Pro-Apoptotic Activity of 4-Isopropyl-2-(1-Phenylethyl) Aniline Isolated from Cordyceps bassiana

• Published in: Biomolecules & therapeutics Vol. 23; no. 4; pp. 367 - 373
• Main Authors: Kim, Mi Seon, Lee, Yunmi, Sung, Gi-Ho, Kim, Ji Hye, Park, Jae Gwang, Kim, Han Gyung, Baek, Kwang Soo, Cho, Jae Han, Han, Jaegu, Lee, Kang-Hyo, Hong, Sungyoul, Kim, Jong-Hoon, Cho, Jae Youl
• Format: Journal Article
• Language: Korean
• Published: 한국응용약물학회 30.07.2015
• Subjects: Anti-cancer activity; Apoptosis; Cell survival; Cordyceps bassiana; KTH-13-amine-monophenyl; Proliferation; Cordyceps bassiana; KTH-13-amine-monophenyl; Cell survival; Proliferation; Anti-cancer activity; Apoptosis
• ISSN: 1976-9148; 2005-4483

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.