgroup analysis was conducted according to different intervention measures in the experimental group.The results showed that:(1)The total effective rate of the subgroup analysis showed that the combined effect of acupuncture treatment alone RR=1.10,95%CI[1.05,1.15],P<0.0001.Results:RR=1.16,95%CI[0.86,1.57],P=0.33.It suggests that the therapeutic effect of acupuncture and moxibustion on herpes zoster is superior to that of western medicine,but acupuncture and western medicine treatment cannot improve the clinical efficacy of western medicine.However,due to the unstable meta-analysis of acupuncture and western medicine treatment in the subgroup,the results need to be treated with caution and further clinical verification is still needed.(2)VAS score improvement analysis showed that the combined effect of acupuncture alone RR=2.20,95%CI[1.53,2.87],P<0.00001.RR=1.12,95%CI[0.39,1.85],P=0.002,suggesting that acupuncture is significantly better than western medicine in improving the pain of shingles,and western medicine combined with acupuncture can improve the analgesic effect.(3)The subgroup analysis of sequelae incidence showed that the combined effect amount of acupuncture alone on sequelae incidence at 30 days was RR=0.34,95%CI[0.25,0.48],P<0.00001,and the combined effect amount of acupuncture combined with western medicine was RR=0.18,95%CI[0.05,0.69],P=0.01.Incidence of sequelae at 60 days RR=0.38,95%CI[0.23,0.62],P=0.0001;The incidence of post-herpetic neuralgia treated with acupuncture alone at 90 days RR=0.39,95%CI[0.20,0.74],P=0.004,suggesting that the incidence of post-herpetic neuralgia treated with acupuncture is significantly lower than that treated with western medicine,and western medicine combined with acupuncture can reduce the incidence of post-herpetic neuralgia.(4)The time analysis of the onset of pain relief showed that the combined effect of acupuncture alone RR=-2.32,95%CI[-2.48,-2.17],P<0.00001.RR=-2.39,95%CI[-2.70,-2.09],P<0.00001,suggesting that the onset time of acupuncture and moxibustion was shorter than that of western medicine,and western medicine combined with acupuncture and moxibustion could accelerate the onset time of analgesia.(5)The time analysis of pain relief showed that the combined effect of acupuncture alone RR=-10.80,95%CI[-12.49,-9.01],P<0.00001.RR=-5.98,95%CI[-11.55,-0.41],P=0.04,suggesting that acupuncture treatment of herpes zoster can significantly reduce the pain time,combined with western medicine can shorten the pain time.Conclusion:Acupuncture and moxibustion treatment of herpes zoster in the total effective rate,pain relief and the incidence of post-neurosis is significantly better than western medicine;Acupuncture and moxibustion combined with western medicine can improve the analgesic effect and reduce the incidence of post-neurosis.In view of the low overall quality of the literature included in this study,further clinical validation is needed for this conclusion.
文摘Objective To investigate analgesic effect of i ntra -articular low -dose tramadol a fter arthroscopic knee surgery.Methods60patients undergoing arthroscopic k nee surgery under lumbar anesthesia were randomly divided into intra -ar ticular injection of tramadol(TJ group),mulscle injection of tramadol(TM)and saline control group.Vision analog scoring was conducted under exte nsion of knee joint 8h and24h after drugs administration.Follow -up was done to observe unwanted e ffects 48h after surgery.Results Score of TJ group was significantly lower than those of other groups(P <0.05).No unwanted effects were found.Conclusion Intra -articular tramadol in low -dose could relieve operative pain.
文摘[Objectives]To observe the clinical analgesic effect of Qianghuo Chushi Decoction(QHCSD)on patients with fasciitis,and explore its possible molecular mechanism based on network pharmacology.[Methods]120 enrolled patients were randomly divided into experimental group and control group,and were separately treated with QHCSD formula granules and Diclofenac Sodium Enteric-coated Tablets for 4 weeks.The patient’s pain visual analogue scale(VAS)was used as the curative effect indicator.The molecular action mechanism of QHCSD was predicted based on network pharmacology,the active components of QHCSD were screened using TCMSP database,potential targets were predicted by PharmMapper server,compound-target network and protein interaction network were constructed,and GO-based enrichment analysis and KEGG-based biological pathway enrichment analysis were performed.[Results]After treatment,the pain scores in each group were significantly lower than those before treatment(P<0.01),the score of the experimental group was significantly lower than that of the control group(P<0.01),and the total effective rate of the experimental group was 83.33%,which was significantly higher than that of the control group(78.33%,P<0.05).Based on 108 active components in QHCSD,a compound-target network was constructed.The PPI network contained 155 nodes and 527 interaction relationships,and key nodes included FOS,ESR1,NCOA1,RELA,EGFR,MAPK8,IL-6,etc.The GO pathway mainly involved steroid hormone and its receptor activity,RNA polymerase II transcriptional regulator binding,nuclear receptor activity,protein heterodimerization activity and other pathways.KEGG metabolic pathways included PI3 K-Akt signaling pathway,Kaposi’s sarcoma-associated herpesvirus(KSHV)infection and other pathways.[Conclusions]QHCSD has a significant analgesic effect on fasciitis,and the PI3 K-Akt signaling pathway may be the key pathway for its analgesic effect.
基金This work was supported by National Natural Science Foundation of China(No.81360684)Guangxi Key Research and Development Plan Project(Gui Ke AB18221095)+3 种基金Teaching Teacher Training Project from Youjiang Medical University for Nationalities-National Teaching Teacher Training Project(You Hospital Zi[2018]No.98)High-level Talent Research Projects from Youjiang Medical University For Nationalities(No.01002018079)China National and Regional University Students Innovation and Entrepreneurship Training Scheme Funding(No.201910599012)China Regional University Students Innovation and Entrepreneurship Training Scheme Funding(No.202010599072).
文摘Objective:This study investigates the in vivo anti-inflammatory and analgesic pharmacological effects of white peony root and mucuna pruriens and their combinations.Methods:In this study,the corresponding solutions were administered in groups,and after 14 days of gavage,xylene-induced ear swelling test,acetic acid torsion test and hot plate pain test were performed.Results:It was found that both Paeonia lactiflora root and Kapok had anti-inflammatory and analgesic effects(P<0.05),with the 2:1 group having the best experimental effect(P<0.05).Conclusion:Paeonia lactiflora root and Kapok and its combination have good anti-inflammatory and analgesic effects in vivo,and the 2:1 group showed significant anti-inflammatory and analgesic effects compared with other groups.
基金supported by the scientific research project of the Inner Mongolia Autonomous Region Colleges in China(No.NJZZ14182)National Natural Science Foundation of China(No.81460654)
文摘The present study was designed to isolate and characterize the analgesic compounds of Artemisa sacrorum Ledeb. The Et OAc crude extracts from the aerial parts of Artemisa sacrorum Ledeb were separated by chromatography and the structures of new compounds were elucidated based on spectral analyses. Analgesic activities of the isolated compounds were assessed in rats with hot plate test and paw pressure assay. Two new flavone C-glycosides, named as Sacroroside A and B(Compounds 1 and 2) were isolated from the Et OAc crude extract of the aerial parts of Artemisa sacrorum Ledeb. They showed significant analgesic effects. In conclusion, Compounds 1 and 2 are new natural products, which show significant analgesic effects in a dose-dependent manner.
文摘Objective:To analyze the effect of pantoprazole and omeprazole in the treatment of patients with gastric ulcer.Methods:The treatment effect,recurrence rate,helicobacter pylori negative conversion rate,adverse reaction status and pain relief time of the two groups were compared.Results:The total effective rate of the experimental group(97.78%,44/45)was higher than that of the control group(84.44%,38/45),P<0.05;The recurrence rate(4.44%,2/45)and Helicobacter pylori negative conversion rate(95.56%,43/45)of the experimental group were significantly higher than those of the control group(P<0.05);The incidence of adverse reactions in the experimental group(11.11%,5/45)was lower than that in the control group(15.56%,7/45)(P>0.05);The pain relief time of the experimental group was(2.24±1.16)d,which was shorter than that of the control group(P<0.05).Conclusion:In the process of clinical treatment of gastric ulcer,pantoprazole has significant curative effect and low recurrence rate,which can eradicate Helicobacter pylori as soon as possible,shorten the pain time and make the treatment safer.
基金2019 Hebei Provincial Medical Science Research Project Plan,No.20191053.
文摘BACKGROUND During anesthesia administration for cataract surgery,low pH of proparacaine may induce pain or complications such as corneal damage and poor wound healing,with the use of additional drops intraoperatively increasing the risk of complications.Accordingly,there is a clinical need for adjuncts to local anesthesia needs to improve the efficiency of anesthesia and reduce the required amount of intraoperative proparacaine.AIM To identify a method of anesthesia for geriatric cataract phacoemulsification that provides more efficient analgesia and improves clinical efficacy.METHODS A total of 130 geriatric patients with cataracts who attended Hebei Eye Hospital from December 2020 to December 2022 were included in the present study.Patients were divided into the proparacaine surface anesthesia(SA)group(65 cases)and the compound acupuncture-medicine anesthesia group(CAMA group,65 cases).Patients in the CAMA group were provided acupuncture analgesia in addition to SA.Preoperative anxiety[Self-Rating Anxiety Scale(SAS)score and state anxiety inventory(SAI)score],intraoperative stress,vital signs,analgesia,and cooperation,as well as postoperative adverse events,were compared between groups.RESULTS More marked reductions in anxiety were observed among patients in the CAMA group,with corresponding reductions in SAS and SAI scores.During the operation,no change in the secretion of E,NE,or Cor group compared to the preoperative period was observed in the CAMA,which was markedly lower than that in the SA group.Heart rate,blood pressure,and respiratory rate were more stable intraoperatively in the CAMA group.In addition,the incidence of intraoperative pain and the number of additional doses of anesthesia required in the CAMA group were markedly lower than in the SA group.Accordingly,patients in the CAMA group were able to avoid eye movements and eyelid closing leading to greater cooperation with surgeons during surgery.Furthermore,marked reductions in intraoperative adverse effects were observed in the CAMA group,indicating greater overall safety.CONCLUSION Proparacaine SA combined with acupuncture as an analgesic provides improved analgesia with greater safety compared to surface anesthesia with proparacaine during geriatric cataract phacoemulsification.
文摘BACKGROUND Laparoscopic surgery has become a common surgical approach for the clinical treatment of intra-abdominal lesions in recent years.We hypothesized that lumbar block with postoperative patient-controlled intravenous analgesia(PCIA)by butorphanol after gynecological surgery under general anesthesia would be more effective than PCIA by butorphanol alone.AIM To investigate the effect of lumbar block with PCIA by butorphanol after gynecological surgery under general anesthesia.METHODS This study assessed 120 women scheduled for laparoscopic surgery at our hospital between May 2017 and May 2020.They were divided using a random number table into a research group(those who received quadratus lumborum block combined with PCIA analgesia by butorphanol)and a control group(those who received only PCIA analgesia by butorphanol),with 60 patients in each group.Demographic factors,visual analog scale scores for pain,serum inflammatory markers,PCIA compressions,Ramsay scores,and adverse events were compared between groups using a t-test,analysis of variance,orχ2 test,as appropriate.RESULTS There were no significant differences in demographic factors between groups(all P>0.05).The visual analog scale scores of the research group in the resting state 12 h and 24 h postoperatively were significantly lower than those of the control group(P<0.05).Two hours after surgery,there were no significant differences in the levels of serum tumor necrosis factor-α,interleukin(IL)-6,or IL-8 between groups(P>0.05).The serum tumor necrosis factor-αlevels of the research group 24 h postoperatively were significantly lower than those of the control group(P<0.05).The levels of serum IL-6 and IL-8 in the study group 24 h and 48 h postoperatively were significantly lower than those in the control group(P<0.05).CONCLUSION Lumbar block with PCIA with butorphanol after gynecological surgery under general anesthesia significantly improves the analgesic effect and reduces the degree of inflammation,instances of PCIA compression,and adverse reactions.
基金Financial support from the National Natural Sciences Foundation of China(81630094,21732008,81373388,and 81573445)CAMS Innovation Fund for Medical Science(2017-I2M-3–010,2016-I2M-1–004,2016-I2M-1–010,and 2017-I2M-3–011)
文摘Eight new C_(19)-diterpenoid alkaloid arabinosides, named aconicarmichosides E–L(1–8), were isolated from an aqueous extract of the lateral roots of Aconitum carmichaelii(Fu Zi). Their structures were determined by spectroscopic and chemical methods including 2D NMR experiments and acid hydrolysis. Compounds 1–8, together with the previously reported four neoline 14-O-arabinosides from the same plant, represent the only examples of glycosidic diterpenoid alkaloids so far. At a dose of 1.0 mg/kg(i.p.), as compared with the black control, compounds 1, 2, and 4–6 exhibited analgesic effects with 465.6% inhibitions against acetic acid-induced writhing of mice. Structure–activity relationship was also discussed.
基金This work was supported by the National Natural Science Foundation of China(51873175)the Special Fund of Guiding Scientific and Technological Innovation and Development in Gansu Province,China(2019ZX-05).
文摘Quantitative evaluation of analgesic efficacy improves understanding of the antinociceptive mechanisms of new analgesics and provides important guidance for their development.Lappaconitine(LA),a potent analgesic drug extracted from the root of natural Aconitum species,has been clinically used for years because of its effective analgesic and non-addictive properties.However,being limited to ethological experiments,previous studies have mainly investigated the analgesic effect of LA at the behavioral level,and the associated antinociceptive mechanisms are still unclear.In this study,electrocorticogram(ECoG)technology was used to investigate the analgesic effects of two homologous derivatives of LA,Lappaconitine hydrobromide(LAH)and Lappaconitine trifluoroacetate(LAF),on Sprague-Dawley rats subjected to nociceptive laser stimuli,and to further explore their antinociceptive mechanisms.We found that both LAH and LAF were effective in reducing pain,as manifested in the remarkable reduction of nocifensive behaviors and laser-evoked potentials(LEPs)amplitudes(N2 and P2 waves,and gamma-band oscillations),and significantly prolonged latencies of the LEP-N2/P2.These changes in LEPs reflect the similar antinociceptive mechanism of LAF and LAH,i.e.,inhibition of the fast signaling pathways.In addition,there were no changes in the auditory-evoked potential(AEP-N1 component)before and after LAF or LAH treatment,suggesting that neither drug had a central anesthetic effect.Importantly,compared with LAH,LAF was superior in its effects on the magnitudes of gamma-band oscillations and the resting-state spectra,which may be associated with their differences in the octanol/water partition coefficient,degree of dissociation,toxicity,and glycine receptor regulation.Altogether,jointly applying nociceptive laser stimuli and ECoG recordings in rats,we provide solid neural evidence for the analgesic efficacy and antinociceptive mechanisms of derivatives of LA.
文摘Objective:To investigate the effect of preemptive analgesia withflurbiprofen axetil injection on the analgesic effect,inflammatory response,stress response and immune response in patients undergoing thoracoscopic lobectomy.Methods:92 patients with early non-small cell lung cancer who underwent thoracoscopic lobectomy from January 2016 to March 2018 in our hospital were divided into observation group and control group according to the method of random digital table,46 cases in each group.The control group was given routine perioperative analgesia,the observation group was given advanced analgesia mode,and the visual simulation scoring method(visual)was used to observe the patients in the two groups at 4,12,24 and 48 h after operation The results showed that the level of inflammation factor,stress response factor and immune response were significantly higher than that of before operation(T0),when anesthesia woke up(T1),12 hours after operation(T2),24 h after operation(T3)and 48 h after operation(T4).Results:(1)The VAS score of the observation group was significantly lower than that of the control group(P<0.05)at 4,12,24 and 48 h after operation;(2)The levels of IL-6,IL-10,SP-A and TNF-αin the two groups were significantly lower than that of the control group(P<0.05)The level of factor-α,TNF-α)was higher than that of to time point,and showed an upward trend;the level of IL-6,IL-10,TNF-α,SP-A decreased gradually at T3,T4 time points,the level of IL-6,TNF-α,SP-A in T1,T2,T3,T4 time points in the observation group was lower than that of the control group,and the level of IL-10 was higher than that of the control group(P<0.05);(3)Compared with T0 time point,the epinephrine(EPIPH)at T1,T2,T3,T4 time points in the two groups The levels of rine,e,noradrenaline,NE and cortisol in the observation group increased first and then decreased;the levels of E,NE and cor in the observation group were lower than those in the control group at T1,T2,T3 and T4 time points(P<0.05);and(4)Compared with T0 time point,the serum IgG,IgM and IgA levels in the two groups decreased gradually at T1,T2,T3 and T4 time points,but the observation group The levels of IgG,IgM and IgA in serum of group A were higher than those of group B(P<0.05).Conclusion:Preemptive analgesia with flurbiprofen axetil injection can significantly improve the postoperative pain,reduce the level of ;inflammation,reduce the stress response and increase the level of immune response.
基金supported by a grant from Ministry of Education,the New Teachers’Fund for Ph.D Stations(Program No.20110096120011)2011’Program for Excellent Scientific and Technological Innovation Team of Jiangsu Higher Education
文摘The uterine tetanic contraction and uterine artery blood flow reduction are possible reasons for primary dysmenorrhea(PD). In the present study, we aimed to evaluate the uterine relaxant effect and the influence on uterine artery blood velocity of Ge-Gen Decoction(GGD), a well-known Chinese herbal formula. In female ICR mice, uterine contraction was induced by oxytocin exposure following estradiol benzoate pretreatment, and the uterine artery blood velocity was detected by Doppler ultrasound. Histopathological examination of the uterine tissue samples were performed by H&E staining. Ex vivo studies demonstrated that oxytocin, posterior pituitary, or acetylcholine induced contractions in isolated mouse uterus. GGD inhibited both spontaneous and stimulated contractions. In vivo study demonstrated that GGD significantly reduced oxytocin-induced writhing responses with a maximal inhibition of 87%. Further study demonstrated that GGD normalized oxytocin-induced abnormalities of prostaglandins F_2 alpha(PGF_(2α)) and Ca^(2+) in mice. In addition, injection of oxytocin induced a decrease in uterine artery blood flow velocity. Pretreatment with GGD reversed the oxytocin response on blood flow velocity. Histopathological examination showed pretreatment with GGD alleviated inflammation and edema in the uterus when compared with the model group. Both ex vivo and in vivo results indicated that GGD possessed a significant spasmolytic effect on uterine tetanic contraction as well as improvement on uterine artery blood velocity which may involve PGF_(2α) and Ca^(2+) signaling, suggesting that GGD may have a clinic potential in PD therapy.
基金Financial support of the National Natural Sciences Foundation of China(81630094,21732008,and 81730093)CAMS Innovation Fund for Medical Science of China(2017-I2M-3-010 and 2016I2M-1-010)the Drug Innovation Major Project(2018ZX09711001-001-001,2018ZX09711001-001-003,and 2018ZX09711001-003-001,China)
文摘Three new C20-diterpenoid alkaloids with a sulfonic acid unit,named aconicarmisulfonines B and C(1 and 2)and chuanfusulfonine A(3),respectively,were isolated from the Aconitum carmichaelii lateral roots("fu zi"in Chinese).Structures of 1-3 were determined by spectroscopic data analysis.Intriguing chemical properties and reactions were observed for the C20-diterpenoid alkaloids:(a)specific selective nucleophilic addition of the carbonyl(C-12)in 1 with CD3 OD;(b)interconversion between 1 and 2 in D2 O;(c)stereo-and/or regioselective deuterations of H-11αin 1-3 and both H-11αand H-11βin aconicarmisulfonine A(4);(d)TMSP-2,2,3,3-d4 promoted cleavage of the C-12-C-13 bond of 4 in D2 O;(e)dehydrogenation of 4 in pyridine-d5,and(f)Na2 SO3-assisted dehydrogenation and N-deethylation of songorine(5,a putative precursor of 1-4).Biogenetically,1 and 2 are correlated with 4,for which the same novel carbon skeleton is proposed to be derived from semipinacol rearrangements via migrations of C-13-C-16 and C-15-C-16 bonds of the napelline-type skeleton,respectively.Meanwhile,3 is a highly possible precursor or a concurrent product in the biosynthetic pathways of 1,2,and 4.In the acetic acid-induced mice writhing assay,at 1.0 mg/kg(i.p.),compounds 1,2,5,5 a,and 5 b exhibited analgesic effects against mice writhing.
