Journal of Microbiology and Biotechnology

The Korean Society for Microbiology and Biotechnology (한국미생물·생명공학회)
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Inhibitory Activity of 4-O-Benzoyl-3'-O-(O-Methylsinapoyl)Sucrose from Polygala tenuifolia on Escherichia coli β-Glucuronidase

  • Kim, Jang Hoon (Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA) ;
  • Vinh, Le Ba (Institute of Marine Biochemistry(IMBC), Vietnam Academy of Science and Technology(VAST)) ;
  • Hur, Mok (Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA) ;
  • Koo, Sung-Cheol (Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA) ;
  • Park, Woo Tae (Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA) ;
  • Moon, Youn-Ho (Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA) ;
  • Lee, Yoon Jeong (Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA) ;
  • Kim, Young Ho (College of Pharmacy, Chungnam National University) ;
  • Huh, Yun-Chan (Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA) ;
  • Yang, Seo Young (Department of Pharmaceutical Engineering, Sangji University)
  • Received : 2021.08.06
  • Accepted : 2021.09.08
  • Published : 2021.11.28
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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-O-Benzoyl-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.

Keywords

Acknowledgement

This work was supported by the basic research project(PJ012559012021) of National Institute of Horticultural and Herbal Science, RDA.

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