Protein Information

Name cytochrome P450 1A1
Synonyms AHH; AHRR; Arylhydrocarbon hydroxylase; CP11; CYP 1; CYP1; CYP1A1; CYPIA 1…

Compound Information

Name thiabendazole
CAS

Reference List

PubMed Abstract RScore(About this table)
14987951 Lemaire G, Delescluse C, Pralavorio M, Ledirac N, Lesca P, Rahmani R: The role of protein tyrosine kinases in CYP1A1 induction by omeprazole and thiabendazole in rat hepatocytes. Life Sci. 2004 Mar 19;74(18):2265-78.

Benzimidazoles compounds like omeprazole (OME) and thiabendazole (TBZ) mediate CYP1A1 induction differently from classical aryl hydrocarbon receptor (AhR) ligands, 3-methylcholanthrene (3-MC) and 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD).
93(1,1,2,8) Details
8607843 Rey-Grobellet X, Ferre N, Eeckhoutte C, Larrieu G, Pineau T, Galtier P: Structural requirements for the induction of cytochromes P450 by benzimidazole anthelmintic derivatives in cultured rabbit hepatocytes. Biochem Biophys Res Commun. 1996 Mar 27;220(3):789-94.

The effect of sulfur-containing benzimidazoles (thiabendazole, 5-hydroxy-thiabendazole, cambendazole) and sulfur-free derivatives (benzimidazole, carbendazim and 5-hydroxycarbendazim) on cytochrome P450 enzymes was investigated in primary cultures of rabbit hepatocytes considered 72 h after plating.
Experiments using actinomycin D strongly suggest that these compounds have a transcriptional control on both CYP1A1 and CYP1A2 genes in primary hepatocytes.
1(0,0,0,1) Details
11226373 Delescluse C, Ledirac N, Li R, Piechocki MP, Hines RN, Gidrol X, Rahmani R: Induction of cytochrome P450 1A1 gene expression, oxidative stress, and genotoxicity by carbaryl and thiabendazole in transfected human HepG2 and lymphoblastoid cells. Biochem Pharmacol. 2001 Feb 15;61(4):399-407.

Carbaryl and thiabendazole were found to activate CYP1A1 at the level of transcription, as demonstrated by the dose-dependent increase in reporter CAT and CYP1A1 mRNAs.
89(1,1,2,4) Details
9784250 Kikuchi H, Hossain A, Yoshida H, Kobayashi S: Induction of cytochrome P-450 1A1 by omeprazole in human HepG2 cells is protein tyrosine kinase-dependent and is not inhibited by alpha-naphthoflavone. Arch Biochem Biophys. 1998 Oct 15;358(2):351-8.

Benzimidazole compounds, such as omeprazole and thiabendazole, are a different type of CYP1A1 inducer from Ah receptor-ligands, such as TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) and 3-methylcholanthrene.
35(0,1,1,5) Details
10445394 Kikuchi H, Hossain A: Signal transduction-mediated CYP1A1 induction by omeprazole in human HepG2 cells. Exp Toxicol Pathol. 1999 Jul;51(4-5):342-6.

Benzimidazole compounds, such as omeprazole and thiabendazole, are a different type of CYP1A1-inducer from Ah receptor-ligands, such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and 3-methylcholanthrene.
34(0,1,1,4) Details
10103034 Backlund M, Weidolf L, Ingelman-Sundberg M: Structural and mechanistic aspects of transcriptional induction of cytochrome P450 1A1 by benzimidazole derivatives in rat hepatoma H4IIE cells. Eur J Biochem. 1999 Apr;261(1):66-71.

Omeprazole, thiabendazole, carbendazim, 2-mercaptobenzimidazole and 2-mercapto-5-methoxybenzimidazole caused a dose-dependent increase in CYP1A1 protein levels that reached maximum effect at 250 microm, as measured by Western blot.
16(0,0,2,6) Details
8900397 Kikuchi H, Kato H, Mizuno M, Hossain A, Ikawa S, Miyazaki J, Watanabe M: Differences in inducibility of CYP1A1-mRNA by benzimidazole compounds between human and mouse cells: evidences of a human-specific signal transduction pathway for CYP1A1 induction. Arch Biochem Biophys. 1996 Oct 15;334(2):235-40.

Three benzimidazole compounds, omeprazole (OP), thiabendazole (TBZ), and lansoprazole (LP), were compared with respect to the induction of CYP1A1-mRNA in human hepatoma cells, HepG2.
9(0,0,1,4) Details
9345309 Calleja C, Eeckhoutte C, Larrieu G, Dupuy J, Pineau T, Galtier P: Differential effects of interleukin-1 beta, interleukin-2, and interferon-gamma on the inducible expression of CYP 1A1 and CYP 1A2 in cultured rabbit hepatocytes. Biochem Biophys Res Commun. 1997 Oct 9;239(1):273-8.


However specific patterns of action are revealed: IL-1 beta is the most potent cytokine in regard to CYP1A1/2 mRNA suppression whereas IL-2 exerts repressive effects only on P4501A1 induced expression.
2(0,0,0,2) Details
15110098 Price RJ, Scott MP, Walters DG, Stierum RH, Groten JP, Meredith C, Lake BG: Effect of thiabendazole on some rat hepatic xenobiotic metabolising enzymes. Food Chem Toxicol. 2004 Jun;42(6):899-908.

The administration of high doses of TB resulted in the induction of 7-ethoxyresorufin O-deethylase and 7-pentoxyresorufin O-depentylase activities, CYP1A1, CYP1A2, CYP2B1 and CYP2B1/2 mRNA levels and CYP1A2 and CYP2B1/2 apoprotein levels.
1(0,0,0,1) Details
8819304 Rey-Grobellet X, Eeckhoutte C, Sutra JF, Alvinerie M, Galtier P: Major involvement of rabbit liver cytochrome P4501A in thiabendazole 5-hydroxylation. Xenobiotica. 1996 Jul;26(7):765-78.

These treatments led to specific induction of CYP1A1, 1A2, 2B4, 3A6 and 4A1 respectively. 3.
1(0,0,0,1) Details
19754423 Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218.

In particular, several therapeutic drugs including antofloxacin, carbamazepine, dihydralazine, furafylline, isoniazid, rofecoxib, clorgyline, thiabendazole, and zileuton are mechanism-based inhibitors of CYP1A2.
Similar to CYP1A1 and 1B1, CYP1A2 is primarily regulated by the aromatic hydrocarbon receptor (AhR), a ligand-activated transcription factor and a basic helix-loop-helix protein belonging to the Per-Arnt-Sim family of transcription factors.
1(0,0,0,1) Details
10936227 Coulet M, Eeckhoutte C, Larrieu G, Sutra JF, Alvinerie M, Mace K, Pfeifer A, Zucco F, Stammati AL, De Angelis I, Vignoli AL, Galtier P: Evidence for cytochrome P4501A2-mediated protein covalent binding of thiabendazole and for its passive intestinal transport: use of human and rabbit derived cells. Chem Biol Interact. 2000 Jul 3;127(2):109-24.

0(0,0,0,0) Details