In Vitro Inhibition Of Herbal Constituents On Ugt2b7 Enzyme Activity

Herb-drug interaction may cause induction and inhibition of drug metabolizing enzymes which may lead to adverse effect in the body. Two major drug-metabolism enzymes in the human body are cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes. Whilst CYP-mediated herb-drug interactions...

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Main Author:	Abdullah, Nurul Huda
Format:	Thesis
Language:	English
Published:	2018
Subjects:	R5-920 Medicine (General)
Online Access:	http://eprints.usm.my/49695/1/NURUL%20HUDA%20BINTI%20ABDULLAH_hj.pdf
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spelling	my-usm-ep.496952021-08-23T09:40:33Z In Vitro Inhibition Of Herbal Constituents On Ugt2b7 Enzyme Activity 2018-08 Abdullah, Nurul Huda R5-920 Medicine (General) Herb-drug interaction may cause induction and inhibition of drug metabolizing enzymes which may lead to adverse effect in the body. Two major drug-metabolism enzymes in the human body are cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes. Whilst CYP-mediated herb-drug interactions have been evaluated in numerous studies, the interactions on UGT enzymes are still limited. In the current study, the in vitro inhibitory effect of thirteen herbal bioactive constituents on one of the most important UGT isoform which is UGT2B7 in human (HLM) and rat liver microsomes (RLM) had been investigated. UGT2B7 is an UGT isoform that is responsible for conjugation of opioids like morphine and codeine, non-steroidal anti-inflammatory drugs such as diclofenac and ketoprofen and an anti-HIV drug, zidovudine (ZDV) with glucuronic acid. In this study, ZDV was used as the probe substrate for evaluating UGT2B7 activity. The herbal bioactive constituents studied for potential UGT2B7 inhibitory potency were andrographolide, arecaidine, arecoline, (+)-catechin, gallic acid, kaempferol-3-rutinoside, mangiferin, mitragynine, quercetin, vanillin, vitexin, isovitexin and zerumbone. The formation of ZDV glucuronide (ZDVG) from ZDV by HLM and RLM was determined using a validated high performance liquid chromatography method. The enzyme kinetics parameters of zidovudine glucuronidation which are Vmax and Km values in HLM were 1450 ± 26.06 pmol/mg/min and 0.88 ± 0.05 mM respectively with an intrinsic clearance value (Vmax/Km) of 1.65 μL/mg/min. 2018-08 Thesis http://eprints.usm.my/49695/ http://eprints.usm.my/49695/1/NURUL%20HUDA%20BINTI%20ABDULLAH_hj.pdf application/pdf en public masters Universiti Sains Malaysia Pusat Penyelidikan Dadah & Ubat-ubatan
institution	Universiti Sains Malaysia
collection	USM Institutional Repository
language	English
topic	R5-920 Medicine (General)
spellingShingle	R5-920 Medicine (General) Abdullah, Nurul Huda In Vitro Inhibition Of Herbal Constituents On Ugt2b7 Enzyme Activity
description	Herb-drug interaction may cause induction and inhibition of drug metabolizing enzymes which may lead to adverse effect in the body. Two major drug-metabolism enzymes in the human body are cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes. Whilst CYP-mediated herb-drug interactions have been evaluated in numerous studies, the interactions on UGT enzymes are still limited. In the current study, the in vitro inhibitory effect of thirteen herbal bioactive constituents on one of the most important UGT isoform which is UGT2B7 in human (HLM) and rat liver microsomes (RLM) had been investigated. UGT2B7 is an UGT isoform that is responsible for conjugation of opioids like morphine and codeine, non-steroidal anti-inflammatory drugs such as diclofenac and ketoprofen and an anti-HIV drug, zidovudine (ZDV) with glucuronic acid. In this study, ZDV was used as the probe substrate for evaluating UGT2B7 activity. The herbal bioactive constituents studied for potential UGT2B7 inhibitory potency were andrographolide, arecaidine, arecoline, (+)-catechin, gallic acid, kaempferol-3-rutinoside, mangiferin, mitragynine, quercetin, vanillin, vitexin, isovitexin and zerumbone. The formation of ZDV glucuronide (ZDVG) from ZDV by HLM and RLM was determined using a validated high performance liquid chromatography method. The enzyme kinetics parameters of zidovudine glucuronidation which are Vmax and Km values in HLM were 1450 ± 26.06 pmol/mg/min and 0.88 ± 0.05 mM respectively with an intrinsic clearance value (Vmax/Km) of 1.65 μL/mg/min.
format	Thesis
qualification_level	Master's degree
author	Abdullah, Nurul Huda
author_facet	Abdullah, Nurul Huda
author_sort	Abdullah, Nurul Huda
title	In Vitro Inhibition Of Herbal Constituents On Ugt2b7 Enzyme Activity
title_short	In Vitro Inhibition Of Herbal Constituents On Ugt2b7 Enzyme Activity
title_full	In Vitro Inhibition Of Herbal Constituents On Ugt2b7 Enzyme Activity
title_fullStr	In Vitro Inhibition Of Herbal Constituents On Ugt2b7 Enzyme Activity
title_full_unstemmed	In Vitro Inhibition Of Herbal Constituents On Ugt2b7 Enzyme Activity
title_sort	in vitro inhibition of herbal constituents on ugt2b7 enzyme activity
granting_institution	Universiti Sains Malaysia
granting_department	Pusat Penyelidikan Dadah & Ubat-ubatan
publishDate	2018
url	http://eprints.usm.my/49695/1/NURUL%20HUDA%20BINTI%20ABDULLAH_hj.pdf
_version_	1747822010668417024

In Vitro Inhibition Of Herbal Constituents On Ugt2b7 Enzyme Activity

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