4-(Tert-butyl)-2,6-bis(1-phenylethyl)phenol induces pro-apoptotic activity.
10.4196/kjpp.2016.20.3.253
- Author:
Jun Ho KIM
1
;
Yunmi LEE
;
Mi Yeon KIM
;
Jae Youl CHO
Author Information
1. Depatment of Genetic Engineering, Sungkyunkwan University, Suwon 16419, Korea. jaecho@skku.edu
- Publication Type:Original Article
- Keywords:
Anti-cancer activity;
KTH-13-t-Bu;
Pro-apoptotic activity;
Src;
STAT-3
- MeSH:
Caspase 3;
Cordyceps;
Glioma
- From:The Korean Journal of Physiology and Pharmacology
2016;20(3):253-259
- CountryRepublic of Korea
- Language:English
-
Abstract:
Previously, we found that KTH-13 isolated from the butanol fraction of Cordyceps bassiana (Cb-BF) displayed anti-cancer activity. To improve its antiproliferative 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.
