1. Academic Validation
  2. Evaluation of Inhibitory Activities of UK-2A, an Antimycin-Type Antibiotic, and Its Synthetic Analogues against the Production of Anti-inflammatory Cytokine IL-4

Evaluation of Inhibitory Activities of UK-2A, an Antimycin-Type Antibiotic, and Its Synthetic Analogues against the Production of Anti-inflammatory Cytokine IL-4

  • J Nat Prod. 2018 Nov 26;81(11):2590-2594. doi: 10.1021/acs.jnatprod.8b00559.
Yoshinosuke Usuki 1 Saho Ishii 1 Minako Ijiri 1 Ken-Ichi Yoshida 1 Tetsuya Satoh 1 Satoru Horigome 2 Izumi Yoshida 2 Takashi Mishima 2 Ken-Ichi Fujita 3
Affiliations

Affiliations

  • 1 Department of Chemistry, Graduate School of Science , Osaka City University , 3-3-138 Sugimoto , Sumiyoshi, Osaka 558-8585 , Japan.
  • 2 Saito Laboratory , Japan Food Research Laboratories , 4-41 Saito-asagi 7-chome , Ibaraki-shi, Osaka 567-0085 , Japan.
  • 3 Department of Biology, Graduate School of Science , Osaka City University , 3-3-138 Sugimoto , Sumiyoshi, Osaka 558-8585 , Japan.
Abstract

The inhibitory activities of the antimycin-class Antibiotics UK-2A, antimycin A, and splenocin B against the production of anti-inflammatory cytokine IL-4, which is related to IgE-mediated allergic responses in rat basophilic leukemia (RBL-2H3) cells, were evaluated. Although antimycin A and splenocin B showed cytotoxicity at concentrations at which IL-4 release from the cells was restricted, UK-2A was found to restrict IL-4 release without cytotoxicity. Three UK-2A analogues (4-6) were then synthesized and assessed. Compound 5 restricted IL-4 release dose-dependently without cytotoxicity, and its effect was more potent than that of UK-2A.

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