2. Academic Validation
  3. Inhibitory effects of flavonoids isolated from Sophora flavescens on indoleamine 2,3-dioxygenase 1 activity

Inhibitory effects of flavonoids isolated from Sophora flavescens on indoleamine 2,3-dioxygenase 1 activity

  • J Enzyme Inhib Med Chem. 2019 Dec;34(1):1481-1488. doi: 10.1080/14756366.2019.1640218.
Mincheol Kwon 1 2,  Sung-Kyun Ko 3,  Mina Jang 1 2,  Gun-Hee Kim 1,  In-Ja Ryoo 1,  Sangkeun Son 1,  Hyung Won Ryu 3,  Sei-Ryang Oh 3,  Won-Kyu Lee 4,  Bo Yeon Kim 1 2,  Jae-Hyuk Jang 2 3,  Jong Seog Ahn 1 2
Affiliations

Affiliations

  • 1 Anticancer Agent Research Center, Korea Research Institute of Bioscience and Biotechnology , Cheongju , Korea.
  • 2 Department of Biomolecular Science, KRIBB School of Bioscience, Korea University of Science and Technology , Daejeon , Korea.
  • 3 Natural Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology , Cheongju , Korea.
  • 4 New Drug Development Center, Osong Medical Innovation Foundation , Cheongju , Korea.
PMID: 31423846 DOI: 10.1080/14756366.2019.1640218
Abstract

Indoleamine 2,3-dioxygenase 1 (IDO1), a tryptophan catabolising Enzyme, is known as a tumour cell survival factor that causes immune escape in several types of Cancer. Flavonoids of Sophora flavescens have a variety of biological benefits for humans; however, Cancer Immunotherapy effect has not been fully investigated. The Flavonoids (1-6) isolated from S. flavescens showed IDO1 inhibitory activities (IC50 4.3-31.4 µM). The representative Flavonoids (4-6) of S. flavescens were determined to be non-competitive inhibitors of IDO1 by kinetic analyses. Their binding affinity to IDO1 was confirmed using thermal stability and surface plasmon resonance (SPR) assays. The molecular docking analysis and mutagenesis assay revealed the structural details of the interactions between the Flavonoids (1-6) and IDO1. These results suggest that the Flavonoids (1-6) of S. flavescens, especially kushenol E (6), as IDO1 inhibitors might be useful in the development of immunotherapeutic agents against cancers.

Keywords

IDO1 inhibitor; Indoleamine 2,3-dioxygenase 1 (IDO1); flavonoid.

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