Anti-cancer effects of a novel compound HS-113 on cell growth, apoptosis, and angiogenesis in human hepatocellular carcinoma cells

Myung Joo Choi, Kyung Hee Jung, Donghee Kim, Hyunseung Lee, Hong Mei Zheng, Byung Hee Park, Sang Won Hong, Mi Hyun Kim, Sungwoo Hong, Soon Sun Hong

Research output: Contribution to journalArticlepeer-review

36 Scopus citations

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 languageEnglish
Pages (from-to)190-196
Number of pages7
JournalCancer Letters
Volume306
Issue number2
DOIs
StatePublished - 28 Jul 2011
Externally publishedYes

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

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