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Current Chemical Biology

Editor-in-Chief

ISSN (Print): 2212-7968
ISSN (Online): 1872-3136

Polyphyllin D - A Potential Anti-Cancer Agent to Kill Hepatocarcinoma Cells with Multi-Drug Resistance

Author(s): Tim T. Kwok, Siu K. Kong, Ming Li, Ho P. Ho, Bao Yu, Kwok P. Fung, Yick K. Suen, Judy Y.W. Chan, Macey M.S. Lee, Yan C. Li, Rebecca K.Y. Lee, Rose C.Y. Ong and Jenny Y.N. Cheung

Volume 3, Issue 1, 2009

Page: [89 - 99] Pages: 11

DOI: 10.2174/2212796810903010089

Price: $65

Abstract

To develop drugs to kill cancer cells, we chemically synthesized a number of anti-cancer agents by adding different side chains to the core backbone of saponin. With the use of bioassay-guided methods, we found one agent that possessed a high cytotoxicity to a number of cancer cell lines. Interestingly, this compound was later found to be an active component of a tradition Chinese herb Paris polyphylla known as Polyphyllin D (PD) (diosgenyl α-L-rhamnopyranosyl- (1→2)-(β-L-ara-binofuranosyl-(1→4)-β-D-glucopyranoside). In China, the rhizome of Paris polyphylla (Chong Lou) has been used as a traditional Chinese medicine to treat a number of cancers including pancreas and liver cancers for a long time. Results from our laboratory demonstrate that PD is a potent anti-cancer agent that bypasses multi-drug resistance (MDR) and induces programmed cell death in R-HepG2 cells over-expressing P-glycoprotein (P-gp). In this paper, we reviewed the mechanisms how PD overcomes the MDR and exhibits a stronger cytotoxicity in the R-HepG2 than its parent line without P-gp through mitochondrial injury.

Keywords: Polyphyllin D, apoptosis, multi-drug resistance, mitochondria, R-HepG2

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