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Research ArticleArticle

Disposition and Pharmacokinetics of Phenethyl Isothiocyanate and 6-Phenylhexyl Isothiocyanate in F344 Rats

C. Clifford Conaway, Ding Jiao, Toshiyuki Kohri, Leonard Liebes and Fung-Lung Chung
Drug Metabolism and Disposition January 1999, 27 (1) 13-20;
C. Clifford Conaway
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Ding Jiao
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Toshiyuki Kohri
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Leonard Liebes
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Fung-Lung Chung
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Abstract

Naturally occurring phenethyl isothiocyanate (PEITC) and its synthetic homolog 6-phenylhexyl isothiocyanate (PHITC) are both effective inhibitors of 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone-induced lung tumor development in A/J mice and F344 rats. To help explain why PHITC is considerably more efficacious than PEITC in chemopreventive potency, comparative disposition and pharmacokinetics data for male F344 rats were obtained after a single gavage dose of 50 μmol/kg (3.71 μCi/μmol) [14C]PEITC or 50 μmol/kg (6.59 μCi/μmol) [14C]PHITC in corn oil. After [14C]PEITC dosing, whole blood 14C peaked at 2.9 h, with an elimination half-life (T1/2e) of 21.7 h; blood 14C from [14C]PHITC-treated rats peaked at 8.9 h, with an T1/2e of 20.5 h. In lungs, the target organ, the T1/2e for [14C]PHITC and its labeled metabolites were more than twice that for [14C]PEITC and its labeled metabolites. The effective dose (area under the concentration-time curve) for 14C from PHITC was greater than 2.5 times the area under the concentration-time curve of14C from PEITC in liver, lungs, and several other tissues. During 48 h, approximately 16.5% of the administered dose of [14C]PHITC was expired as [14C]CO2, more than 100 times the [14C]CO2 expired by rats treated with [14C]PEITC. In rats given [14C]PEITC, 88.7 ± 2.2% and 9.9 ± 1.9% of the dose appeared in the urine and feces, respectively, during 48 h; however, rats given [14C]PHITC excreted 7.2 ± 0.8% of the dose of14C in urine and 47.4 ± 14.0% in the feces. Higher effective doses of PHITC in the lungs and other organs may be the basis, in part, for its greater potency as a chemopreventive agent.

Footnotes

  • Send reprint requests to: Dr. C. C. Conaway, Division of Carcinogenesis and Molecular Epidemiology, American Health Foundation, 1 Dana Road, Valhalla, NY 10595.

  • ↵1 Present address: Mitsui Norin Co., Ltd., Food Research Laboratories, 233 Miyabara, Fujieda City, Shizouka 426-01, Japan.

  • This study was supported by Grant CA46535 from the National Cancer Institute. This article is number 29 in the series “Dietary Inhibitors of Chemical Carcinogenesis”.

  • Abbreviations used are::
    PEITC
    phenethyl isothiocyanate
    ITC
    isothiocyanate
    PHITC
    6-phenylhexyl isothiocyanate
    PEITC-NAC
    N-acetylcysteine conjugate of PEITC
    PHITC-NAC
    N-acetylcysteine conjugate of PHITC
    GSH
    glutathione
    NNK
    4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone
    AUC
    area under the concentration-time curve
    T1/2a
    half-life of absorption
    T1/2e
    half-life of elimination
    Tmax
    time at maximum concentration
    Cmax
    maximum ITC concentration in tissue
    KCN
    potassium cyanide
    TLC
    thin layer chromatography
    HPLC
    high-pressure liquid chromatography
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 27 (1)
Drug Metabolism and Disposition
Vol. 27, Issue 1
1 Jan 1999
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Research ArticleArticle

Disposition and Pharmacokinetics of Phenethyl Isothiocyanate and 6-Phenylhexyl Isothiocyanate in F344 Rats

C. Clifford Conaway, Ding Jiao, Toshiyuki Kohri, Leonard Liebes and Fung-Lung Chung
Drug Metabolism and Disposition January 1, 1999, 27 (1) 13-20;

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Research ArticleArticle

Disposition and Pharmacokinetics of Phenethyl Isothiocyanate and 6-Phenylhexyl Isothiocyanate in F344 Rats

C. Clifford Conaway, Ding Jiao, Toshiyuki Kohri, Leonard Liebes and Fung-Lung Chung
Drug Metabolism and Disposition January 1, 1999, 27 (1) 13-20;
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