Biomol Ther.
2016 Jul;24(4):402-409. 10.4062/biomolther.2015.166.
Anti-Proliferative and Pro-Apoptotic Activities of 4-Methyl-2,6-bis(1-phenylethyl)phenol in Cancer Cells
- Affiliations
-
- 1Department of Genetic Engineering, Sungkyunkwan University, Suwon 16419, Republic of Korea. jaecho@skku.edu
- 2Division of Gynecologic Oncology Department of Obstetrics and Gynecology, Ewha Womans University Mokdong Hospital College of Medicine, Ewha Womans University, Seoul 03760, Republic of Korea.
- 3Department of Chemistry, Kwangwoon University, Seoul 01897, Republic of Korea.
- 4Institute for Bio-Medical Convergence, International St. Mary's Hospital and College of Medicine, Catholic Kwandong University, Incheon 22711, Republic of Korea.
- 5Department of Veterinary Physiology, College of Veterinary Medicine, Chonbuk National University, Iksan 54596, Republic of Korea. jhkim1@chonbuk.ac.kr
- KMID: 2351689
- DOI: http://doi.org/10.4062/biomolther.2015.166
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.
- Full Text Links
-
- Actions
-
Cited
- CITED
-
- Close
- Share
-
- Similar articles
-
- 4-(Tert-butyl)-2,6-bis(1-phenylethyl)phenol induces pro-apoptotic activity
- Resveratrol at High Doses Acts as an Apoptotic Inducer in Endothelial Cells
- Protective Effects of Epigallocatechin-3-gallate against 1-methyl-4-phenylpyridinium-induced Dopaminergic Neuronal Cell Death
- Effect of Estradiol-induced E2IG5 on Breast Cancer Cell Line
- Pro-Apoptotic Activity of 4-Isopropyl-2-(1-Phenylethyl) Aniline Isolated from Cordyceps bassiana
