The Ginsenosides of Black Ginseng Against Prostatic Cancer by Spectrum-Effect and Structure-Effect Relationships

Meiyang Sun, Linlin Liu, Xueying Liu and Deqiang Dou

Background and Objective: Black Ginseng (BG) is a new type of processed ginseng and presently, there is almost no anti-cancer comparison among the ginsenosides of BG together. To elucidate the anti-cancer substance of BG and lay a foundation for the development of new drugs. Materials and Methods: Firstly, the anti-cancer activities of BG decoction and its separated fractions were compared on prostate cancer cells (DU145) with the serum pharmacology method. And then, the constituents of BG and its separated fractions as well as their serum after BG and its separated fractions administered intragastrically were identified by Ultra-High-Performance Liquid Chromatography-Quadrupole Time-Of-Flight Tandem Mass spectrometry (UPLCQ-TOF-MS/MS). Then, the spectrum-effect relationship was carried out by the analysis of the spectra of 10 batches of BG with High-Performance Liquid Chromatography (HPLC) and Methyl Thiazolyl Tetrazolium (MTT) assay to evaluate the inhibitory rate of BG against DU145. Finally, an anticancer structure-effect relationship of ginsenosides was performed to revalidate the conclusion. Results: The results showed that the fractions of Total Saponins (TSF) and 95% Alcohol Eluate (AEF) were the effective fractions for anti-prostate cancer action. There were eight chromatographic peaks (ginsenosides S-Rg2, S-Rg3, R-Rg3, RK1, Rg5, peak number of 17 and 18) which contributed greatly to anti-prostate cancer of black ginseng. The IC50 of ginsenosides Rg5, S-Rh2, R-Rh2, S-Rh1, R-Rh1, RK1, RK3, R-Rg3, PPT and Compound K were less than 50 μmol L^–1, which have better anti-prostate cancer activity compared with other ginsenosides. Conclusion: The effective components of BG against prostate cancer were its secondary ginsenosides.

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