Bioactivity of a polyhydroxy gorgostane steroid from Xenia umbellata

Abstract

Abstract A C-30 steroid, 3β-,5α-,6β-,11α-,20β-pentahydroxygorgosterol was isolated from the soft coral Xenia umbellata Lamarck (Xeniidae). The chemical structure was elucidated by examining the NMR spectral data and comparison with the previously published data. Compound 1 inhibited the growth of ovarian cancer (SKOV-3), breast cancers (MCF-7 and MDA-MB-231) and hepatocellular carcinoma (HepG2) using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide assay. Notably against HepG2, compound 1 showed significant effect with an IC50 value of 19.70 ± 1.98 µg/mL. It significantly increased the population in the SubG1 phase for 2.01- and 2.05-folds, respectively, compared to untreated cells. Additionally, it showed potent inhibitory activities of superoxide dismutase (384.6 vs 8594.2 U/g protein in dimethyl sulfoxide-treated cells), catalase (0.3 vs 0.07 U/g protein), decreased the level of reduced glutathione (1.7 vs 0.6 mg/g protein) and the activity of matrix metalloproteases (MMP-2 and MMP-9 [0.5-fold of change in MMP activity]) in HepG2 cells. The results indicated the potent antiproliferative activity of the gorgostane derivative (1) against HepG2 cells. This study provides a scientific basis of the antiproliferative effects of steroidal compound with gorgostane nucleus against hepatocellular carcinoma cells.