Pro-Apoptotic Activity of 4-Isopropyl-2-(1-Phenylethyl) Aniline Isolated from Cordyceps bassiana.
10.4062/biomolther.2015.021
- Author:
Mi Seon KIM
1
;
Yunmi LEE
;
Gi Ho SUNG
;
Ji Hye KIM
;
Jae Gwang PARK
;
Han Gyung KIM
;
Kwang Soo BAEK
;
Jae Han CHO
;
Jaegu HAN
;
Kang Hyo LEE
;
Sungyoul HONG
;
Jong Hoon KIM
;
Jae Youl CHO
Author Information
1. Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea. jaecho@skku.edu
- Publication Type:Original Article
- Keywords:
Cordyceps bassiana;
KTH-13-amine-monophenyl;
Anti-cancer activity;
Proliferation;
Apoptosis;
Cell survival
- MeSH:
Apoptosis;
Caspase 3;
Caspase 8;
Caspase 9;
Cell Survival;
Cordyceps*;
Dietary Supplements;
Glioma;
Phosphorylation
- From:Biomolecules & Therapeutics
2015;23(4):367-373
- CountryRepublic of Korea
- Language:English
-
Abstract:
Cordyceps species including Cordyceps bassiana are a notable anti-cancer dietary supplement. Previously, we identified several compounds with anti-cancer activity from the butanol fraction (Cb-BF) of Cordyceps bassiana. To expand the structural value of Cb-BF-derived anti-cancer drugs, we employed various chemical moieties to produce a novel Cb-BF-derived chemical derivative, KTH-13-amine-monophenyl [4-isopropyl-2-(1-phenylethyl) aniline (KTH-13-AMP)], which we tested for anti-cancer activity. KTH-13-AMP suppressed the proliferation of MDA-MB-231, HeLa, and C6 glioma cells. KTH-13-AMP also dose-dependently induced morphological changes in C6 glioma cells and time-dependently increased the level of early apoptotic cells stained with annexin V-FITC. Furthermore, the levels of the active full-length forms of caspase-3 and caspase-9 were increased. In contrast, the levels of total forms of caspases-3, caspase-8, caspase-9, and Bcl-2 were decreased in KTH-13-AMP treated-cells. We also confirmed that the phosphorylation of STAT3, Src, and PI3K/p85, which is linked to cell survival, was diminished by treatment with KTH-13-AMP. Therefore, these results strongly suggest that this compound can be used to guide the development of an anti-cancer drug or serve as a lead compound in forming another strong anti-proliferative agent.
