Anti-androgen-independent prostate cancer effects of ginsenoside metabolites in vitro: mechanism and possible structure-activity relationship investigation.
Treatment of androgen-independent prostate cancer (AIPC) remains unsatisfactory. In our present experiment, natural occurring ginsenosides (NOGs) and intestinal bacterial metabolites (IBMs) were employed to investigate their anti-AIPC cell growth activity using PC-3 cells. Our results showed that the IBMs exerted more portent anti-AIPC activity than NOGs, by decreasing survival rate, inhibiting proliferation, inducing apoptosis, and leading to cell cycle arrest in AIPC PC-3 cells. The increase of LogP and decrease of C-6 steric hindrance, which were caused by deglycosylation by intestinal bacteria, may be the reason for the higher anti-AIPC activity of IBMs.
Li
Wei
W
Graduate University of Chinese Academy of Sciences, Beijing, China. yling@dicp.ac.cn
Liu
Yong
Y
Zhang
Jiang-Wei
JW
Ai
Chun-Zhi
CZ
Xiang
Nan
N
Liu
Hui-Xin
HX
Yang
Ling
L
D000726:Androgen Antagonists / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001419:Bacteria / Q000378:metabolism; D001711:Biotransformation; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D019925:Cyclin A / Q000378:metabolism; D019938:Cyclin D1 / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D019008:Drug Resistance, Neoplasm; D036145:Ginsenosides / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D006031:Glycosylation; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007422:Intestines / Q000382:microbiology; D008297:Male; D008928:Mitochondria / Q000187:drug effects / Q000473:pathology; D015394:Molecular Structure; D011471:Prostatic Neoplasms / Q000378:metabolism / Q000473:pathology*; D013329:Structure-Activity Relationship
D000726:Androgen Antagonists; D000970:Antineoplastic Agents; C530104:CCND1 protein, human; D019925:Cyclin A; D036145:Ginsenosides; D019938:Cyclin D1