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α-Glucosidase inhibition by prenylated and lavandulyl compounds from Sophora flavescens roots and in silico analysis.
Kim, Jang Hoon; Cho, Chong Woon; Kim, Hyo Young; Kim, Kyung Tae; Choi, Gug-Seoun; Kim, Hyeong-Hwang; Cho, In Sook; Kwon, Sun Jung; Choi, Seung-Kook; Yoon, Ju-Yeon; Yang, Seo Young; Kang, Jong Seong; Kim, Young Ho.
Afiliación
  • Kim JH; College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea; Department of Horticultural and Crop Environment, National Institute of Horticultural and Herbal Science, RDA, Wanju, 55365, Republic of Korea; Advanced Radiation Technology Institute, Korea Atomic Energy Research I
  • Cho CW; College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea.
  • Kim HY; College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea; Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeollabuk 56212, Republic of Korea.
  • Kim KT; College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea.
  • Choi GS; Department of Horticultural and Crop Environment, National Institute of Horticultural and Herbal Science, RDA, Wanju, 55365, Republic of Korea.
  • Kim HH; Department of Horticultural and Crop Environment, National Institute of Horticultural and Herbal Science, RDA, Wanju, 55365, Republic of Korea.
  • Cho IS; Department of Horticultural and Crop Environment, National Institute of Horticultural and Herbal Science, RDA, Wanju, 55365, Republic of Korea.
  • Kwon SJ; Department of Horticultural and Crop Environment, National Institute of Horticultural and Herbal Science, RDA, Wanju, 55365, Republic of Korea.
  • Choi SK; Department of Horticultural and Crop Environment, National Institute of Horticultural and Herbal Science, RDA, Wanju, 55365, Republic of Korea.
  • Yoon JY; Department of Horticultural and Crop Environment, National Institute of Horticultural and Herbal Science, RDA, Wanju, 55365, Republic of Korea.
  • Yang SY; College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea.
  • Kang JS; College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea. Electronic address: Kangjss@cnu.ac.kr.
  • Kim YH; College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea. Electronic address: yhk@cnu.ac.kr.
Int J Biol Macromol ; 102: 960-969, 2017 Sep.
Article en En | MEDLINE | ID: mdl-28455256
The enzyme α-glucosidase is a good drug target for the treatment of diabetes mellitus. Four minor flavonoids (1-4) from roots of Sophora flavescens showed the inhibitory activity, with IC50 values ranging from 11.0±0.3 to 50.6±1.3µM, toward α-glucosidase. An enzyme kinetics analysis of them revealed that the compounds 1 and 4 were non-competitive, and compounds 2 and 3 were un-competitive inhibitors. For molecular docking, 3-dimensional structure of α-glucosidase was built by homology modeling. As the result, four compounds 1-4 were confirmed to interact into common binding site of α-glucosidase. In addition, all of the four prenylated and lavandulyl compounds (1-4) were abundant in an ethyl acetate fraction separated from a methanol extract, and the potential inhibitor (3) was extracted best using tetrahydrofuran.
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Terpenos / Simulación por Computador / Extractos Vegetales / Raíces de Plantas / Sophora / Alfa-Glucosidasas / Prenilación Idioma: En Revista: Int J Biol Macromol Año: 2017 Tipo del documento: Article

Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Terpenos / Simulación por Computador / Extractos Vegetales / Raíces de Plantas / Sophora / Alfa-Glucosidasas / Prenilación Idioma: En Revista: Int J Biol Macromol Año: 2017 Tipo del documento: Article