Title of article :
In vitro evidence for bakuchiol’s influence towards drug metabolism through inhibition of UDP-glucuronosyltransferase (UGT) 2B7
Author/Authors :
Xu, Yu Nanjing Medical University - Huai’an First People’s Hospital - Department of Otorhinolaryngology, China , Li, Peizhong Nanjing Medical University - Huai’an First People’s Hospital - Department of Otorhinolaryngology, China , Zhang, Xin Nanjing Medical University - Huai’an First People’s Hospital - Department of Otorhinolaryngology, China , Wang, Junying Nanjing Medical University - Huai’an First People’s Hospital - Department of Otorhinolaryngology, China , Gu, Dongsheng Nanjing Medical University - Huai’an First People’s Hospital - Department of Otorhinolaryngology, China , Wang, Yao Nanjing Medical University - Huai’an First People’s Hospital - Pharmaceutical Preparation Section, China , xu, y. department of otorhinolaryngology,huai’an first people’s hospital,nanjing medical university,6 beijing road west,huai’an, China , li, p. department of otorhinolaryngology,huai’an first people’s hospital,nanjing medical university,6 beijing road west,huai’an, China , zhang, x. department of otorhinolaryngology,huai’an first people’s hospital,nanjing medical university,6 beijing road west,huai’an, China , wang, j. department of otorhinolaryngology,huai’an first people’s hospital,nanjing medical university,6 beijing road west,huai’an, China , gu, d. department of otorhinolaryngology,huai’an first people’s hospital,nanjing medical university,6 beijing road west,huai’an, China , wang, y. pharmaceutical preparation section,huai’an first people’s hospital,nanjing medical university,6 beijing road west,huai’an, China
From page :
564
To page :
569
Abstract :
Background: Inhibition of drug-metabolizing enzymes (DMEs) has been regarded as one of the most important reason for clinical drug-drug interaction. Aim: The aim of the present study is to evaluate the inhibition of bakuchiol towards UDP-glucuronosyltransferase (UGT) 2B isoforms. Methods: In vitro recombinant UGT2B-catalyzed 4-methylumbelliferone glucuronidation was used as the probe reaction. Dixon plot and Lineweaver-Burk plot were employed to determine the inhibition kinetic type, and nonlinear regression of data was utilized to calculate the inhibition kinetic parameter (Ki). In vitro-in vivo extrapolation (IVIVE) was carried out to predict in vivo inhibition magnitude. Results: Among the tested UGT2B isoforms, UGT2B7 was inhibited by the strongest intensity. The noncompetitive inhibition was demonstrated by the results obtained from Dixon plot and Lineweaver-Burk plot. The Ki value was calculated to be 10.7 μM. In combination with the reported concentration after an intravenous administration of bakuchiol (15 mg/kg) in rats, the high risk of in vivo inhibition of bakuchiol towards UGT2B7-catalyzed metabolism of drugs was indicated.Conclusion: All these results provide an important information for the risk evaluation of the clinical utilization of bakuchiol.
Keywords :
bakuchiol , drug , drug interaction , drug , metabolizing enzymes
Journal title :
African Health Sciences
Journal title :
African Health Sciences
Record number :
2634388
Link To Document :
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