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KMID : 0606920150230040367
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Biomolecules & Therapeutics
2015 Volume.23 No. 4 p.367 ~ p.373
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Pro-Apoptotic Activity of 4-Isopropyl-2-(1-Phenylethyl) Aniline Isolated from Cordyceps bassiana
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Kim Mi-Seon
Lee Yun-mi
Sung Gi-Ho
Kim Ji-Hye
Park Jae-Gwang
Kim Han-Gyung
Baek Kwang-Soo
Cho Jae-Han
Han Jae-Gu
Lee Kang-Hyo
Hong Sung-Youl
Kim Jong-Hoon
Cho Jae-Youl
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Abstract
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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.
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KEYWORD
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Cordyceps bassiana, KTH-13-amine-monophenyl, Anti-cancer activity, Proliferation, Apoptosis, Cell survival
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