title: Pro-Apoptotic Activity of 4-Isopropyl-2-(1-Phenylethyl) Aniline Isolated from Cordyceps bassiana.
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.
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746.
authors.forename: Mi Seon
authors.initials: MS
authors.lastname: Kim
authors.affiliation: Department of Chemistry, Kwangwoon University, Seoul 139-701.
authors.forename: Yunmi
authors.initials: Y
authors.lastname: Lee
authors.affiliation: Institute for Bio-Medical Convergence, International St. Mary's Hospital and College of Medicine, Catholic Kwandong University, Incheon 404-834.
authors.forename: Gi-Ho
authors.initials: GH
authors.lastname: Sung
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746.
authors.forename: Ji Hye
authors.initials: JH
authors.lastname: Kim
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746.
authors.forename: Jae Gwang
authors.initials: JG
authors.lastname: Park
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746.
authors.forename: Han Gyung
authors.initials: HG
authors.lastname: Kim
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746.
authors.forename: Kwang Soo
authors.initials: KS
authors.lastname: Baek
authors.affiliation: Mushroom Research Division, Department of Herbal Crop Research, National Institute of Horticultural & Herbal Science, RDA, Eumseong 369-873.
authors.forename: Jae Han
authors.initials: JH
authors.lastname: Cho
authors.affiliation: Mushroom Research Division, Department of Herbal Crop Research, National Institute of Horticultural & Herbal Science, RDA, Eumseong 369-873.
authors.forename: Jaegu
authors.initials: J
authors.lastname: Han
authors.affiliation: Mushroom Research Division, Department of Herbal Crop Research, National Institute of Horticultural & Herbal Science, RDA, Eumseong 369-873.
authors.forename: Kang-Hyo
authors.initials: KH
authors.lastname: Lee
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746.
authors.forename: Sungyoul
authors.initials: S
authors.lastname: Hong
authors.affiliation: Department of Veterinary Physiology, College of Veterinary Medicine, Biosafety Research Institute, Chonbuk National University, Jeonju 561-756, Republic of Korea.
authors.forename: Jong-Hoon
authors.initials: JH
authors.lastname: Kim
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746.
authors.forename: Jae Youl
authors.initials: JY
authors.lastname: Cho
keywords: Anti-cancer activity; Apoptosis; Cell survival; Cordyceps bassiana; KTH-13-amine-monophenyl; Proliferation