4-(Tert-butyl)-2,6-bis(1-phenylethyl)phenol induces pro-apoptotic activity
- Authors
- Kim, Jun Ho; Lee, Yunmi; Kim, Mi-Yeon; Cho, Jae Youl
- Issue Date
- May-2016
- Publisher
- KOREAN JOURNAL OF PHYSIOLOGY & PHARMACOLOGY
- Keywords
- Anti-cancer activity; KTH-13-t-Bu; Pro-apoptotic activity; Src; STAT-3
- Citation
- KOREAN JOURNAL OF PHYSIOLOGY & PHARMACOLOGY, v.20, no.3, pp.253 - 259
- Journal Title
- KOREAN JOURNAL OF PHYSIOLOGY & PHARMACOLOGY
- Volume
- 20
- Number
- 3
- Start Page
- 253
- End Page
- 259
- URI
- http://scholarworks.bwise.kr/ssu/handle/2018.sw.ssu/7613
- DOI
- 10.4196/kjpp.2016.20.3.253
- ISSN
- 1226-4512
- Abstract
- 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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