[Objectives]This paper aimed to prepare derivatives of protopanaxadiol from Panax notoginseng(Burk.)FH Chen with acid anhydrides and study their anti-tumor activity.[Methods]The 3-hydroxyl group of protopanaxadiol was...[Objectives]This paper aimed to prepare derivatives of protopanaxadiol from Panax notoginseng(Burk.)FH Chen with acid anhydrides and study their anti-tumor activity.[Methods]The 3-hydroxyl group of protopanaxadiol was subjected to structural modification and reacted with acid anhydrides to prepare derivatives,in order to improve the anti-tumor activity of protopanaxadiol.None of the five compounds designed and synthesized had been reported in the literature,and they were novel compounds.The anti-tumor activity of the derivatives was studies using MTS method.Taking cisplatin and paclitaxel as positive control drugs,the bioactivity of the compounds 1-5 on anti-tumor cell lines(HL-60 cells,SMMC-7721 cells,A-549 cells,MCF-7 cells and SW480 cells)in vitro was screened.[Results]The compound 5 showed inhibitory effect on HL-60 cells,SMMC-7721 cells and A-549 cells.[Conclusions]The acid anhydride esterification method is simple to operate and easy to control.This study has reference value for the structural modification and anti-tumor activity research of protopanaxadiol from P.notoginseng(Burk.)FH Chen.展开更多
This paper reviews recent progress in the structural modification and activities on Panax notoginseng saponins(PNS).PNS can not only improve the function of cardio-cerebral system,central nervous system and immune sys...This paper reviews recent progress in the structural modification and activities on Panax notoginseng saponins(PNS).PNS can not only improve the function of cardio-cerebral system,central nervous system and immune system,but also reveal anticancer,anti-aging and anti-oxidation activities.In order to solve the problem of low bioavailability and poor absorbability of PNS in vivo,usually,the researchers modified the structure of PNS with three methods:glycoside cleavage(including acid hydrolysis,sulfation,etc.),biotransformation method(including enzyme hydrolysis,microbial transformation)and combinatorial chemical method.It was found that the structural modification sites of PNS were single,mainly aimed at C-3,C-6 and C-20,which provided a new perspective for the structural modification of PNS.Therefore,structural modification on PNS with high yield and ready availability are significant in the discovery of new active ingredients and industrialization.Derivatives of PNS are applied to research of structure-activity relationship,which is beneficial to the development of new medicines.展开更多
基金Supported by Science&Technology Department of Yunnan Province-Kunming Medical University Joint Fund for Applied Basic Research[2017FE468(-001)]NSFC-Yunnan Joint Fund[U1502226].
文摘[Objectives]This paper aimed to prepare derivatives of protopanaxadiol from Panax notoginseng(Burk.)FH Chen with acid anhydrides and study their anti-tumor activity.[Methods]The 3-hydroxyl group of protopanaxadiol was subjected to structural modification and reacted with acid anhydrides to prepare derivatives,in order to improve the anti-tumor activity of protopanaxadiol.None of the five compounds designed and synthesized had been reported in the literature,and they were novel compounds.The anti-tumor activity of the derivatives was studies using MTS method.Taking cisplatin and paclitaxel as positive control drugs,the bioactivity of the compounds 1-5 on anti-tumor cell lines(HL-60 cells,SMMC-7721 cells,A-549 cells,MCF-7 cells and SW480 cells)in vitro was screened.[Results]The compound 5 showed inhibitory effect on HL-60 cells,SMMC-7721 cells and A-549 cells.[Conclusions]The acid anhydride esterification method is simple to operate and easy to control.This study has reference value for the structural modification and anti-tumor activity research of protopanaxadiol from P.notoginseng(Burk.)FH Chen.
基金Supported by High-level Talent Training Program for Graduate Students of Tibet University(2020-GSP-B014)National Natural Science Foundation of China(81560589)Yunnan Provincial Department of Science and Technology-Kunming Medical University Applied Basic Research Joint Special Fund(2017FE468-001)。
文摘This paper reviews recent progress in the structural modification and activities on Panax notoginseng saponins(PNS).PNS can not only improve the function of cardio-cerebral system,central nervous system and immune system,but also reveal anticancer,anti-aging and anti-oxidation activities.In order to solve the problem of low bioavailability and poor absorbability of PNS in vivo,usually,the researchers modified the structure of PNS with three methods:glycoside cleavage(including acid hydrolysis,sulfation,etc.),biotransformation method(including enzyme hydrolysis,microbial transformation)and combinatorial chemical method.It was found that the structural modification sites of PNS were single,mainly aimed at C-3,C-6 and C-20,which provided a new perspective for the structural modification of PNS.Therefore,structural modification on PNS with high yield and ready availability are significant in the discovery of new active ingredients and industrialization.Derivatives of PNS are applied to research of structure-activity relationship,which is beneficial to the development of new medicines.
