The Korean Journal of Physiology and Pharmacology

The Korean Society of Pharmacology (대한약리학회)
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4-(Tert-butyl)-2,6-bis(1-phenylethyl)phenol induces pro-apoptotic activity

  • Kim, Jun Ho (Depatment of Genetic Engineering, Sungkyunkwan University) ;
  • Lee, Yunmi (Department of Chemistry, Kwangwoon University) ;
  • Kim, Mi-Yeon (School of Systems Biomedical Science, Soongsil University) ;
  • Cho, Jae Youl (Depatment of Genetic Engineering, Sungkyunkwan University)
  • Received : 2015.10.10
  • Accepted : 2016.03.29
  • Published : 2016.05.01
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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.

Keywords

References

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