Abstract
Hepatocellular carcinoma (HCC) is one of the most common malignancies, yet there have been no significant advances in effective therapeutics. In this study, HS-113 was synthesized as a novel compound, N-(5-(2-bromobenzyl) thiazole-2-yl) benzofuran-2-carboxamide and its cytotoxic activity and anti-cancer effect were examined in human HCC cells. HS-113 strongly suppressed growth of HCC cells in a dose-dependent manner, induced apoptosis by increasing the proportion of sub-G1 apoptotic cells, and caused cell cycle arrest at G0/G1 phase. Also, HS-113 increased the expression of p27 and decreased that of cyclin D1 associated with cell cycle arrest. Apoptosis by HS-113 was confirmed by DAPI and TUNEL staining, and the increases of the cleaved PARP and caspase-3 were observed. Furthermore, HS-113 decreased protein expression of HIF-1α and secretion of VEGF, and inhibited the tube formation of HUVECs. These results showed that HS-113 not only inhibited cell growth and angiogenesis, but also induced apoptosis of human HCC cells. We suggest that HS-113 may be a potential candidate for caner therapy against HCC.
Original language | English |
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Pages (from-to) | 190-196 |
Number of pages | 7 |
Journal | Cancer Letters |
Volume | 306 |
Issue number | 2 |
DOIs | |
State | Published - 28 Jul 2011 |
Externally published | Yes |
Bibliographical note
Funding Information:This work was supported by the Korean Health Technology R&D Project (A101185) and the National R&D Program for Cancer Control (1020250), Ministry of Health & Welfare, and National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (NRF 2010-0011895, 0015340, and 0022179).
Keywords
- Angiogenesis
- Apoptosis
- HCC
- HS-113