1. Academic Validation
  2. Synergistic anti-colon cancer effect of glycyrol and butyrate is associated with the enhanced activation of caspase-3 and structural features of glycyrol

Synergistic anti-colon cancer effect of glycyrol and butyrate is associated with the enhanced activation of caspase-3 and structural features of glycyrol

  • Food Chem Toxicol. 2020 Feb;136:110952. doi: 10.1016/j.fct.2019.110952.
Shangyun Lu 1 Shutao Yin 1 Chong Zhao 1 Lihong Fan 2 Hongbo Hu 3
Affiliations

Affiliations

  • 1 Beijing Advanced Innovation Center for Food Nutrition and Human Health, College of Food Science and Nutritional Engineering, China Agricultural University, No 17, Qinghua East Road, Haidian District, Beijing, 10083, China.
  • 2 College of Veterinary Medicine, China Agricultural University, No. 2 Yuanmingyuan West Road, Haidian District, Beijing, 100193, China. Electronic address: flh@cau.edu.cn.
  • 3 Beijing Advanced Innovation Center for Food Nutrition and Human Health, College of Food Science and Nutritional Engineering, China Agricultural University, No 17, Qinghua East Road, Haidian District, Beijing, 10083, China. Electronic address: hongbo@cau.edu.cn.
Abstract

Coumarin-based anti-cancer agents have attracted considerable attention recently. Butyrate, a major short-chain fatty acid produced in colon by gut microbiota, has been shown to exert Anticancer activity both in vitro and in vivo. In this study, we evaluated the anti-cancer effect of combining glycyrol (GC), a representative of coumarin compounds in licorice, or its analogues Glycycoumarin/Demethylsuberosin/Coumestrol (GCM/De/Coum) with butyrate in HT29 and HCT116 cells, and explored the relationship between the combined anti-cancer effect and structural features of coumarin compounds. Results showed the strongest inhibitory effect on Cancer cells was induced by GC/butyrate combination via enhanced activation of Caspase-3. Our data indicated the benzofuranyl, isopentenyl and methoxy groups presented in GC played critical role in its anti-cancer activity, while the furan group led to the further enhancement. The findings of the present study will be beneficial for developing coumarin-based compounds and coumarin compound-based regimen to fight against colon Cancer.

Keywords

Butyrate; Colon cancer; Coumarin; Glycyrol; Structure-activity.

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