search
for
 About Bioline  All Journals  Testimonials  Membership  News


African Health Sciences
Makerere University Medical School
ISSN: 1680-6905
EISSN: 1680-6905
Vol. 15, No. 1, 2015, pp. 146-149
Bioline Code: hs15021
Full paper language: English
Document type: Research Article
Document available free of charge

African Health Sciences, Vol. 15, No. 1, 2015, pp. 146-149

 en Ganoderic acid B’s influence towards the therapeutic window of trifluoperazine (TFP)
Guo, Jun; Ni, Chenming; Liu, Xiaoyang & Liu, Tao

Abstract

Background: Ganoderic acid B is an important bioactive ingredient isolated from Ganoderma lucidum check for this species in other resources , and exhibits various pharmacological activities.
Aims: To investigate the influence of Ganoderic acid B towards the therapeutic window of trifluoperazine (TFP).
Methods: In vitro human liver microsomes (HLMs) incubation system was used to determine the inhibition of Ganoderic acid B towards the glucuronidation of trifluoperazine (TFP).
Result: Ganoderic acid B exerted concentration-dependent inhibition towards the glucuronidation of TFP. Furthermore, Dixon plot was used to determine the inhibition type. The intersection point was located in the second quadrant in Dixon plot, indicating the competitive inhibition of Ganoderic acid B towards TFP glucuronidation. Through fitting the data using competitive nonlinear fitting equation, the inhibition kinetic parameter was calculated to be 56.7 uM.
Conclusion: All this data indicated the potential influence of Ganoderic acid B-containing herbs towards therapeutic window of TFP. Given that the glucuronidation reaction of TFP is the probe reaction of UGT1A4, the data obtained from the present study also indicated the potential influence of Ganoderic acid-containing herbs towards the therapeutic window of drugs mainly undergoing UGT1A4-mediated metabolism.

Keywords
Ganoderic acid B; trifluoperazine (TFP); UDP-glucuronosyltransferase (UGT) 1A4

 
© Copyright 2015 - African Health Sciences

Home Faq Resources Email Bioline
© Bioline International, 1989 - 2024, Site last up-dated on 01-Sep-2022.
Site created and maintained by the Reference Center on Environmental Information, CRIA, Brazil
System hosted by the Google Cloud Platform, GCP, Brazil