Inhibitory Effects of Bis(2-aminohexyl)disulfide and Its Analogues on Polymorphonuclear Leukocyte Functions in Vitro

Yasuhiro Kohama, Masaru Okabe, Tsujikawa Kazutake, Tetsuyuki Teramoto, Norihito Murayama, Tsutomu Mimura, Takuzo Ohtani, Takefumi Matsukura, Yuzo Kayamori, Yoshiaki Katayama

研究成果: Contribution to journalArticle査読

2 被引用数 (Scopus)

抄録

Water soluble analogues of the anti-inflammatory compound, bis(2-aminopropyl)disulfide dihydrochloride (compd. I) with a butyl (II), phenyl (III), benzyl (IV) or pyrrolidinyl group (V) instead of the methyl group were synthesized, and their effects on the functions of cells related to inflammation were studied in vitro. Compounds II, III and IV showed much higher inhibitory activity than compd. I on formyl Met-Leu-Phe (FMLP)-induced O - 2 -generation of polymorphonuclear leukocytes (PMNs) and platelet aggregation. Compound II showed the strongest activity among the compounds (IC50 values: 2.6 /im).The inhibition of O2-generation of PMNs by compd. II was the most effective when FMLP was used as a stimulant rather than when phorbol myristate acetate, A-23187 and opsonized zymosan were used. However, compd. II was not an O 2-scavenger. Compounds II, III and IV significantly inhibited a series of activation processes in PMNs, chemotaxis, phagocytosis and lysosomal enzyme release at doses ranging from 10 to 100 /im. Under these doses, compds II, III and IV did not affect the histamine release from mast cells or the hemolysis of erythrocytes. These results strongly suggest that the anti-inflammatory action caused by compd. II and its analogues was at least partly due to inhibition of several functions of PMNs and platelets.

本文言語英語
ページ(範囲)414-418
ページ数5
ジャーナルChemical and Pharmaceutical Bulletin
40
2
DOI
出版ステータス出版済み - 1992

All Science Journal Classification (ASJC) codes

  • 化学 (全般)
  • 創薬

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