Relationship between Chemical Structure and Activity. II. Influences of Isomers in Dichlorobenzene, Trichlorobenzene, and Tetrachlorobenzene on the Activities of Drug-Metabolizing Enzymes

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概要

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• Hepatic constituents and the cytochrome contents in addition to activities of drugmetabolizing enzymes and δ-aminolevulinic acid (δ-ALA) synthetase were examined in rats treated with each isomer of dichlorobenzene (DCB), trichlorobenzene (TRCB) and tetrachlorobenzene (TECB) in an oral dose of 250 mg/kg once daily for 3 days. 1) In the studies on DCB-isomers, activities of aminopyrine demethylase and aniline hydroxylase were enhanced markedly by treatment with m-DCB, whereas cytochrome content was not altered significantly by treatment with any DCB-isomers. δ-ALA synthetase activity was enhanced 63,32 and 42% by treatment with o-, m- and p-DCB, respectively, but these enhancement were not paralleled with the changes in cytochrome P-450 content. 2) In the administration of TRCB-isomers, enzyme activities were enhanced markedly by treatment with 1,2,4-TRCB. Cytochrome P-450 content was also increased by treatment with 1,2,4-TRCB, and this increase could be partly related with the enhancement of δ-ALA synthetase activity. 3) By treatment with all TECB-isomers, activity of aminopyrine demethylase was enhanced, whereas aniline hydroxylase was not altered. Cytochrome P-450 content was increased by treatment with all TECB-isomers. 4) Microsomal protein content was increased with all isomers of DCB, TRCB and TECB treatment. Microsomal Pi was increased markedly 36,70 and 91% by treatment with m-DCB, 1,2,4-TRCB and 1,2,3,5-TECB, respectively. Hepatic glycogen content was decreased only by 1,2,3,5-TECB, but triglyceride content was not altered. 5) The spectral change induced by substrate-cytochrome P-450 binding was characterized by type I in each treatment, but conversion of the type occurred in treatment with 1,2,4,5-TECB in high concentration of 1 mM.

• 社団法人日本薬学会の論文
• 1975-04-25

著者

• 新垣 光雄

  長崎県立女子短期大学

• 井手口 勝美

  Faculty of Pharmaceutical Sciences, Nagasaki University

• 岩崎 一秀

  Faculty of Pharmaceutical Sciences, Nagasaki University

• 新垣 光雄

  Faculty of Pharmaceutical Sciences, Nagasaki University

• 岩崎 一秀

  Faculty Of Pharmaceutical Sciences Nagasaki University

• 井手口 勝美

  Faculty Of Pharmaceutical Sciences Nagasaki University

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