KG-135, enriched with selected ginsenosides, inhibits the proliferation of human prostate cancer cells in culture and inhibits xenograft growth in athymic mice.
Sun ginseng (SG) was recently developed as a heat-processed form of ginseng. The Rg3, Rk1, and Rg5 ginsenosides are its main ginsenoside components. SG has been reported to have more potent pharmacological activities than red ginseng (RG), where these pharmacological activities include vasodilatory, anti-oxidant and anti-tumorigenic effects. In the present study, we investigated KG-135, the ginsenoside-rich fraction of SG and demonstrated that this fraction inhibits proliferation of human prostate cancer cells both in vitro and in vivo. KG-135 caused a significant growth inhibition of DU145 and PC-3 human prostate cancer cells. KG-135 induced cell cycle arrest in the G1 phase and caused an associated increase in the p21(Cip1) protein levels. When KG-135 was fed to mice that had been xenografted with DU145 tumors, a time-dependent inhibition of tumor growth was noted without any observed toxicity. Immunohistochemical analysis of the tumor tissues showed that KG-135 led to a decrease in the expression of proliferating cell nuclear antigen (PCNA). Microarray analysis of the tumors revealed that KG-135 inhibited tumor growth and also caused changes in the expression levels of multiple cancer-related genes. These data suggest that KG-135 effectively inhibits prostate cancer cell proliferation. Its mechanism of action likely involves cyclin inhibition and regulation of the expression of the TNFRSF25 and ADRA2A genes.
Yoo
Ji-Hye
JH
Natural Products Research Center, Korea Institute of Science and Technology, Gangneung, Gangwon-do, 210-340, Republic of Korea.
Kwon
Hak Cheol
HC
Kim
Young-Joo
YJ
Park
Jeong Hill
JH
Yang
Hyun Ok
HO
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004591:Electrophoresis, Polyacrylamide Gel; D036145:Ginsenosides / Q000494:pharmacology*; D006801:Humans; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D046228:Microarray Analysis; D005894:Panax / Q000737:chemistry*; D010936:Plant Extracts / Q000494:pharmacology*; D016133:Polymerase Chain Reaction; D011471:Prostatic Neoplasms; D014183:Transplantation, Heterologous
D000970:Antineoplastic Agents; D036145:Ginsenosides; D010936:Plant Extracts