The in Vitro Structure-Related Anti-Cancer Activity of Ginsenosides and Their Derivatives

被引：84

作者：

Dong, Hang ^{[1
]}

Bai, Li-Ping ^{[1
,2
]}

Wong, Vincent Kam Wai ^{[1
,2
]}

Zhou, Hua ^{[1
,2
]}

Wang, Jing-Rong ^{[1
,2
]}

Liu, Yan ^{[1
]}

Jiang, Zhi-Hong ^{[1
,2
]}

Liu, Liang ^{[1
,2
]}

机构：

[1] Hong Kong Baptist Univ, Sch Chinese Med, Shum Yiu Foon Shum Bik Chuen Mem Ctr Canc & Infla, Kowloon Tong, Hong Kong, Peoples R China

[2] Macau Univ Sci & Technol, State Key Lab Qual Res Chinese Med, Taipa, Macau, Peoples R China

来源：

MOLECULES | 2011年 / 16卷 / 12期

关键词：

ginsenosides; anti-cancer; cytotoxicity; protopanaxadiol; structure-related activity; GINSENG SAPONINS; DEGRADATION; HYDROLYSIS; VIVO;

D O I：

10.3390/molecules161210619

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Panax ginseng has long been used in Asia as a herbal medicine for the prevention and treatment of various diseases, including cancer. The current study evaluated the cytotoxic potency against a variety of cancer cells by using ginseng ethanol extracts (RSE), protopanaxadiol (PPD)-type, protopanaxatriol (PPT)-type ginsenosides fractions, and their hydrolysates, which were prepared by stepwise hydrolysis of the sugar moieties of the ginsenosides. The results showed that the cytotoxic potency of the hydrolysates of RSE and total PPD-type or PPT-type ginsenoside fractions was much stronger than the original RSE and ginsenosides; especially the hydrolysate of PPD-type ginsenoside fractions. Subsequently, two derivatives of protopanaxadiol (1), compounds 2 and 3, were synthesized via hydrogenation and dehydration reactions of compound 1. Using those two derivatives and the original ginsenosides, a comparative study on various cancer cell lines was conducted; the results demonstrated that the cytotoxic potency was generally in the descending order of compound 3 > 20(S)-dihydroprotopanaxadiol (2) > PPD (1) > 20(S)-Rh2 > 20(R)-Rh2 approximate to 20(R)-Rg3 approximate to 20(S)-Rg3. The results clearly indicate the structure-related activities in which the compound with less polar chemical structures possesses higher cytotoxic activity towards cancer cells.

引用

页码：10619 / 10630

页数：12

共 17 条

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