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KMID : 0811720160200030253
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Korean Journal of Physiology & Pharmacology
2016 Volume.20 No. 3 p.253 ~ p.259
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4-(Tert-butyl)-2,6-bis(1-phenylethyl)phenol induces pro-apoptotic activity
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Kim Jun-Ho
Lee Yun-mi
Kim Mi-Yeon
Cho Jae-Youl
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Abstract
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Previously, we found that KTH-13 isolated from the butanol fraction of Cordyceps bassiana (Cb-BF) displayed anti-cancer activity. To improve its anti-proliferative activity and production yield, we employed a total synthetic approach and derivatized KTH-13 to obtain chemical analogs. In this study, one KTH-13 derivative, 4-(tert-butyl)-2,6-bis(1-phenylethyl)phenol (KTH-13-t-Bu), was selected to test its anti-cancer activity. KTH-13-t-Bu diminished the proliferation of C6 glioma, MDA-MB-231, LoVo, and HCT-15 cells. KTH-13-t-Bu induced morphological changes in C6 glioma cells in a dose-dependent manner. KTH-13-t-Bu also increased the level of early apoptotic cells stained with annexin V-FITC. Furthermore, KTH-13-t-Bu increased the levels of cleaved caspase-3 and -9. In contrast, KTH-13-t-Bu upregulated the levels of pro- and cleaved forms of caspase-3, -8, and -9 and Bcl-2. Phospho-STAT3, phospho-Src, and phospho-AKT levels were also diminished by KTH13-t-Bu treatment. Therefore, these results strongly suggest that KTH-13-t-Bu can be considered a novel anti-cancer drug displaying pro-apoptotic activity.
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KEYWORD
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Anti-cancer activity, KTH-13-t-Bu, Pro-apoptotic activity, Src, STAT-3
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