Indole alkaloids extract(IAAS)was prepared from leaves of Alstonia scholaris(L.)R.Br.,an evergreen tropical plant widely distributed throughout the world.This plant has been used historically by the Dai ethnic people ...Indole alkaloids extract(IAAS)was prepared from leaves of Alstonia scholaris(L.)R.Br.,an evergreen tropical plant widely distributed throughout the world.This plant has been used historically by the Dai ethnic people of China to treat respiratory diseases.This study evaluated the genotoxicity and safety pharmacology of IAAS to support clinical use.The bacterial reverse mutation(Ames)test,in vitro mammalian chromosomal aberration test,and in vivo mammalian erythrocyte micronucleus(MN)test were performed to evaluate genotoxicity.Mice were administered IAAS(240,480,or 960 mg/kg bw)once orally to observe adverse central nervous system effects.Furthermore,beagle dogs were administered IAAS(10,30,60 mg/kg bw)once via the duodenum to evaluate its effects on the cardiovascular and respiratory systems.IAAS with or without S9-induced metabolic activation showed no genotoxicity in the Ames test up to 500μg/plate,in the mammalian chromosomal aberration test up to 710μg/mL,or in the MN test up to 800 mg/kg bw.No abnormal neurobehavioral effects were observed in mice following treatment with up to 960 mg/kg bw of IAAS.Moreover,blood pressure,heart rate,electrocardiogram parameters,and depth and rate of breathing in anesthetized beagle dogs did not differ among the IAAS doses or from the vehicle group.These data indicated that IAAS did not induce mutagenicity,clastogenicity,or genotoxicity,and no pharmaco-toxicological effects were observed in the respiratory,cardiovascular,or central nervous systems.Our results increased understanding of safety considerations associated with IAAS,and may indicate that IAAS is a possible drug candidate.展开更多
[Objective]This study aimed to analyze the low-polar components and antioxidant activities of Vernonia divergens.[Method]After extraction,the relative contents of various components were calculated with peak area norm...[Objective]This study aimed to analyze the low-polar components and antioxidant activities of Vernonia divergens.[Method]After extraction,the relative contents of various components were calculated with peak area normalization method.In addition,V.divergens were extracted with n-hexane,ethyl acetate and n-butanol,respectively;DPPH scavenging capacity and reducing capacity of these three extracts were analyzed and compared with that of vitamin C.[Result]A total of 29 compounds were identified that accounted for 88.30%of the total amount of low-polar chemical components.The results indicated that n-butanol extract exhibited higher DPPH scavenging capacity and reducing capacity than ethyl acetate extract and n-hexane extract.[Conclusion]This study provided a theoretical basis for the development and utilization of V.divergens.展开更多
基金The authors are grateful to Yunnan Major Science and Technology Project(2019ZF003,2019FY003004)the National Key Research and Development Program of China(2017YFC1704007)the general program of applied basic research of Yunnan province(2019FB116)for partial financial support.
文摘Indole alkaloids extract(IAAS)was prepared from leaves of Alstonia scholaris(L.)R.Br.,an evergreen tropical plant widely distributed throughout the world.This plant has been used historically by the Dai ethnic people of China to treat respiratory diseases.This study evaluated the genotoxicity and safety pharmacology of IAAS to support clinical use.The bacterial reverse mutation(Ames)test,in vitro mammalian chromosomal aberration test,and in vivo mammalian erythrocyte micronucleus(MN)test were performed to evaluate genotoxicity.Mice were administered IAAS(240,480,or 960 mg/kg bw)once orally to observe adverse central nervous system effects.Furthermore,beagle dogs were administered IAAS(10,30,60 mg/kg bw)once via the duodenum to evaluate its effects on the cardiovascular and respiratory systems.IAAS with or without S9-induced metabolic activation showed no genotoxicity in the Ames test up to 500μg/plate,in the mammalian chromosomal aberration test up to 710μg/mL,or in the MN test up to 800 mg/kg bw.No abnormal neurobehavioral effects were observed in mice following treatment with up to 960 mg/kg bw of IAAS.Moreover,blood pressure,heart rate,electrocardiogram parameters,and depth and rate of breathing in anesthetized beagle dogs did not differ among the IAAS doses or from the vehicle group.These data indicated that IAAS did not induce mutagenicity,clastogenicity,or genotoxicity,and no pharmaco-toxicological effects were observed in the respiratory,cardiovascular,or central nervous systems.Our results increased understanding of safety considerations associated with IAAS,and may indicate that IAAS is a possible drug candidate.
基金Supported by of Natural Science Foundation of Guangxi Zhuang Autonomous Region(2014GXNSFBA118050)Project of State Key Laboratory of Chemical and Molecular Engineering(CMEMR2014-B)
文摘[Objective]This study aimed to analyze the low-polar components and antioxidant activities of Vernonia divergens.[Method]After extraction,the relative contents of various components were calculated with peak area normalization method.In addition,V.divergens were extracted with n-hexane,ethyl acetate and n-butanol,respectively;DPPH scavenging capacity and reducing capacity of these three extracts were analyzed and compared with that of vitamin C.[Result]A total of 29 compounds were identified that accounted for 88.30%of the total amount of low-polar chemical components.The results indicated that n-butanol extract exhibited higher DPPH scavenging capacity and reducing capacity than ethyl acetate extract and n-hexane extract.[Conclusion]This study provided a theoretical basis for the development and utilization of V.divergens.