Protein Information

Name CYP3A4
Synonyms CP33; CYP3; HLP; CYP3A; CP34; CYP 3A4; CYP 3; CYP3A3…

Compound Information

Name 1-naphthol
CAS 1-naphthalenol

Reference List

PubMed Abstract RScore(About this table)
19142739 Thibaut R, Schnell S, Porte C: Assessment of metabolic capabilities of PLHC-1 and RTL-W1 fish liver cell lines. Cell Biol Toxicol. 2009 Dec;25(6):611-22. Epub 2009 Jan 15.

Functionality of CYP3A-, CYP2M- and CYP2K-like enzymes was assessed by studying the hydroxylation of testosterone (T) and lauric acid (LA), and glucuronidation and sulfation capacity was assessed by looking at 1-naphthol (1-N) and T conjugation.
32(0,1,1,2) Details
16243959 Cho TM, Rose RL, Hodgson E: In vitro metabolism of naphthalene by human liver microsomal cytochrome P450 enzymes. Drug Metab Dispos. 2006 Jan;34(1):176-83. Epub 2005 Oct 21.

P450 isoform screening of naphthalene metabolism identified CYP1A2 as the most efficient isoform for producing dihydrodiol and 1-naphthol, and CYP3A4 as the most effective for 2-naphthol production.
32(0,1,1,2) Details
18447001 Cho TM, Rose RL, Hodgson E: The effect of chlorpyrifos-oxon and other xenobiotics on the human cytochrome P450-dependent metabolism of naphthalene and deet. Drug Metabol Drug Interact. 2007;22(4):235-62.

CPO significantly activated the production of 1-naphthol (5-fold), 2-naphthol (10-fold), trans-1,2-dihydro-1,2-naphthalenediol (1.5-fold), and 1,4-naphthoquinone from naphthalene by human liver microsomes (HLM).
CPO inhibited CYP1A2 production of naphthalene metabolites, while activating their production by CYP3A4.
5(0,0,0,5) Details
18602459 Croera C, Ferrario D, Gribaldo L: In vitro toxicity of naphthalene, 1-naphthol, 2-naphthol and 1,4-naphthoquinone on human CFU-GM from female and male cord blood donors. Toxicol In Vitro. 2008 Sep;22(6):1555-61. Epub 2008 Jun 17.

The mRNA expression of Cyp1A2 and Cyp3A4 was also evaluated.
1(0,0,0,1) Details
11311212 Schaaf GJ, de Groene EM, Maas RF, Commandeur JN, Fink-Gremmels J: Characterization of biotransformation enzyme activities in primary rat proximal tubular cells. Chem Biol Interact. 2001 Apr 16;134(2):167-90.

Specific marker substrates for determining cytochrome P450 (CYP450) activity of primary cultured PT cells include 7-ethoxyresorufin (CYP1A1), caffeine (CYP1A), testosterone (CY2B/C, CYP3A), tolbutamide (CYP2C) and dextromethorphan (CYP2D1).
Activity of the phase II biotransformation enzymes GST, GGT, beta-lyase and UGT was determined with 1-chloro-2,4-dinitrobenzene, L-glutamic acid gamma-(7-amido-4-methyl-coumarin), S-(1,1,2,2-tetrafluoroethyl)-L-cysteine and 1-naphthol, respectively, as marker substrates.
1(0,0,0,1) Details
9134007 Le HT, Franklin MR: Selective induction of phase II drug metabolizing enzyme activities by quinolines and isoquinolines. Chem Biol Interact. 1997 Mar 14;103(3):167-78.

Rats treated with quinoline, and to a lesser extent, isoquinoline (75 mg/kg, daily for 3 days) showed induction of phase II drug metabolizing enzyme activities without inducing either cytochrome P450 concentration or CYP1A-, CYP2B-, CYP2E-, and CYP3A-selective activities.
Elevations of UDP-glucuronosyltransferase activities towards 4-nitrophenol, 1-naphthol, and morphine elicited by quinoline (1.9- to 2.7-fold), were greater than those elicited by isoquinoline (1.4- to 1.8-fold).
1(0,0,0,1) Details
14738905 Nebbia C, Dacasto M, Carletti M: Postnatal development of hepatic oxidative, hydrolytic and conjugative drug-metabolizing enzymes in female horses. Life Sci. 2004 Feb 13;74(13):1605-19.

Accordingly, a general increasing trend was recorded in the rate of the in vitro metabolism of the substrates reported to be related to CYP2B-, CYP2E- or CYP3A, although, as detected by Western immunoblotting, only the levels of proteins recognized by anti-rat CYP3A- and CYP2B antibodies appeared to increase consistently.
Also the carboxylesterases and uridindiphosphoglucuronyl-transferase (UGT) activity toward 1-naphthol displayed a similar trend, glutathione S-transferase accepting 3,4-dichloronitrobenzene as a substrate being the only enzyme activity showing an age-related decline.
1(0,0,0,1) Details