Biomolecules & Therapeutics  https://doi.org/10.4062/biomolther.2022.090
Synthetic Homoisoflavane Derivatives of Cremastranone Suppress Growth of Colorectal Cancer Cells through Cell Cycle Arrest and Induction of Apoptosis
Ha-Eun Shin1,†, Seul Lee2,†, Yeram Choi1, Sangkyu Park3, Sangil Kwon2, Jun-Kyu Choi3, Seung-Yong Seo2,* and Younghee Lee1,3,*
1Department of Biochemistry, College of Natural Sciences, Chungbuk National University, Cheongju 28644,
2College of Pharmacy, Gachon University, Incheon 21936,
3Biotechnology Research Institute, Chungbuk National University, Cheongju 28644, Republic of Korea
*E-mail: yhl4177@cbnu.ac.kr (Lee Y), syseo@gachon.ac.kr (Seo SY)
Tel: +82-43-261-3387 (Lee Y), +82-32-820-4949 (Seo SY)
Fax: +82-43-267-2306 (Lee Y), +82-32-820-4829 (Seo SY)
The first two authors contributed equally to this work.
Received: July 1, 2022; Revised: July 17, 2022; Accepted: July 20, 2022; Published online: August 8, 2022.
© The Korean Society of Applied Pharmacology. All rights reserved.

This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/4.0/) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract
Colorectal cancer is diagnosed as the third most prevalent cancer; thus, effective therapeutic agents are urgently required. In this study, we synthesized six homoisoflavane derivatives of cremastranone and investigated their cytotoxic effects on the human colorectal cancer cell lines HCT116 and LoVo. We further examined the related mechanisms of action using two of the potent compounds, SH-19027 and SHA-035. They substantially reduced the cell viability and proliferation in a dose-dependent manner. Treatment with SH-19027 and SHA-035 induced cell cycle arrest at the G2/M phase and increased expression of p21 both of which are implicated in cell cycle control. In addition, the apoptotic cell population and apoptosis-associated marker expression were accordingly increased. These results suggest that the synthesized cremastranone derivatives have anticancer effects through the suppression of cell proliferation and induction of apoptosis. Therefore, the synthesized cremastranone derivatives could be applied as novel therapeutic agents against colorectal cancer.
Keywords: Anticancer effect, Homoisoflavane derivatives of cremastranone, Cell cycle, Apoptosis, Colorectal cancer


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