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

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

doi:10.4062/biomolther.2015.021

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

Biomolecules & therapeutics, v.23 no.4, 2015년, pp.367 - 373

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 Resear) , Cho, Jae Youl

Abstract ▼ AI-Helper

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.

주제어

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문제 정의

Also, these results led us to further investigate the mechanism underlying the compound’s anti-cancer effect.

제안 방법

, 2015). In our study, we synthesized a new artifi cial synthetic compound, 4-isopropyl-2-(1-phenylethyl) aniline [KTH-13-amine-monophenyl (KTH-13-AMP), (Fig 1)], a structural analog of KTH-13, and then examined its anti-cancer activity by analyzing its ability to inhibit proliferation, and checked the pro-apoptosis mechanism in various cancer cells.
These results imply that the structurally similar derivative from KTH-13 might also have anti-proliferative and pro-apoptotic effects. To test this hypothesis, we synthesized KTH-13-AMP and tested whether this derivative can lower the viability of several types of cancer cells including MDA-MB-231, HeLa, and C6 glioma cells.

대상 데이터

All data presented in this paper are the mean ± standard deviation (SD) of an experiment performed with six numbers of samples.

데이터처리

For statistical comparisons, the results were analyzed using ANOVA/Scheffe’s post hoc test and Kruskal- Wallis/Mann-Whitney tests.

후속연구

Our results show that KTH-13-AMP possesses anti-cancer activity and has the potential to be used for cancer treatment. In addition, this study implies the possibility of developing new cancer therapeutics designed from Cordyceps bassiana-derived anti-cancer compounds.

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