Alpinoid C analog inhibits angiogenesis and induces apoptosis in COLO205 cell line

Publication date: Available online 6 May 2019Source: Chemico-Biological InteractionsAuthor(s): Loka Reddy Velatooru, V. Sridhar, Vasudevarao Penugurti, S. Purushotham ReddyAbstractDiarylheptanoids display an array of biological and pharmacological properties. We previously reported the synthesis of a diarylheptanoid Alpinoid c and a series of its derivatives, evaluated their cytotoxicity against various human cancer cells. We found some of these derivatives were significantly more potent than Alpinoid c in preventing the proliferation of various cancer cell lines. Among these, (S, E)-1-(3, 4 dimethoxy phenyl)-6-hydroxy-7-phenylhept-4-en-3-one (DPHP) showed most potent cytotoxicity against COLO205 cells, however, the mechanism by which DPHP prevents the growth of these colon cancer cells remains unknown. In the current study, we investigated the molecular mechanism of DPHP on colon cancer cells. DPHP inhibited the proliferation of COLO205 (IC50 7.01 ± 0.62 μM) and A549 (IC50 20.03 ± 3.11 μM) cells more specifically than normal Human colon epithelial cell line NCM460 (IC50 55.6 ± 4.02 μM). In COLO205 cells, DPHP induced cell shrinkage, membrane blebbing, chromatin condensation, phosphatidylserine externalization, and an accumulation of cells at sub-G1 phase. Further analysis these cells treated with DPHO revealed a decrease in mitochondrial membrane potential, an increase in Bax/Bcl2 ratio, the release of cytochrome c, activation of caspases −9, âˆ...
Source: Chemico Biological Interactions - Category: Biochemistry Source Type: research