Anti-cancer activity of Homogentisic acid 2-O-I-D-glucoside (Phaseoloidin) and Exploration of its underlying Molecular mechanism

In this exploratory research MEEP was screened against various cancer cell lines (HeLa, MDA MB 231, DU 145, A 549, and HepG2) and phaseoloidin against HepG2 cell line. The MTT assay was employed to evaluate the cancer cells’ viability. Detection of intracellular ROS by using DCF-DA, measurement of mitochondrial super oxide generation (Mitosox™ Red), mitochondrial membrane potential using JC-1 staining and analyzed by flow cytometer, and molecular features were performed by western blotting. Phaseoloidin showed a promising best result against human hepatic carcinoma cells (HepG2 cells). HepG2 cells were exposed to various concentrations (1.23, 3.70, 11.11, 33.33, and 100 µM) of phaseoloidin, where it was found to trigger the apoptosis dose-dependently on HepG2 cells. This included characteristic changes in nuclear morphology, the breakdown of mitochondrial membrane potential (Δψm), up-regulation of pro-apoptotic BAX, and down-regulation of anti-apoptotic Bcl-2, which initiates the transformation of caspase-3 to cleaved caspase-3, thus actuating PARP promoting apoptosis.The data showed that Phaseoloidin induces cell death through up-regulation of cellular ROS production. This implies that Phaseoloidin could be a novel anticancer molecule from the natural source in treating hepatic cancer.