Preparation and evaluation of oridonin derivatives
- VernacularTitle:冬凌草甲素衍生物的制备和评价
- Author:
Xu WU
;
Feng ZHAO
;
Ke LIU
- Publication Type:Journal Article
- Keywords:
oridonin;
14-p-tolylsulfonyl-oridonin;
14-acetyl-1-oxo-oridonin;
14-p-tolylsulfonyl-1-oxo-oridonin;
structural modification;
cytotoxicity
- From:
Chinese Traditional and Herbal Drugs
1994;0(03):-
- CountryChina
- Language:Chinese
-
Abstract:
Objective In order to study the structure-activity relationship of oridonin,Some derivatives of oridonin were synthesized and their cytotoxicity activity was evaluated.Methods Oridonin (Ⅰ) was isolated and purified by silica gel column chromatography.The derivatives were synthesized from oridonin through oxidation and acylation.All compounds were confirmed by spectrum analyses and their cytotoxicity was evaluated by MTT method.Results Six compounds were obtained and identified as: 14-acetyl-oridonin(Ⅱ),1,14-diacetyl-oridonin(Ⅲ),14-p-tolylsulfonyl-oridonin(Ⅳ),1-oxo-oridonin(Ⅴ),14-acetyl-1-oxo-oridonin(Ⅵ),14-p-tolylsulfonyl-1-oxo-oridonin(Ⅶ).Among them compounds Ⅳ,Ⅵ,and Ⅶ were new compounds.Five compounds showed better cytotoxicity than oridonin.Conclusion The cytotoxicity of 1oxo oridonin derivatives is first evaluated and shows the stronger cytotoxicity than oridonin.
