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Molecules 2011, 16(12), 10619-10630; doi:10.3390/molecules161210619

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

1,†, 1,2,†, 1,2, 1,2, 1,2, 1, 1,2,*  and 1,2,*
1 Shum Yiu Foon Shum Bik Chuen Memorial Centre for Cancer and Inflammation Research, School of Chinese Medicine, Hong Kong Baptist University, 7 Baptist University Road, Kowloon Tong, Hong Kong, China 2 State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Avenida Wai Long, Taipa, Macau, China These authors contributed equally to this work.
* Authors to whom correspondence should be addressed.
Received: 25 October 2011 / Revised: 9 December 2011 / Accepted: 16 December 2011 / Published: 19 December 2011
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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 ≈ 20(R)-Rg3 ≈ 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.
Keywords: ginsenosides; anti-cancer; cytotoxicity; protopanaxadiol; structure-related activity ginsenosides; anti-cancer; cytotoxicity; protopanaxadiol; structure-related activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Dong, H.; Bai, L.-P.; Wong, V.K.W.; Zhou, H.; Wang, J.-R.; Liu, Y.; Jiang, Z.-H.; Liu, L. The in Vitro Structure-Related Anti-Cancer Activity of Ginsenosides and Their Derivatives. Molecules 2011, 16, 10619-10630.

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