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Anti-Proliferative and Pro-Apoptotic Activities of 4-Methyl-2,6-bis(1-phenylethyl)phenol in Cancer Cells

Title
Anti-Proliferative and Pro-Apoptotic Activities of 4-Methyl-2,6-bis(1-phenylethyl)phenol in Cancer Cells
Authors
Sung, Nak YoonKim, Seung CheolKim, Yun HwanKim, GihyeonLee, YunmiSung, Gi-HoKim, Ji HyeYang, Woo SeokKim, Mi SeonBaek, Kwang-SooKim, Jong-HoonChoi, Jae Youl
Ewha Authors
김승철김윤환
SCOPUS Author ID
김승철scopus; 김윤환scopus
Issue Date
2016
Journal Title
BIOMOLECULES & THERAPEUTICS
ISSN
1976-9148JCR Link2005-4483JCR Link
Citation
vol. 24, no. 4, pp. 402 - 409
Keywords
4-methyl-2,6-bis(1-phenylethyl)pbenolApoptotisAnti-cancer activityCordyceps Bassiana
Publisher
KOREAN SOC APPLIED PHARMACOLOGY
Indexed
SCIE; SCOPUS; KCI WOS scopus
Abstract
It has been found that 4-isopropyl-2,6-bis(1-phenylethyl)phenol (KTH-13), a novel compound isolated from Cordyceps bassiana, is able to suppress tumor cell proliferation by inducing apoptosis. To mass-produce this compound, we established a total synthesis method. Using those conditions, we further synthesized various analogs with structural similarity to KTH-13. In this study, we aimed to test their anti-cancer activity by measuring anti-proliferative and pro-apoptotic activities. Of 8 compounds tested, 4-methyl-2,6-bis(1-phenylethyl)phenol (KTH-13-Me) exhibited the strongest anti-proliferative activity toward MDA-MB 231 cells. KTH-13-Me also similarly suppressed the survival of various cancer cell lines, including C6 glioma, HCT-15, and LoVo cells. Treatment of KTH-13-Me induced several apoptotic signs in 06. glioma cells, such as morphological changes, induction of apoptotic bodies, and nuclear fragmentation and chromatin condensation. Concordantly, early-apoptotic cells were also identified by staining with FITC-Annexin V/Pl. Moreover, KTH-13-Me highly enhanced the activation of caspase-3 and caspase-9, and decreased the protein level of Bcl-2. In addition, the phosphorylation levels of Src and STAT3 were diminished in KTH-13-Me-treated C6 cells. Therefore, these results suggest that KTH-13-Me can be developed as a novel anti-cancer drug capable of blocking proliferation, inducing apoptosis, and blocking cell survival signaling in cancer cells.
DOI
10.4062/biomolther.2015.166
Appears in Collections:
의학전문대학원 > 의학과 > Journal papers
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