Kinetics of glyburide metabolism by hepatic and placental microsomes of human and baboon.

Kinetics of glyburide metabolism by hepatic and placental microsomes of human and baboon. Research Abstract Details 

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Kinetics of glyburide metabolism by hepatic and placental microsomes of human and baboon. Abstract Text:

Olga L Zharikova,Selvan Ravindran,Tatiana N Nanovskaya,Ronald A Hill,Gary D V Hankins,Mahmoud S Ahmed,

Glyburide (glibenclamide) is under investigation for treatment of gestational diabetes. Two metabolites of glyburide have been previously identified in patients, namely, 4-trans-(M1) and 3-cis-(M2) hydroxycyclohexyl glyburide. Recently, the metabolism of glyburide by microsomes of liver and placenta from humans and baboons revealed the formation of four additional metabolites: 4-cis-(M2a), 3-trans-(M3), and 2-trans-(M4) hydroxycyclohexyl glyburide, and ethyl-hydroxy glyburide (M5). The aim of this investigation was to determine the kinetics for the metabolism of glyburide by cytochrome P450 (CYP) isozymes of human and baboon placental and hepatic microsomes. The metabolism of glyburide by microsomes from the four organs revealed saturation kinetics and apparent K(m) values between 4 and 12 microM. However, the rates for formation of the metabolites varied between organs and species. M1 was the major metabolite (36% of total), formed by human hepatic microsomes with V(max) of 80+/-13 pmol mg protein(-1)min(-1), and together with M2, accounted for only 51% of the total. M5 was the major metabolite (87%) formed by human placental microsomes with V(max) of 11 pmol mg protein(-1)min(-1). In baboon liver, M5 had the highest rate of formation (V(max) 135+/-32 pmol mg protein(-1)min(-1), 39% of total), and in its placenta, was M4 (V(max) 0.7+/-0.1 pmol mg protein(-1)min(-1), 65%). The activity of human and baboon hepatic microsomes in metabolizing glyburide was similar, but the activity of human and baboon placental microsomes was 7% and 0.3% of their respective hepatic microsomes. The data obtained suggest that more than 1 CYP isozyme is responsible for catalyzing the hydroxylation of glyburide.

Kinetics of glyburide metabolism by hepatic and placental microsomes of human and baboon. Publishing Authors By Initials

OL Zharikova,S Ravindran,TN Nanovskaya,RA Hill,GD Hankins,MS Ahmed,

For similar biological phenomena, cell phenomena, and immunity: immunity: antibody specificity: species specificity research abstracts see: biological phenomena, cell phenomena, and immunity: immunity: antibody specificity: species specificity research

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Kinetics of glyburide metabolism by hepatic and placental microsomes of human and baboon. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Biochemical pharmacology

VOLUME: 73

Page Numbers: 2012-9

Journal Abbreviation:

ISSN: 0006-2952

DAY: 12

MONTH: 03

YEAR: 2007

Kinetics of glyburide metabolism by hepatic and placental microsomes of human and baboon. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 101032

Kinetics of glyburide metabolism by hepatic and placental microsomes of human and baboon. Keywords Mesh Terms:

KEYWORDS: Species Specificity

MESH TERMS: enzymology

Chemical & Substance for Abstract: Kinetics of glyburide metabolism by hepatic and placental microsomes of human and baboon. Information

Substance Name: Cytochrome P-450 Enzyme System

Registry Number: 9035-51-2

Grant and Affiliation Information for Kinetics of glyburide metabolism by hepatic and placental microsomes of human and baboon.

AFFILIATION: Department of Obstetrics & Gynecology, University of Texas Medical Branch, 301 University Blvd., Galveston, TX 77555-0587, USA.

Country: England

AGENCY: United States NICHD

GRANT: U10-HD0478

ACRONYM: HD

MEDLINETA: Biochem Pharmacol

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