Anti-proliferative and pro-apoptotic activities of 4-methyl-2,6-bis(1-phenylethyl)phenol in cancer cells

Nak Yoon Sung, Seung Cheol Kim, Yun Hwan Kim, Gihyeon Kim, Yunmi Lee, Gi Ho Sung, Ji Hye Kim, Woo Seok Yang, Mi Seon Kim, Kwang Soo Baek, Jong Hoon Kim, Jae Youl Cho

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

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 C6 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/PI. 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.

Original languageEnglish
Pages (from-to)402-409
Number of pages8
JournalBiomolecules and Therapeutics
Volume24
Issue number4
DOIs
StatePublished - Jul 2016

Keywords

  • 4-methyl-2,6-bis(1-phenylethyl)phenol
  • Anti-cancer activity
  • Apoptotis
  • Cordyceps bassiana

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