2. Academic Validation
  3. Comparison of the Inhibitory Potential of Bavachalcone and Corylin against UDP-Glucuronosyltransferases

Comparison of the Inhibitory Potential of Bavachalcone and Corylin against UDP-Glucuronosyltransferases

  • Evid Based Complement Alternat Med. 2014;2014:958937. doi: 10.1155/2014/958937.
Lina Shan 1,  Shuman Yang 2,  Gang Zhang 3,  Dun Zhou 1,  Zhenyu Qiu 1,  Lei Tian 1,  Hongxia Yuan 1,  Yujun Feng 4,  Xianbao Shi 1
Affiliations

Affiliations

  • 1 The First Affiliated Hospital of Liaoning Medical University, Jinzhou 121001, China.
  • 2 Department of Environmental Health, University of Cincinnati, Cincinnati, OH 45267, USA.
  • 3 Department of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA 23219, USA.
  • 4 Maternal and Child Care Center of Qinhuangdao, Qinhuangdao 066000, China.
PMID: 24829606 DOI: 10.1155/2014/958937
Abstract

Bavachalcone and corylin are two major bioactive compounds isolated from Psoralea corylifolia L., which has been widely used as traditional Chinese medicine for many years. As two Antibiotic or Anticancer drugs, bavachalcone and corylin are used in combination with other drugs; thus it is necessary to evaluate potential pharmacokinetic herb-drug interactions (HDI) of the two bioactive compounds. The aim of the present study was to compare the effects of liver UDP-glucuronosyltransferase (UGT) 1A1, UGT1A3, UGT1A7, UGT1A8, UGT 1A10, and UGT2B4 inhibited by bavachalcone and corylin. 4-Methylumbelliferone (4-MU) was used as a nonspecific "probe" substrate. Bavachalcone had stronger inhibition on UGT1A1 and UGT1A7 than corylin which did not inhibit UGT1A1, UGT1A3, UGT1A7, UGT1A8, UGT1A10, and UGT2B4. Data fitting using Dixon and Lineweaver-Burk plots demonstrated the noncompetitive inhibition of bavachalcone against UGT1A1 and UGT1A7-mediated 4-MU glucuronidation reaction. The values of inhibition kinetic parameters (Ki) were 5.41 μ M and 4.51 μ M for UGT1A1 and UGT1A7, respectively. The results of present study suggested that there was a possibility of UGT1A1 and UGT1A7 inhibition-based herb-drug interaction associated with bavachalcone and provided the basis for further in vivo studies to investigate the HDI potential between bavachalcone and UGT substrates.

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