Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Pro-Apoptotic Activity of 4-Isopropyl-2-(1-Phenylethyl) Aniline Isolated from Cordyceps bassiana

  • Kim, Mi Seon (Department of Genetic Engineering, Sungkyunkwan University) ;
  • Lee, Yunmi (Department of Chemistry, Kwangwoon University) ;
  • Sung, Gi-Ho (Institute for Bio-Medical Convergence, International St. Mary's Hospital and College of Medicine, Catholic Kwandong University) ;
  • Kim, Ji Hye (Department of Genetic Engineering, Sungkyunkwan University) ;
  • Park, Jae Gwang (Department of Genetic Engineering, Sungkyunkwan University) ;
  • Kim, Han Gyung (Department of Genetic Engineering, Sungkyunkwan University) ;
  • Baek, Kwang Soo (Department of Genetic Engineering, Sungkyunkwan University) ;
  • Cho, Jae Han (Mushroom Research Division, Department of Herbal Crop Research, National Institute of Horticultural & Herbal Science, RDA) ;
  • Han, Jaegu (Mushroom Research Division, Department of Herbal Crop Research, National Institute of Horticultural & Herbal Science, RDA) ;
  • Lee, Kang-Hyo (Mushroom Research Division, Department of Herbal Crop Research, National Institute of Horticultural & Herbal Science, RDA) ;
  • Hong, Sungyoul (Department of Genetic Engineering, Sungkyunkwan University) ;
  • Kim, Jong-Hoon (Department of Veterinary Physiology, College of Veterinary Medicine, Biosafety Research Institute, Chonbuk National University) ;
  • Cho, Jae Youl (Department of Genetic Engineering, Sungkyunkwan University)
  • Received : 2015.02.23
  • Accepted : 2015.05.19
  • Published : 2015.07.01
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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.

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References

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