LIU Dingrui, WANG Xiaoyan
Using silica gel column chromatography, a compound named F1-3 was isolated from Pholiota adiposa fruiting bodies, and then determined to be ergosta-4,6,8(14),22-tetraen-3-one (ETO) by MS and NMR. ETO was then studied for its inhibitory effects on HepG2, MCF-7, HeLa, and A549 cancer cells by Cell Counting Kit-8 (CCK8), and antitumor effect on H22 tumor-bearing mice in vivo. ICR mice were randomly divided into five groups as follows: model group, positive group (cyclophosphamide, 0.1× 10-3 mmol·kg-1), low dose ETO group (LD, 0.025 mmol·kg-1), medium dose ETO group (MD, 0.05 mmol·kg-1) and high dose ETO group (0.1 mmol·kg-1). Gavage with saline was the blank control. Mice in different groups were measured for tumor suppression rate and organ indices after 15 consecutive days of treatment. The contents of IFN-γ, IL-2, IL-6, TNF-α and VEGF in mouse serum were determined by ELISA. Tumor cell arrangement, cell integrity, number of nuclei were observed by hematoxylin-eosin (HE) staining, and the degree of apoptosis in tumor tissues was determined by TUNEL assay. The expression levels of VEGF, Bcl-2 and BAX were determined by immunohistochemistry. The results showed that ETO inhibited the proliferation of HepG2, MCF-7 and HeLa cells in vitro, i.e. the inhibition rate of 100 μg·mL-1 ETO on HepG-2 cells reached 91.04%. ETO inhibited tumor growth in H22 mice, and the tumor inhibition rate of HD group reached 72.06%, with thymus index and spleen index significantly improved. In the model group, the tumor cells were arranged neatly and tightly, the growth status was good, and the apoptosis rate was low. In contrast, the tumor cells of the ETO treated groups showed different degrees of deformation, rupture, blurring, and massive apoptosis. Compared with the model group, ETO increased the contents of IFN-γ, IL-2 and IL-6 in mouse serum, decreased VEGF level, and showed a good antitumor effect through decreasing the expression levels of VEGF, Bcl-2, and increasing the expression level of BAX.