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Titolo:
INHIBITORY EFFECT OF TMK688 ON SKIN TUMOR INITIATION CAUSED BY 7,12-DIMETHYLBENZ[A]ANTHRACENE IN RELATION TO INHIBITION OF ARYL-HYDROCARBONHYDROXYLASE-ACTIVITY AND CYP1A1 MESSENGER-RNA INDUCTION
Autore:
JIANG H; YAMAMOTO S; OZAWA S; SHIMADA M; YAMAZOE Y; KATO R;
Indirizzi:
KEIO UNIV,SCH MED,DEPT PHARMACOL,SHINJUKU KU,35 SHINANOMACHI TOKYO 160 JAPAN KEIO UNIV,SCH MED,DEPT PHARMACOL,SHINJUKU KU TOKYO 160 JAPAN
Titolo Testata:
Pharmacology
fascicolo: 2, volume: 53, anno: 1996,
pagine: 123 - 132
SICI:
0031-7012(1996)53:2<123:IEOTOS>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
LIPOXYGENASE INHIBITOR; BALB/C MICE; MOUSE SKIN; CARCINOGENESIS; SEQUENCE; ACID; RNA; CYTOCHROME-P450; TUMORIGENESIS; ACTIVATION;
Keywords:
CYP1A1; ARYL HYDROCARBON HYDROXYLASE; TMK688; TMK777; POLYCYCLIC AROMATIC HYDROCARBONS; 3-METHYLCHOLANTHRENE; 7,12-DIMETHYLBENZ[A] ANTHRACENE; BENZO[A]PYRENE; SKIN TUMOR INITIATION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
31
Recensione:
Indirizzi per estratti:
Citazione:
H. Jiang et al., "INHIBITORY EFFECT OF TMK688 ON SKIN TUMOR INITIATION CAUSED BY 7,12-DIMETHYLBENZ[A]ANTHRACENE IN RELATION TO INHIBITION OF ARYL-HYDROCARBONHYDROXYLASE-ACTIVITY AND CYP1A1 MESSENGER-RNA INDUCTION", Pharmacology, 53(2), 1996, pp. 123-132

Abstract

Oral administration of TMK688 (1-([5'-(3 ''-methoxy-4 ''- ethoxycarbonyloxyphenyl)-2',4'-pentadienoyl] aminoethyl)-4-diphenylmethoxypiperidine: 30 mg/kg) at 6 h and 30 min prior to and at 30 min after a singletopical application of 7,12-dimethylbenz[a]anthracene (DMBA) to dorsal skins of mice reduced both tumor incidence and number of tumors per mouse in the DMBA-initiated and 12-O-tetradecanoylphorbol-13-acetate (TPA)-promoted two-stage mouse skin carcinogenesis, TMK688 and its active metabolite TMK777 (1-{[5'(3 ''-methoxy-4 2',4'-pentadienoyl]-amino-ethyl}-4-diphenylmethoxy piperidine) inhibited 3-methylchol-anthrene (MC)-induced epidermal aryl hydrocarbon hydroxylase (AHH) activity in aconcentration-dependent manner. IC50 Of TMK688 and TMK777 was 0.18 and 0.01 mu mol/l, respectively. Oral administration of TMK688 (30 mg/kg) almost completely suppressed Cyp1a1 mRNA levels in mouse epidermis induced by a topical application of MC (40 mg/kg) or benzo[a]pyrene (200 nmol) to mouse skin, Oral administration of TMK688 (30 mg/kg) also almost completely inhibited induction of epidermal AHH activity caused by a topical application of MC. These results indicate that oral administration of TMK688 inhibited DMBA-caused skin tumor initiation at least in part by inhibiting Cyp1a1 mRNA induction and epidermal AHH activity.

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Documento generato il 05/12/20 alle ore 00:22:04