Role of Human Liver Microsomes in In Vitro Metabolism of Drugs-A Review

被引：151

作者：

Asha, Sepuri ^{[1
]}

Vidyavathi, Maravajhala ^{[1
]}

机构：

[1] Sri Padmavati Mahila Visvavidyalayam Womens Univ, Inst Pharmaceut Technol, Tirupati 517502, Andhra Pradesh, India

来源：

APPLIED BIOCHEMISTRY AND BIOTECHNOLOGY | 2010年 / 160卷 / 06期

关键词：

Biotransformation; CYP450; Drug; Human liver microsomes; In vitro metabolism study; Metabolism; Metabolites; HUMAN CYTOCHROME-P450 ISOFORMS; ENZYME-KINETIC PARAMETERS; N-DEMETHYLATION; OXIDATIVE-METABOLISM; S-MEPHENYTOIN; STEREOSELECTIVE METABOLISM; CULTURED-HEPATOCYTES; P450; 2D6; TRIAZOLAM BIOTRANSFORMATION; HEPATIC BIOTRANSFORMATION;

D O I：

10.1007/s12010-009-8689-6

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Drug metabolism studies are essential and necessary during the evaluation of drugs. This review discusses the in vitro human liver models to estimate the drug metabolic fates in vivo. Different approaches are provided and emphasis is placed on the potential of human liver microsomes for drug metabolism and inhibition studies. The methodology for these studies using human liver microsomes, applications of human liver microsomes, and the drugs studied by human liver microsomes are listed. Human liver microsomes represent a critical experimental model for the evaluation of drug metabolites with a high probability of clinical success.

引用

页码：1699 / 1722

页数：24

共 179 条

[1]

Abou-Donia M.B., 1995, CRC HDB TOXICOLOGY, P539

[2] DIAZEPAM METABOLISM BY HUMAN LIVER-MICROSOMES IS MEDIATED BY BOTH S-MEPHENYTOIN HYDROXYLASE AND CYP3A ISOFORMS [J].

ANDERSSON, T ;

MINERS, JO ;

VERONESE, ME ;

BIRKETT, DJ .

BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1994, 38 (02) :131-137

[3]

Annaert PP, 2001, DRUG METAB DISPOS, V29, P1277

[4] 6α-hydroxylation of taurochenodeoxycholic acid and lithocholic acid by CYP3A4 in human liver microsomes [J].

Araya, Z ;

Wikvall, K .

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS, 1999, 1438 (01) :47-54

[5]

Baldwin SJ, 1999, BRIT J CLIN PHARMACO, V48, P424

[6] Venlafaxine: In vitro inhibition of CYP2D6 dependent imipramine and desipramine metabolism; Comparative studies with selected SSRIs, and effects on human hepatic CYP3A4, CYP2C9 and CYPIA2 [J].

Ball, SE ;

Ahern, D ;

Scatina, J ;

Kao, J .

BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1997, 43 (06) :619-626

[7] Characterization of the cytochrome P450 enzymes and enzyme kinetic parameters for metabolism of BVT.2938 using different in vitro systems [J].

Baranczewski, P ;

Edlund, PO ;

Postlind, H .

JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2006, 40 (05) :1121-1130

[8] Halofantrine metabolism in microsomes in man: Major role of CYP 3A4 and CYP 3A5 [J].

Baune, B ;

Flinois, JP ;

Furlan, V ;

Gimenez, F ;

Taburet, AM ;

Becquemont, L ;

Farinotti, R .

JOURNAL OF PHARMACY AND PHARMACOLOGY, 1999, 51 (04) :419-426

[9] Utility of hepatocytes to model species differences in the metabolism of loxtidine and to predict pharmacokinetic parameters in rat, dog and man [J].

Bayliss, MK ;

Bell, JA ;

Jenner, WN ;

Park, GR ;

Wilson, K .

XENOBIOTICA, 1999, 29 (03) :253-268

[10]

BEAUNE PH, 1986, DRUG METAB DISPOS, V14, P437

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