Inhibitory effects of flavonoids isolated from Sophora flavescens on indoleamine 2,3-dioxygenase 1 activity = Sophora flavescens에서 분리 한 flavonoids가 indoleamine 2,3-dioxygenase 1 활성에 미치는 억제 효과

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Title
Inhibitory effects of flavonoids isolated from Sophora flavescens on indoleamine 2,3-dioxygenase 1 activity = Sophora flavescens에서 분리 한 flavonoids가 indoleamine 2,3-dioxygenase 1 활성에 미치는 억제 효과
Author(s)
Mincheol Kwon; Sung-Kyun Ko; Mina Jang; Gun-Hee Kim; In Ja Ryoo; Sangkeun Son; Hyung Won RyuSei-Ryang Oh; W K Lee; Bo Yeon KimJae-Hyuk JangJong Seog Ahn
Bibliographic Citation
Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 34, no. 1, pp. 1481-1488
Publication Year
2019
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.
Keyword
flavonoidIDO1 inhibitorIndoleamine 2,3-dioxygenase 1 (IDO1)Sophora flavescens
ISSN
1475-6366
Publisher
T&F (Taylor & Francis)
DOI
http://dx.doi.org/10.1080/14756366.2019.1640218
Type
Article
Appears in Collections:
Ochang Branch Institute > Natural Medicine Research Center > 1. Journal Articles
Ochang Branch Institute > Anticancer Agent Research Center > 1. Journal Articles
Ochang Branch Institute > 1. Journal Articles
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