Effect of Amino Acids on the Generation of Ginsenoside Rg3 Epimers by Heat Processing and the Anticancer Activities of Epimers in A2780 Human Ovarian Cancer Cells.

Jun Yeon Park,Jungyeob Ham,Dahae Lee,Pilju Choi,Buyng-Su Hwang,Eun Bee Jung,Ki Sung Kang,Taejung Kim

doi:10.1155/2016/3146402

Abstract

Ginsenosides are the active components of Panax ginseng. Many research studies indicate that these deglycosylated, less-polar ginsenosides have better bioactivity than the major ginsenosides. In the present study, we sought to verify the enhanced anticancer effect of P. ginseng extract after undergoing the Maillard reaction as well as elucidate the underlying mechanism of action. The effects of 9 amino acids were tested; among them, the content of 20(S)-Rg3 in the ginseng extract increased to more than 30, 20, and 20% when processed with valine, arginine, and alanine, respectively, compared with that after normal heat processing. The ginseng extract that was heat-processed with arginine exhibited the most potent inhibitory effect on A2780 ovarian cancer cell proliferation. Therefore, the generation of 20(S)-Rg3 was suggested to be involved in this effect. Moreover, the inhibitory effect of 20(S)-Rg3 on A2780 cell proliferation was significantly stronger than that of 20(R)-Rg3. Protein expression levels of cleaved caspase-3, caspase-8, caspase-9, and PARP in the A2780 ovarian cancer cells markedly increased, whereas the expression of BID decreased after 20(S)-Rg3 treatment. Therefore, we confirmed that the anticancer effects of the products of ginseng that was heat-processed with arginine are mediated mainly via the generation of the less-polar ginsenoside 20(S)-Rg3.

Highlights

The use of naturally occurring compounds for the design of novel anticancer drugs has increased in recent years, especially owing to increasing demand for natural remedies among cancer patients [1,2,3,4]
Experimental as well as clinical studies have shown that ginseng and its components are beneficial for chemotherapy since they inhibit proliferation and induce apoptosis in various malignancies, including ovarian cancer [5,6,7,8]
We have extensively studied and developed novel heat processing methods that facilitate the deglycosylation of major ginsenosides Rb1, Rb2, Rc, Rd, and Re [4, 10]

Summary

Introduction

The use of naturally occurring compounds for the design of novel anticancer drugs has increased in recent years, especially owing to increasing demand for natural remedies among cancer patients [1,2,3,4]. The saponins that are present in high concentrations in ginseng are the major ginsenosides Rb1, Rb2, Rc, Rd, and Re (Figure 1) [9, 10]. The development of ginseng extract containing an increased concentration of deglycosylated ginsenosides has been investigated.

Results

Conclusion