Dryocrassin ABBA Induces Apoptosis in Human Hepatocellular Carcinoma HepG2 Cells Through a Caspase-Dependent Mitochondrial Pathway

Background: Biological and pharmacological activities of dryocrassin ABBA, a phloroglucinol derivative extracted from Dryopteris crassirhizoma, have attracted attention. In this study, the apoptotic effect of dryocrassin ABBA on human hepatocellular carcinoma HepG2 cells was investigated.

Materials and methods: We tested the effects of dryocrassin ABBA on HepG2 in vitro by MTT, flow cytometry, Real-Time PCR, and Western blotting. KM male mice were used to detect the effect of dryocrassin ABBA on H22 cells in vivo.

Results: Dryocrassin ABBA inhibited the growth of HepG2 cells in a concentration-dependent manner. After treatment with 25, 50, and 75 μg/mL dryocrassin ABBA, the cell viability was 68%, 60% and 49%, respectively. Dryocrassin ABBA was able to induce Apoptosis, measured by propidium iodide (PI)/annexin V-FITC double staining. The results of Real-Time PCR and Western ting showed that dryocrassin ABBA up-regulated p53 and Bax expression and inhibited Bcl-2 expression which led to an activation of Caspase-3 and caspase-7 in the cytosol, and then induction of cell Apoptosis. In vivo experiments also showed that dryocrassin ABBA treatment significantly suppressed tumor growth, without major side effects.

Conclusions: Overall, these findings provide evidence that dryocrassin ABBA may induce Apoptosis in human hepatocellular carcinoma cells through a caspase-mediated mitochondrial pathway.