|
KMID : 0545120210310111576
|
|
Journal of Microbiology and Biotechnology
2021 Volume.31 No. 11 p.1576 ~ p.1582
|
|
|
Inhibitory Activity of 4-O-Benzoyl-3′-O-(OMethylsinapoyl) Sucrose from Polygala tenuifolia on Escherichia coli β-Glucuronidase
|
|
Kim Jang-Hoon
Vinh Le Ba
Hur Mok
Koo Sung-Cheol
Park Woo-Tae
Moon Youn-Ho
Lee Yoon-Jeong
Kim Young-Ho
Huh Yun-Chan
Yang Seo-Young
|
|
|
Abstract
|
|
|
|
Bacterial β-glucuronidase in the intestine is involved in the conversion of 7-ethyl-10- hydroxycamptochecin glucuronide (derived from irinotecan) to 7-ethyl-10-hydroxycamptothecin, which causes intestinal bleeding and diarrhea (side effects of anti-cancer drugs). Twelve compounds (1?12) from Polygala tenuifolia were evaluated in terms of β-glucuronidase inhibition in vitro. 4-OBenzoyl- 3′-O-(O-methylsinapoyl) sucrose (C3) was highly inhibitory at low concentrations. C3 (an uncompetitive inhibitor) exhibited a ki value of 13.4 μM; inhibitory activity increased as the substrate concentration rose. Molecular simulation revealed that C3 bound principally to the Gln158?Tyr160 enzyme loop. Thus, C3 will serve as a lead compound for development of new β- glucuronidase inhibitors.
|
|
|
KEYWORD
|
|
|
β-glucuronidase, Polygala tenuifolia, uncompetitive inhibitor, molecular simulation
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
  
|