Clinical Medicine Institute & Department of Surgery, University of Ulsan College of Medicine , Gangneung 210-711, Korea.
J Agric Food Chem. 2014 Apr 2;62(13):2830-6. doi: 10.1021/jf5000776. Epub 2014 Mar 25.
Ginsenoside Re is a triol type triterpene glycoside and is abundantly present in ginseng berry. In the present study, we verified that ginsenoside Re can be transformed into less-polar ginsenosides, namely, Rg2, Rg6, and F4, by heat-processing. The products of heat-processed ginsenoside Re inhibited phosphorylation of CDK2 at Thr160 by upregulation of p21 level, resulting in S phase arrest. The products of heat-processed ginsenoside Re also activated caspase-8, caspase-9, and caspase-3, followed by cleavage of PARP, a substrate of caspase-3, in a dose-dependent manner. Concurrently, alteration of mitochondrial factors such as Bcl-2 and Bax was also observed. Moreover, pretreatment with Z-VAD-fmk abrogated caspase-8, -9, and -3 activations by the products of heat-processed ginsenoside Re. We further confirmed that the anticancer effects of the products of heat-processed ginsenoside Re in AGS cells are mainly mediated via generation of less-polar ginsenosides Rg6 and F4.
人参皂苷 Re 是一种三醇型三萜皂苷，在人参果中含量丰富。在本研究中，我们验证了人参皂苷 Re 经热加工可转化为极性较小的人参皂苷，即 Rg2、Rg6 和 F4。热加工后的产物通过上调 p21 水平抑制 CDK2 在 Thr160 的磷酸化，导致 S 期停滞。热加工后的产物还可剂量依赖性地激活 caspase-8、caspase-9 和 caspase-3，随后裂解 caspase-3 的底物 PARP。同时，还观察到线粒体因子如 Bcl-2 和 Bax 的改变。此外，用 Z-VAD-fmk 预处理可消除热加工后的产物对 caspase-8、-9 和 -3 的激活。我们进一步证实，热加工后的产物在 AGS 细胞中的抗癌作用主要是通过生成极性较小的人参皂苷 Rg6 和 F4 来介导的。
