The phenolic profiles, antioxidant activity, antiproliferative property and the underlying molecular mechanisms of cell apoptosis of Rhodiola rosea free phenolic (RFE) were analyzed in this work. Overall, Rhodiola rosea rhizome phenolic extract (RE) contained Rhodiola rosea rhizome free phenolic extract (RFE) and Rhodiola rosea rhizome bound phenolic extract (RBE). Compared with RBE, RFE contained higher phenolic contents and possessed stronger antioxidant activity. High-performance liquid chromatography (HPLC) results demonstrated that the main phenolics of were epigallocatechin (EGC), epigallocatechin gallate (EGCG), gallic acid (GA) and catechin. Gas chromatography-mass spectrometry (GC-MS) analysis found that Rhodiola rosea L. was rich in volatile phytochemicals. In addition, many types of vitamin E and a few kinds of carotenoids were found in Rhodiola rosea. In addition, the main compounds in RFE (GA, EGC, EGCG) and RFE all exhibited excellent antiproliferative activity, indicating the antiproliferative activity of RFE was partly attributed to the synergy effects of the main compounds. Further study confirmed that RFE could block 16.99% of HepG2 cells at S phase and induce 20.32% programmed cell death compared with the control group. Specifically, RFE dose-dependently induced cell apoptosis and cell cycle arrest via modulating the p53 signaling pathway including up-regulation of the expression of p53 and Bax while down-regulation of the Bcl-2, cyclin D1 and CDK4 levels. Therefore, RFE exhibited the potential of being developed as an auxiliary antioxidant and a therapeutic agent for cancer.
Keywords: Rhodiola rosea; antiproliferative activity; cell apoptosis; cell cycle; p53 signaling pathway; phytochemical profiles.