Anticancer effects of KI-10F: A novel compound affecting apoptosis, angiogenesis and cell growth in colon cancer

Title
Anticancer effects of KI-10F: A novel compound affecting apoptosis, angiogenesis and cell growth in colon cancer
Authors
홍상원정경희최명주김다영이희승홍메이젱광영리이브리엄박병선이소하홍순선
Keywords
colon cancer; anticancer effect; pyrazole; angiogenesis; cell cycle; apoptosis
Issue Date
2012-11
Publisher
International journal of oncology
Citation
VOL 41, NO 5, 1715-1722
Abstract
The anticancer effect of a new pyrazole derivative, KI-10F (2-(4-(2-(4-(dimethylamino) phenyl)pyridin-4-yl)-5-(3-methoxy-5-methylphenyl)-1H-pyrazol‑1-yl) acetonitrile)•3.5HCl) was evaluated in human colon cancer cells. KI-10F strongly suppressed the growth of human colon cancer cells and induced apoptosis by increasing the proportion of sub-G1 presenting apoptotic cells as well as causing cell cycle arrest at the G2/M phase. Apoptosis by KI-10F was confirmed by observation of an increase in the expression of cleaved caspase-3, caspase-8, caspase-9 and Bax, and the decrease of Bcl-2. Decreased expression of HIF-1α and VEGF, and the inhibition of HUVEC tube formation and migration showed that KI-10F effectively inhibited the angiogenesis process. Furthermore, in vivo study in a mouse xenograft model showed that KI-10F produced a stronger antitumor activity than 5-FU, a conventional anticancer drug prescribed for the treatment of colon cancer. The effects of KI-10F on tumor proliferation (PCNA), angiogenesis (CD34) and apoptosis (cleaved caspase-3) were evaluated by immunohistochemistry using isolated tumor tissue samples. Taken together, our results demonstrated that KI-10F induces apoptosis and inhibits cell growth and angiogenesis both in vitro and in vivo. We suggest that KI-10F is an effective chemotherapeutic candidate for use against colon cancer.
URI
http://pubs.kist.re.kr/handle/201004/43815
ISSN
10196439
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KIST Publication > Article
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