Twelve healthy rats were divided into the T-2 toxin group receiving gavage of 1 mg/kg T-2 toxin and the control group receiving gavage of normal saline. Total relative concentrations of T-2 toxin and HT-2 toxin in the...Twelve healthy rats were divided into the T-2 toxin group receiving gavage of 1 mg/kg T-2 toxin and the control group receiving gavage of normal saline. Total relative concentrations of T-2 toxin and HT-2 toxin in the skeletal system(thighbone, knee joints, and costal cartilage) were significantly higher than those in the heart, liver, and kidneys(P < 0.05). The relative concentrations of T-2 toxin and HT-2 toxin in the skeletal system(thighbone and costal cartilage) were also significantly higher than those in the heart, liver, and kidneys. The rats administered T-2 toxin showed rapid metabolism compared with that in rats administered HT-2 toxin, and the metabolic conversion rates in the different tissues were 68.20%-90.70%.展开更多
[Objectives]To investigate the acute toxicity and hepatoprotective effect of Jinchuan formula plum wine extract on mice,determine its safety range,and evaluate its hepatoprotective effect.[Methods]The median lethal do...[Objectives]To investigate the acute toxicity and hepatoprotective effect of Jinchuan formula plum wine extract on mice,determine its safety range,and evaluate its hepatoprotective effect.[Methods]The median lethal dose(LD_(50))was determined by acute toxicity test with the toxic reaction and mortality of mice as indexes.Sixty Kunming mice were randomly divided into 6 groups:normal control group,model group(ConA-induced liver injury model),Jinchuan formula plum wine high,medium and low dose groups(1.0,0.5,0.25 g/kg)and silybin group(0.1 g/kg).The levels of ALT,AST,LDH in serum and TG,VLDL in liver were measured.After HE staining,the pathological changes of liver tissue in mice were observed,and the liver protective effect of Jinchuan formula plum wine extract was analyzed and evaluated.[Results]LD_(50)was 11.18 g/kg,and the 95%confidence limit of LD_(50)was 10.31-12.05 g/kg.The high-dose group of Jinchuan formula plum wine extract could significantly reduce the serum ALT and AST activities of ConA-induced liver injury mice(P<0.05).[Conclusions]Jinchuan formula plum wine extract is relatively safe,and also has a protective effect on liver injury.展开更多
Systemic toxicity caused by repeated exposure to both polar and nonpolar leachables of di(2-ethylhexyl)-1,2-cyclohexane plasticized polyvinyl chloride(PVC)was evaluated with dual routes of parenteral administration me...Systemic toxicity caused by repeated exposure to both polar and nonpolar leachables of di(2-ethylhexyl)-1,2-cyclohexane plasticized polyvinyl chloride(PVC)was evaluated with dual routes of parenteral administration method on rats in the study.Experimental group and control group were designed by researchers.Tail intravenous injection with 0.9%sodium chloride injection extracts and intraperitoneal injection with corn oil extracts were conducted to the experimental rats while tail intravenous injection with 0.9%sodium chloride Injection and intraperitoneal injection with corn oil were conducted to the control rats.After 14 days,blood specimens were collected for clinical pathology(hematology and clinical chemistry)analysis.Selected organs were weighed and a histopathological examination was conducted.As a result,compared with the control animals,there were no toxicity-related changes on the parameters above.The results show that the rats do not show obvious systemic toxicity reaction caused by repeated exposure with dual routes of parenteral administration method on rats after administration with both polar and nonpolar exacts of di(2-ethylhexyl)-1,2-cyclohexane plasticized PVC simultaneously up for 14 days.展开更多
Mg alloys have mechanical properties compatible with human bones.However,their rapid degradation and associated foreign body reactions in vivo significantly limit their application for human implants.In this study,thr...Mg alloys have mechanical properties compatible with human bones.However,their rapid degradation and associated foreign body reactions in vivo significantly limit their application for human implants.In this study,three differently processed Mg alloys,pure Mg(PM),cold extruded Mg alloy AZ31(CE AZ31),and fully annealed AZ31 Mg alloy(FA AZ31)were comparatively investigated for their potential as implants using a rat model.All three implanted Mg alloys do not show any impact on hepato-and renal function,nor any signs of observable changes to vital organs.Proteomics analysis of tissues directly contacting the implants 2.5 months post implantation revealed that FA AZ31 activates very few inflammation and immune associated signaling pathways;while the CE AZ31 and PM produce more significant inflammatory responses as confirmed by cytokine array analyses.Further,FA AZ31 activated pathways for cell organization and development that may improve the recovery of injured tissues.Structurally,EBSD analysis reveals that the FA AZ31 alloy has a higher ratio of first-order pyramidal orientated(10–11){10–1–2}grain texture with a value of 0.25,while PM and CE AZ31 alloys have lower ratios of first-order pyramidal orientated texture with the values of 0.16 and 0.17,respectively.This is associated with recovery and recrystallisation during annealing which promotes grain texture which exhibits enhanced degradation behaviours and induces a more limited immune response in vivo.In conclusion,the FA AZ31 demonstrated better biocompatibility and corrosion resistance and is a promising candidate for metal-based degradable implants which warrants further investigation.展开更多
Objective:To assess the potential toxicity of hydroalcoholic extract of Allium affine(A.affine)aerial parts after acute and sub-acute administration in female and male Wistar rats.Methods:For acute toxicity assay,anim...Objective:To assess the potential toxicity of hydroalcoholic extract of Allium affine(A.affine)aerial parts after acute and sub-acute administration in female and male Wistar rats.Methods:For acute toxicity assay,animals orally received the limit test dose of 2000 mg/kg of A.affine extract and were observed for 2 weeks.For sub-acute toxicity study,rats were orally treated with 125,250,and 500 mg/kg/day of the extract over 28 days,and hematological,biochemical,and histological evaluations were then conducted.Results:All rats were alive with normal body weight gain over 14 days,with LD50˃2000 mg/kg.No abnormality in body weight changes but significant increases in the relative weight of spleen and lung were detected after administration of the highest dose of extract for 28 days in sub-acute assay.Hematological analysis showed prominent elevations in total white blood cells in male rats and neutrophils count in female rats after exposure to 500 mg/kg of A.affine extract.In biochemical evaluations,significant increases in serum creatinine level(female rats,250 and 500 mg/kg)and in aspartate aminotransferase(male and female rate,500 mg/kg)and alanine aminotransferase(male,250 and 500 mg/kg and female,500 mg/kg)activities,however,notable decreases in serum blood glucose(male rats,125 and 500 mg/kg),triglycerides(male rats,500 mg/kg and female rates,250 mg/kg),and low-density lipoprotein cholesterol levels(male,250 mg/kg)were found.Histological examinations presented slight portal inflammation in liver tissue,moderate pneumocyte hyperplasia,congestion and peri-bronchial inflammation in lung tissue,and mild histiocytosis and lymphoid follicular activation in spleen tissue after exposure to 500 mg/kg of A.affine extract in male and female animals.Conclusions:The present investigation reveals the safety of A.affine extract at doses of lower than 250 mg/kg in rats and monitoring of lung,spleen,and liver functions is suggested during excessive and prolonged uses.展开更多
We optimized the extraction process of Lysurus mokusin(L.)Fr.insecticidal compound(LMIC)using response surface methodology with ultrasonic extraction(UE).The surface morphologies of maceration extract(ME)and UE residu...We optimized the extraction process of Lysurus mokusin(L.)Fr.insecticidal compound(LMIC)using response surface methodology with ultrasonic extraction(UE).The surface morphologies of maceration extract(ME)and UE residues were compared by scanning electron microscopy,and then the activity of LMIC on Lymantria dispar(Asian gypsy moths)larvae was determined.Results showed that the optimal condition of UE was followed by 80 min of extraction time,60%of ethanol concentration and 80 mL g^-1 of liquid–solid ratio.The surface morphologies of UE residue were looser and rougher than ME residue.The corrected mortalities of LMIC on L.dispar larvae was 59.77%.This result indicated that L.mokusin was a good candidate as pesticide for pest management.展开更多
The impact of diflubenzuron (DFB) on Tetrahymena pyriformis, a ciliated protiste was studied. The treatment with DFB at concentrations of 10 and 20 μg/mL could appreciably reduce the growth of the protiste. The surve...The impact of diflubenzuron (DFB) on Tetrahymena pyriformis, a ciliated protiste was studied. The treatment with DFB at concentrations of 10 and 20 μg/mL could appreciably reduce the growth of the protiste. The surveillance of protozoa′s respiratory metabolism with polarography technique showed a sensitive inhibition of its oxygen consumption, and at 20 μg/mL concentration the oxygen consumption was increased. For any malformation of morphology and perturbation in swimming trajectory, the neutral red coloration was done. This technique (neutral red) showed that there was a toxic effect of DFB on T. pyriformis, especially at the highest concentration; this toxicity was translated by rotatory swimming in same place and the increasing of coloration quantity in digestive vacuoles. Fig 5, Ref展开更多
OBJECTIVE:To study the anti-inflammatory and anti-tussive effects of Qingfei Dayuan granules(清肺达原颗粒,QFDY),and to evaluate the acute and sub-chronic toxicity of QFDY.METHODS:Anti-inflammatory effects were evaluat...OBJECTIVE:To study the anti-inflammatory and anti-tussive effects of Qingfei Dayuan granules(清肺达原颗粒,QFDY),and to evaluate the acute and sub-chronic toxicity of QFDY.METHODS:Anti-inflammatory effects were evaluated by murine model of xylene induced ear edema in mice.Ear swelling degree was calculated and tumor necrosis factor-α,interleukin-1βand interleukin-6 were determined.Anti-tussive evaluations were carried out in the mouse cough model induced by ammonia liquor.Latent period cough and number of cough within 3 min were counted.In acute toxicity study,the rats were randomly divided into test group and solvent control group.Body weighs,food intakes and general clinical signs were monitored.In the sub-chronic toxicity study,QFDY was administered to rats at 0,4,8 and 16 g/kg per day for 28 and 30 d of post treatment was conducted.Mortalities,clinical signs,body weight changes,food intakes,ophthalmological examinations,hematological parameters,biochemical indicators,electrolyte indicators,urinalyses and histopathological examinations were monitored.RESULTS:QFDY significantly inhibited the development of ear edema in anti-inflammatory assay and decreased cough frequency caused by ammonia liquor.The results presented a dose-effect relationship.In acute toxicity study,no abnormality exhibited at dose of 24.0 g/kg per day during the 14-d observation period.In the sub-chronic toxicity study,higher reticulocyte count,lymphocyte and lower Cl-,blood urea nitrogen were analyzed compared with the solvent control group.But the differences were considered to be incidental and not clinically toxic.Obvious dose-effect relationship of urine color was observed,and the three test groups at the end of the experiments resulted in significant increase in urobilinogen,bilirubin,ketone body and urine leukocyte.However,all the positive indicators returned to normal in the recovery period.Therefore,no toxicological changes were found during the study period.CONCLUSION:QFDY showed significant anti-inflammatory and anti-tussive effects in mice.The lethal dose(LD50)of per oral QFDY in rats was estimated to be more than 24.0 g/kg per day and the no observed adverse effect level was over 16 g/kg per day,which suggested that QFDY is relatively safe for oral medication at the present dose on rats.Our experimental results provide a reference for the further development and research of QFDY.展开更多
It has previously been shown that tryptophan, the biosynthesis precursor ofPeganum harmala alkaloids, and its derivatives have anti-TMV activity bothin vitro and in vivo. Further exploration of this led to the identif...It has previously been shown that tryptophan, the biosynthesis precursor ofPeganum harmala alkaloids, and its derivatives have anti-TMV activity bothin vitro and in vivo. Further exploration of this led to the identification of NK0238as a highly effective agent for the prevention and control of diseases caused byplant viruses, but the existing routes are unsuitable for its large-scale synthesis.This study optimized a route for two-step synthesis of this virucide candidate viareaction of L-tryptophan with triphosgene to produce L-tryptophan-N-carboxylicanhydride, which then reacts with n-octylamine to give NK0238 at up to 94%yield and nearly 97% HPLC purity. In addition, the route was used for thepreparation of NK0238 on a > 40 g scale permitting further assessment of itsantivirus activity in the greenhouse and field experiments, and toxicity tests.NK0238 exhibited useful antiviral activities against a variety of viruses both ingreenhouse and field experiments. The toxicity tests showed that NK0238 wasnot acutely toxic to birds, fish, honey bees and silkworms. The optimized routeprovides a solid foundation for its large-scale synthesis and subsequent efficacyand toxicity studies, its excellent activity and safety make NK0238 a promisingdrug candidate for further development.展开更多
OBJECTIVE:To investigate the efficacy of Fig fruit powder and olive on hepatic,renal and splenic injury induced by 2-nitropropane(2-NP)in mice,especially if they were used in combination.METHODS:A total of 40 adult BA...OBJECTIVE:To investigate the efficacy of Fig fruit powder and olive on hepatic,renal and splenic injury induced by 2-nitropropane(2-NP)in mice,especially if they were used in combination.METHODS:A total of 40 adult BALB/c male mice weighting 25-30 g/each.Mice were categorized into five groups(8 each).Group 1 as negative control.Group 2 as positive control group intraperitoneally injected with 2-NP(100 mg/kg b.w.)3 times/weekly for eight weeks.Group 3 injected with 2-NP and were orally supplemented with Fig(300 mg/kg).Group 4 injected with 2-NP and were orally supplemented with olive(100 mg/kg).Group 5 injected with 2-NP and were orally supplemented with mixture of Fig and olive(3∶1 respectively).RESULTS:Histopathological observation of liver in mice treated with 2-NP showed cellular degeneration,pyknosis,and congestion of the portal vein.In kidney there were disorganization of the cortical tissues,cellular necrosis and plenty of inflammatory lymphocytic aggregation.Significant elevations in liver function parameters(alanine aminotransferase and aspartate aminotransferase),m RNA expression levels of tumor necrosis factor-α,nicotinamide adenine dinucleotide phosphate oxidase and cyclooxygenase were detected as anti-inflammatory markers and 5-lipoxygenase,interleukin-1βand interleukin-6 as inflammatory biomarkers for liver and spleen,also significant elevations was detected in lipid peroxidation levels.The levels of antioxidants,glutathione,glutathione peroxidase,catalase and superoxide dismutase were significantly decreased.CONCLUSION:our findings indicated that Fig fruit powder and olive protected against hepatic,renal and splenic injury induced with 2-NP in mice,especially if they were used in combination.展开更多
Along with the increase in the consumption of traditional Chinese medicine(TCM), the safety of TCM has dramatically attracted the attention and concern of the public. Here, we review previous studies, which focused ma...Along with the increase in the consumption of traditional Chinese medicine(TCM), the safety of TCM has dramatically attracted the attention and concern of the public. Here, we review previous studies, which focused mainly on the toxicity of toxic TCM and the interpretations for combination, to elaborate on advances and important issues existing in the safety evaluation of TCM, aiming to provide scientific advice for the clinical use. Moreover, we emphasize the importance of a safe evaluation system for TCM based on the material basis for toxicity, which integrates new toxicity testing strategy and is launched under the guidance of TCM theories in future researches.展开更多
Objective:To determine the toxicity profile,anti-angiogenic and antibacterial activity of the crude and semi-crude leaf extracts of Tinomiscium philippinense(T.philippinense).Methods:The leaves of T.philippinense were...Objective:To determine the toxicity profile,anti-angiogenic and antibacterial activity of the crude and semi-crude leaf extracts of Tinomiscium philippinense(T.philippinense).Methods:The leaves of T.philippinense were extracted with methanol and partitioned with solvents of different polarities,namely,hexane,dichloromethane and butanol.The extracts were subjected to duck chorioallantoic membrane assay to establish its anti-angiogenic property.Microwell assay was utilized to determine the minimum inhibitory concentration and minimum bactericidal concentration of the different extracts of the plant.Results:The dichloromethane leaf extract of T.philippinense at 1000μg/disc showed the highest anti-angiogenic activity with 37.46%inhibition.All the fractions exhibited a bacteriostatic and bactericidal effect on the three bacterial strains with Pseudomonas aeruginosa,a Gram negative lactose fermenter exhibiting a higher sensitivity to dichloromethane semi-crude extract among the treatment groups.For the toxicity test,no mortality and no change in behavior were observed in the Sprague-Dawley rats 14 days after the oral administration of the plant extracts.The methanolic leaf extract of T.philippinense is non-toxic at a maximum dose of 5000 mg/kg.Conclusions:The dichloromethane leaf extract of T.philippinense is a potential antiangiogenic endemic plant species.This plant extract is also a potential antibacterial candidate as determined by microwell assay.The anti-angiogenic and antibacterial activity of the plant may be attributed to the essential oil,steroid,flavonoid,sterol and triterpene content of the plant.展开更多
Increasing lung diseases,mutating coronaviruses,and the development of new compounds urgently require biomimetic in vitro lung models for lung pathology,toxicology,and pharmacology.The current construction strategies ...Increasing lung diseases,mutating coronaviruses,and the development of new compounds urgently require biomimetic in vitro lung models for lung pathology,toxicology,and pharmacology.The current construction strategies for lung models mainly include animal models,2D cell culture,lung-on-a-chip,and lung organoids.However,current models face difficulties in reproducing in vivo-like alveolar size and vesicle-like structures,and are unable to contain multiple cell types.In this study,a strategy for constructing alveolar models based on degradable hydrogel microspheres is proposed.Hydrogel microspheres,200-250μm in diameter,were prepared using a self-developed printing technique driven by alternating viscous and inertial forces.Microcapsules were further constructed using a coacervation-based layer-by-layer technique and core liquefaction.Three types of cells were inoculated and co-cultured on hydrogel capsules based on optimized microcapsule surface treatment strategies.Finally,an in vitro three-dimensional endothelial alveolar model with a multicellular composition and vesicle-like structure with a diameter of approximately 230μm was successfully constructed.Cells in the constructed alveolar model maintained a high survival rate.The LD_(50)values of glutaraldehyde based on the constructed models were in good agreement with the reference values,validating the potential of the model for future toxicant and drug detection.展开更多
基金partially supported by National Natural Scientific Foundation of China[81620108026,81302393]
文摘Twelve healthy rats were divided into the T-2 toxin group receiving gavage of 1 mg/kg T-2 toxin and the control group receiving gavage of normal saline. Total relative concentrations of T-2 toxin and HT-2 toxin in the skeletal system(thighbone, knee joints, and costal cartilage) were significantly higher than those in the heart, liver, and kidneys(P < 0.05). The relative concentrations of T-2 toxin and HT-2 toxin in the skeletal system(thighbone and costal cartilage) were also significantly higher than those in the heart, liver, and kidneys. The rats administered T-2 toxin showed rapid metabolism compared with that in rats administered HT-2 toxin, and the metabolic conversion rates in the different tissues were 68.20%-90.70%.
文摘[Objectives]To investigate the acute toxicity and hepatoprotective effect of Jinchuan formula plum wine extract on mice,determine its safety range,and evaluate its hepatoprotective effect.[Methods]The median lethal dose(LD_(50))was determined by acute toxicity test with the toxic reaction and mortality of mice as indexes.Sixty Kunming mice were randomly divided into 6 groups:normal control group,model group(ConA-induced liver injury model),Jinchuan formula plum wine high,medium and low dose groups(1.0,0.5,0.25 g/kg)and silybin group(0.1 g/kg).The levels of ALT,AST,LDH in serum and TG,VLDL in liver were measured.After HE staining,the pathological changes of liver tissue in mice were observed,and the liver protective effect of Jinchuan formula plum wine extract was analyzed and evaluated.[Results]LD_(50)was 11.18 g/kg,and the 95%confidence limit of LD_(50)was 10.31-12.05 g/kg.The high-dose group of Jinchuan formula plum wine extract could significantly reduce the serum ALT and AST activities of ConA-induced liver injury mice(P<0.05).[Conclusions]Jinchuan formula plum wine extract is relatively safe,and also has a protective effect on liver injury.
基金The authors are grateful to the financial support of National Key Research and Development Program,No.2016YFC1103205.
文摘Systemic toxicity caused by repeated exposure to both polar and nonpolar leachables of di(2-ethylhexyl)-1,2-cyclohexane plasticized polyvinyl chloride(PVC)was evaluated with dual routes of parenteral administration method on rats in the study.Experimental group and control group were designed by researchers.Tail intravenous injection with 0.9%sodium chloride injection extracts and intraperitoneal injection with corn oil extracts were conducted to the experimental rats while tail intravenous injection with 0.9%sodium chloride Injection and intraperitoneal injection with corn oil were conducted to the control rats.After 14 days,blood specimens were collected for clinical pathology(hematology and clinical chemistry)analysis.Selected organs were weighed and a histopathological examination was conducted.As a result,compared with the control animals,there were no toxicity-related changes on the parameters above.The results show that the rats do not show obvious systemic toxicity reaction caused by repeated exposure with dual routes of parenteral administration method on rats after administration with both polar and nonpolar exacts of di(2-ethylhexyl)-1,2-cyclohexane plasticized PVC simultaneously up for 14 days.
基金supported in part by JSPS research grant(No.P16718)Natural Science Foundation of Guangdong Province(No.2020A1515010855)+2 种基金National Science Foundation of China(31971355)Genecology MCR Seed Funding of University of the Sunshine CoastDeng Feng Project of Foshan First People’s Hospital(2019A008)。
文摘Mg alloys have mechanical properties compatible with human bones.However,their rapid degradation and associated foreign body reactions in vivo significantly limit their application for human implants.In this study,three differently processed Mg alloys,pure Mg(PM),cold extruded Mg alloy AZ31(CE AZ31),and fully annealed AZ31 Mg alloy(FA AZ31)were comparatively investigated for their potential as implants using a rat model.All three implanted Mg alloys do not show any impact on hepato-and renal function,nor any signs of observable changes to vital organs.Proteomics analysis of tissues directly contacting the implants 2.5 months post implantation revealed that FA AZ31 activates very few inflammation and immune associated signaling pathways;while the CE AZ31 and PM produce more significant inflammatory responses as confirmed by cytokine array analyses.Further,FA AZ31 activated pathways for cell organization and development that may improve the recovery of injured tissues.Structurally,EBSD analysis reveals that the FA AZ31 alloy has a higher ratio of first-order pyramidal orientated(10–11){10–1–2}grain texture with a value of 0.25,while PM and CE AZ31 alloys have lower ratios of first-order pyramidal orientated texture with the values of 0.16 and 0.17,respectively.This is associated with recovery and recrystallisation during annealing which promotes grain texture which exhibits enhanced degradation behaviours and induces a more limited immune response in vivo.In conclusion,the FA AZ31 demonstrated better biocompatibility and corrosion resistance and is a promising candidate for metal-based degradable implants which warrants further investigation.
基金financially supported by Vice-Chancellery for Research and Technology,Isfahan University of Medical Sciences(Grant No.399187).
文摘Objective:To assess the potential toxicity of hydroalcoholic extract of Allium affine(A.affine)aerial parts after acute and sub-acute administration in female and male Wistar rats.Methods:For acute toxicity assay,animals orally received the limit test dose of 2000 mg/kg of A.affine extract and were observed for 2 weeks.For sub-acute toxicity study,rats were orally treated with 125,250,and 500 mg/kg/day of the extract over 28 days,and hematological,biochemical,and histological evaluations were then conducted.Results:All rats were alive with normal body weight gain over 14 days,with LD50˃2000 mg/kg.No abnormality in body weight changes but significant increases in the relative weight of spleen and lung were detected after administration of the highest dose of extract for 28 days in sub-acute assay.Hematological analysis showed prominent elevations in total white blood cells in male rats and neutrophils count in female rats after exposure to 500 mg/kg of A.affine extract.In biochemical evaluations,significant increases in serum creatinine level(female rats,250 and 500 mg/kg)and in aspartate aminotransferase(male and female rate,500 mg/kg)and alanine aminotransferase(male,250 and 500 mg/kg and female,500 mg/kg)activities,however,notable decreases in serum blood glucose(male rats,125 and 500 mg/kg),triglycerides(male rats,500 mg/kg and female rates,250 mg/kg),and low-density lipoprotein cholesterol levels(male,250 mg/kg)were found.Histological examinations presented slight portal inflammation in liver tissue,moderate pneumocyte hyperplasia,congestion and peri-bronchial inflammation in lung tissue,and mild histiocytosis and lymphoid follicular activation in spleen tissue after exposure to 500 mg/kg of A.affine extract in male and female animals.Conclusions:The present investigation reveals the safety of A.affine extract at doses of lower than 250 mg/kg in rats and monitoring of lung,spleen,and liver functions is suggested during excessive and prolonged uses.
基金The work was supported by the Central University Fundamental Research Funds Special Fund Project[2572016AA03,25720171118]Harbin Applied Technology Research and Development Project[2016RAXXJ035]the Central Financial Forest Science and Technology Promotion Demonstration Fund Project[JLT[2016]13].
文摘We optimized the extraction process of Lysurus mokusin(L.)Fr.insecticidal compound(LMIC)using response surface methodology with ultrasonic extraction(UE).The surface morphologies of maceration extract(ME)and UE residues were compared by scanning electron microscopy,and then the activity of LMIC on Lymantria dispar(Asian gypsy moths)larvae was determined.Results showed that the optimal condition of UE was followed by 80 min of extraction time,60%of ethanol concentration and 80 mL g^-1 of liquid–solid ratio.The surface morphologies of UE residue were looser and rougher than ME residue.The corrected mortalities of LMIC on L.dispar larvae was 59.77%.This result indicated that L.mokusin was a good candidate as pesticide for pest management.
文摘The impact of diflubenzuron (DFB) on Tetrahymena pyriformis, a ciliated protiste was studied. The treatment with DFB at concentrations of 10 and 20 μg/mL could appreciably reduce the growth of the protiste. The surveillance of protozoa′s respiratory metabolism with polarography technique showed a sensitive inhibition of its oxygen consumption, and at 20 μg/mL concentration the oxygen consumption was increased. For any malformation of morphology and perturbation in swimming trajectory, the neutral red coloration was done. This technique (neutral red) showed that there was a toxic effect of DFB on T. pyriformis, especially at the highest concentration; this toxicity was translated by rotatory swimming in same place and the increasing of coloration quantity in digestive vacuoles. Fig 5, Ref
基金Department of Science and Technology of Hubei Province:Preclinical Study on Qingfei Dayuan granules (No.2021BGE017)
文摘OBJECTIVE:To study the anti-inflammatory and anti-tussive effects of Qingfei Dayuan granules(清肺达原颗粒,QFDY),and to evaluate the acute and sub-chronic toxicity of QFDY.METHODS:Anti-inflammatory effects were evaluated by murine model of xylene induced ear edema in mice.Ear swelling degree was calculated and tumor necrosis factor-α,interleukin-1βand interleukin-6 were determined.Anti-tussive evaluations were carried out in the mouse cough model induced by ammonia liquor.Latent period cough and number of cough within 3 min were counted.In acute toxicity study,the rats were randomly divided into test group and solvent control group.Body weighs,food intakes and general clinical signs were monitored.In the sub-chronic toxicity study,QFDY was administered to rats at 0,4,8 and 16 g/kg per day for 28 and 30 d of post treatment was conducted.Mortalities,clinical signs,body weight changes,food intakes,ophthalmological examinations,hematological parameters,biochemical indicators,electrolyte indicators,urinalyses and histopathological examinations were monitored.RESULTS:QFDY significantly inhibited the development of ear edema in anti-inflammatory assay and decreased cough frequency caused by ammonia liquor.The results presented a dose-effect relationship.In acute toxicity study,no abnormality exhibited at dose of 24.0 g/kg per day during the 14-d observation period.In the sub-chronic toxicity study,higher reticulocyte count,lymphocyte and lower Cl-,blood urea nitrogen were analyzed compared with the solvent control group.But the differences were considered to be incidental and not clinically toxic.Obvious dose-effect relationship of urine color was observed,and the three test groups at the end of the experiments resulted in significant increase in urobilinogen,bilirubin,ketone body and urine leukocyte.However,all the positive indicators returned to normal in the recovery period.Therefore,no toxicological changes were found during the study period.CONCLUSION:QFDY showed significant anti-inflammatory and anti-tussive effects in mice.The lethal dose(LD50)of per oral QFDY in rats was estimated to be more than 24.0 g/kg per day and the no observed adverse effect level was over 16 g/kg per day,which suggested that QFDY is relatively safe for oral medication at the present dose on rats.Our experimental results provide a reference for the further development and research of QFDY.
基金The authors are grateful to the National Natural Science Foundation of China(21977056,21732002)the Fundamental Research Funds for the Central Universities,Nankai University(63201043)for generous financial support for their programs.
文摘It has previously been shown that tryptophan, the biosynthesis precursor ofPeganum harmala alkaloids, and its derivatives have anti-TMV activity bothin vitro and in vivo. Further exploration of this led to the identification of NK0238as a highly effective agent for the prevention and control of diseases caused byplant viruses, but the existing routes are unsuitable for its large-scale synthesis.This study optimized a route for two-step synthesis of this virucide candidate viareaction of L-tryptophan with triphosgene to produce L-tryptophan-N-carboxylicanhydride, which then reacts with n-octylamine to give NK0238 at up to 94%yield and nearly 97% HPLC purity. In addition, the route was used for thepreparation of NK0238 on a > 40 g scale permitting further assessment of itsantivirus activity in the greenhouse and field experiments, and toxicity tests.NK0238 exhibited useful antiviral activities against a variety of viruses both ingreenhouse and field experiments. The toxicity tests showed that NK0238 wasnot acutely toxic to birds, fish, honey bees and silkworms. The optimized routeprovides a solid foundation for its large-scale synthesis and subsequent efficacyand toxicity studies, its excellent activity and safety make NK0238 a promisingdrug candidate for further development.
文摘OBJECTIVE:To investigate the efficacy of Fig fruit powder and olive on hepatic,renal and splenic injury induced by 2-nitropropane(2-NP)in mice,especially if they were used in combination.METHODS:A total of 40 adult BALB/c male mice weighting 25-30 g/each.Mice were categorized into five groups(8 each).Group 1 as negative control.Group 2 as positive control group intraperitoneally injected with 2-NP(100 mg/kg b.w.)3 times/weekly for eight weeks.Group 3 injected with 2-NP and were orally supplemented with Fig(300 mg/kg).Group 4 injected with 2-NP and were orally supplemented with olive(100 mg/kg).Group 5 injected with 2-NP and were orally supplemented with mixture of Fig and olive(3∶1 respectively).RESULTS:Histopathological observation of liver in mice treated with 2-NP showed cellular degeneration,pyknosis,and congestion of the portal vein.In kidney there were disorganization of the cortical tissues,cellular necrosis and plenty of inflammatory lymphocytic aggregation.Significant elevations in liver function parameters(alanine aminotransferase and aspartate aminotransferase),m RNA expression levels of tumor necrosis factor-α,nicotinamide adenine dinucleotide phosphate oxidase and cyclooxygenase were detected as anti-inflammatory markers and 5-lipoxygenase,interleukin-1βand interleukin-6 as inflammatory biomarkers for liver and spleen,also significant elevations was detected in lipid peroxidation levels.The levels of antioxidants,glutathione,glutathione peroxidase,catalase and superoxide dismutase were significantly decreased.CONCLUSION:our findings indicated that Fig fruit powder and olive protected against hepatic,renal and splenic injury induced with 2-NP in mice,especially if they were used in combination.
基金financially supported by the National Natural Science Foundation of China(No.81630102 and No.81803833)
文摘Along with the increase in the consumption of traditional Chinese medicine(TCM), the safety of TCM has dramatically attracted the attention and concern of the public. Here, we review previous studies, which focused mainly on the toxicity of toxic TCM and the interpretations for combination, to elaborate on advances and important issues existing in the safety evaluation of TCM, aiming to provide scientific advice for the clinical use. Moreover, we emphasize the importance of a safe evaluation system for TCM based on the material basis for toxicity, which integrates new toxicity testing strategy and is launched under the guidance of TCM theories in future researches.
基金Supported by the Research Center for the Natural and Applied Sciences and the DOST-National Science Consortium.
文摘Objective:To determine the toxicity profile,anti-angiogenic and antibacterial activity of the crude and semi-crude leaf extracts of Tinomiscium philippinense(T.philippinense).Methods:The leaves of T.philippinense were extracted with methanol and partitioned with solvents of different polarities,namely,hexane,dichloromethane and butanol.The extracts were subjected to duck chorioallantoic membrane assay to establish its anti-angiogenic property.Microwell assay was utilized to determine the minimum inhibitory concentration and minimum bactericidal concentration of the different extracts of the plant.Results:The dichloromethane leaf extract of T.philippinense at 1000μg/disc showed the highest anti-angiogenic activity with 37.46%inhibition.All the fractions exhibited a bacteriostatic and bactericidal effect on the three bacterial strains with Pseudomonas aeruginosa,a Gram negative lactose fermenter exhibiting a higher sensitivity to dichloromethane semi-crude extract among the treatment groups.For the toxicity test,no mortality and no change in behavior were observed in the Sprague-Dawley rats 14 days after the oral administration of the plant extracts.The methanolic leaf extract of T.philippinense is non-toxic at a maximum dose of 5000 mg/kg.Conclusions:The dichloromethane leaf extract of T.philippinense is a potential antiangiogenic endemic plant species.This plant extract is also a potential antibacterial candidate as determined by microwell assay.The anti-angiogenic and antibacterial activity of the plant may be attributed to the essential oil,steroid,flavonoid,sterol and triterpene content of the plant.
基金supported by Beijing Municipal Natural Science Foundation of China(Grant No.3212007)Tsinghua University Spring Breeze Fund(Grant No.20201080760)+2 种基金Tsinghua University Ini-tiative Scientific Research Program(Grant No.20213080030)Na-tional Key Research and Development Program of China(Grant No.2018YFA0703004)National Natural Science Foundation of China(Grant No.52175273),and 111 Project(Grant No.B17026).
文摘Increasing lung diseases,mutating coronaviruses,and the development of new compounds urgently require biomimetic in vitro lung models for lung pathology,toxicology,and pharmacology.The current construction strategies for lung models mainly include animal models,2D cell culture,lung-on-a-chip,and lung organoids.However,current models face difficulties in reproducing in vivo-like alveolar size and vesicle-like structures,and are unable to contain multiple cell types.In this study,a strategy for constructing alveolar models based on degradable hydrogel microspheres is proposed.Hydrogel microspheres,200-250μm in diameter,were prepared using a self-developed printing technique driven by alternating viscous and inertial forces.Microcapsules were further constructed using a coacervation-based layer-by-layer technique and core liquefaction.Three types of cells were inoculated and co-cultured on hydrogel capsules based on optimized microcapsule surface treatment strategies.Finally,an in vitro three-dimensional endothelial alveolar model with a multicellular composition and vesicle-like structure with a diameter of approximately 230μm was successfully constructed.Cells in the constructed alveolar model maintained a high survival rate.The LD_(50)values of glutaraldehyde based on the constructed models were in good agreement with the reference values,validating the potential of the model for future toxicant and drug detection.
