Literature DB >> 3138501

Sulphation and glucuronidation of ethinyloestradiol in human liver in vitro.

G M Pacifici1, D J Back.   

Abstract

The sulphotransferase and the glucuronyltransferase activities were measured with [3H]ethinyloestradiol in vitro using subcellular fractions from human liver. A rapid and sensitive assay based on a single extraction in ether of the unmetabolized EE2 is described. The mean (+/- SD) of the sulphotransferase and glucuronyltransferase activities from 8 livers was 68.2 +/- 16.5 and +/- 190.4 +/- 82.3 pmol/min/mg, respectively. The kinetic parameters of both enzymes were measured in 4 livers by varying the concentrations of EE2 or the endogenous substrate. At varying concentrations of EE2 the average (+/- SD) of Vmax was 66.5 +/- 15.8 pmol/min/mg (sulphotransferase) and 404 +/- 317 pmol/min/mg (glucuronyltransferase). The mean (+/- SD) of Km was 0.0072 +/- 0.0019 mM (sulphotransferase) and 0.20 +/- 0.12 mM (glucuronyltransferase).

Entities:  

Keywords:  Biology; Contraception; Contraceptive Agents, Estrogen--analysis; Contraceptive Agents, Female--analysis; Contraceptive Agents--analysis; Developed Countries; Enzymes; Enzymes And Enzyme Inhibitors; Ethinyl Estradiol--analysis; Europe; Examinations And Diagnoses; Family Planning; Hepatic Effects; Histology; Laboratory Examinations And Diagnoses; Northern Europe; Physiology; United Kingdom

Mesh:

Substances:

Year:  1988        PMID: 3138501     DOI: 10.1016/0022-4731(88)90360-3

Source DB:  PubMed          Journal:  J Steroid Biochem        ISSN: 0022-4731            Impact factor:   4.292


  12 in total

1.  Proceedings of the British Pharmacological Society, British Pharmacology Section. 18-20 April 1990, Sheffield. Abstracts.

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2.  Effects of cytochrome P450 inducers on 17alpha-ethinyloestradiol (EE2) conjugation by primary human hepatocytes.

Authors:  A P Li; N R Hartman; C Lu; J M Collins; J M Strong
Journal:  Br J Clin Pharmacol       Date:  1999-11       Impact factor: 4.335

Review 3.  Pharmacokinetic drug interactions involving 17alpha-ethinylestradiol: a new look at an old drug.

Authors:  Hongjian Zhang; Donghui Cui; Bonnie Wang; Yong-Hae Han; Praveen Balimane; Zheng Yang; Michael Sinz; A David Rodrigues
Journal:  Clin Pharmacokinet       Date:  2007       Impact factor: 6.447

4.  Effect of ritonavir on the pharmacokinetics of ethinyl oestradiol in healthy female volunteers.

Authors:  D Ouellet; A Hsu; J Qian; C S Locke; C J Eason; J H Cavanaugh; J M Leonard; G R Granneman
Journal:  Br J Clin Pharmacol       Date:  1998-08       Impact factor: 4.335

5.  Conjugation pathways in liver disease.

Authors:  G M Pacifici; A Viani; M Franchi; S Santerini; A Temellini; L Giuliani; M Carrai
Journal:  Br J Clin Pharmacol       Date:  1990-09       Impact factor: 4.335

6.  Developmental aspects of human hepatic drug glucuronidation in young children and adults.

Authors:  C P Strassburg; A Strassburg; S Kneip; A Barut; R H Tukey; B Rodeck; M P Manns
Journal:  Gut       Date:  2002-02       Impact factor: 23.059

7.  Testosterone sulphation and glucuronidation in the human liver: interindividual variability.

Authors:  G M Pacifici; A Gucci; L Giuliani
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1997 Jul-Sep       Impact factor: 2.441

8.  The effect of various drugs on the glucuronidation of zidovudine (azidothymidine; AZT) by human liver microsomes.

Authors:  S M Sim; D J Back; A M Breckenridge
Journal:  Br J Clin Pharmacol       Date:  1991-07       Impact factor: 4.335

9.  Distribution of UDP-glucuronosyltransferase and its endogenous substrate uridine 5'-diphosphoglucuronic acid in human tissues.

Authors:  M Cappiello; L Giuliani; G M Pacifici
Journal:  Eur J Clin Pharmacol       Date:  1991       Impact factor: 2.953

10.  Interindividual variability in the glucuronidation and sulphation of ethinyloestradiol in human liver.

Authors:  A Temellini; L Giuliani; G M Pacifici
Journal:  Br J Clin Pharmacol       Date:  1991-06       Impact factor: 4.335

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