Identification and biological evaluation of natural product Biochanin A

  • Bioorg Chem. 2020 Apr;97:103674. doi: 10.1016/j.bioorg.2020.103674.
Lei Wang  1 ,  Lingzhao Li  1 ,  Quanxiang Han  1 ,  Xiaofang Wang  2 ,  Di Zhao  3 ,  Junqi Liu  4
Affiliations
  • 1. Department of Radiation Oncology, Zhengzhou Central Hospital Affiliated to Zhengzhou University, Zhengzhou 450007, China.
  • 2. Henan Provincial People's Hospital, Henan Reproductive Hospital, People's Hospital of Zhengzhou University, Zhengzhou 450003, China.
  • 3. Department of Radiation Oncology, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China.
  • 4. Department of Radiation Oncology, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China. Electronic address: [email protected].
PMID: 32097796 DOI: 10.1016/j.bioorg.2020.103674
Abstract

Natural products have shown promise for epigenetic modulations and thus are therapeutically potential for Cancer prevention and treatment. In this work, we report the identification of natural product Biochanin A as a new LSD1 inhibitor and further biological evaluation in gastric MGC-803 cells. Biochanin A effectively and reversibly inhibited LSD1 (IC50 = 2.95 μM) and showed selective inhibition to LSD1 over MAO-A/B. In gastric MGC-803 cells, Biochanin A induced accumulation of H3K4me1/2, inhibited cell growth moderately (IC50 = 6.77 µM), but was less toxic to normal GES-1 (IC50 > 32 µM). Mechanistic studies showed that Biochanin A suppressed colony formation, cell Apoptosis, and migration of MGC-803 cells. This study may help to elucidate the Anticancer mechanisms of Biochanin A.

Keywords
Biochanin A; Cancer therapy; LSD1 inhibitor; Natural products.
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