摘要
[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.
[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 Science&Technology Department of Yunnan Province-Kunming Medical University Joint Fund for Applied Basic Research[2017FE468(-001)]
NSFC-Yunnan Joint Fund[U1502226].
