Abstract
Peiminine is a compound isolated from Bolbostemma paniculatum (Maxim) Franquet (Cucurbitaceae family), which has demonstrated antitumor activities. But its precise molecular mechanism underlying antitumor activity remain elusive. In this study, peiminine-induced apoptosis towards human hepatocellular carcinoma and its molecular mechanism were investigated. MTT assay was employed to assess anticancer effects of peiminine upon Hela, HepG2, SW480 and MCF-7 cell lines. Nuclear staining and flow cytometry were carried out to detect apoptosis induced by peiminine. Mitochondrial membrane potential evaluation and Western blot analysis were performed to investigate the mechanism of peiminine-induced apoptosis. The results showed peiminine reduced the viability of HepG2 cells in a time- and dose-dependent manner and had an IC50 of 4.58 μg/mL at 24h. Peiminine significantly increased the percentage of apoptotic cells and the mitochondrial membrane potential dose-dependently in HepG2 cells. The results of Western blotting indicated the expressions of Bcl-2, procaspase-3, procaspase-8, procaspase-9, and PARP decreased in HepG2 cells treated with peiminine, while the expressions of Bax, caspase-3, caspase-8, caspase-9, and cleaved PARP1 increased. The result suggests that peiminine can induce apoptosis in human hepatocellular carcinoma HepG2 cells through both extrinsic and intrinsic apoptotic pathways.
Highlights
Hepatocellular carcinoma (HCC) ranks third among malignancies related to death, and annually occurs in approximately 600,000 individuals worldwide[1]
The results indicated that peiminine displays the marked cytotoxicity to experimental cells
We found peiminine displays significant cytotoxicity toward experimental cancer cells and inhibited cellular proliferation in a time- and dose-dependent manner
Summary
Hepatocellular carcinoma (HCC) ranks third among malignancies related to death, and annually occurs in approximately 600,000 individuals worldwide[1]. Significant advances in frontline cancer research and chemotherapy have been made in treating HCC, many of the proposed drugs cause potent toxic adverse effects[2], thereby significantly hampering their usage in the clinic[3]. There is an unmet need to identify novel chemical compounds with less adverse effects to combat this devastating disease. Apoptosis is a type of cell death that is characterized by the preservation of plasma membrane integrity, which prevents local inflammatory reactions and tissue damage[4].
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