Bisorbicillinol inhibits Lyn tyrosine kinase for allergic response on RBL-2H3 cells

  • Bioorg Med Chem Lett. 2019 Mar 15;29(6):832-835. doi: 10.1016/j.bmcl.2019.01.019.
Kouichi Sugaya  1 ,  Takehito Terajima  1 ,  Aika Takahashi  1 ,  Jun-Ichi Onose  2 ,  Naoki Abe  3
Affiliations
  • 1. Department of Nutritional Science and Food Safety, Faculty of Applied Bio-Science, Tokyo University of Agriculture, 1-1-1 Sakuragaoka, Setagaya-ku, Tokyo 156-8502, Japan.
  • 2. Department of Nutritional Science and Food Safety, Faculty of Applied Bio-Science, Tokyo University of Agriculture, 1-1-1 Sakuragaoka, Setagaya-ku, Tokyo 156-8502, Japan. Electronic address: [email protected].
  • 3. Department of Nutritional Science and Food Safety, Faculty of Applied Bio-Science, Tokyo University of Agriculture, 1-1-1 Sakuragaoka, Setagaya-ku, Tokyo 156-8502, Japan. Electronic address: [email protected].
PMID: 30711393 DOI: 10.1016/j.bmcl.2019.01.019
Abstract

Bisorbicillinol, which is isolated from Trichoderma sp. USF2690, is an inhibitor of β-hexosaminidase release and tumor necrosis factor (TNF)-α, and Interleukin (IL)-4 secretion from rat basophilic leukemia (RBL-2H3) cells, with IC50 values of 2.8 μM, 2.9 μM and 2.8 μM respectively. We showed that the inhibitory mechanism of β-hexosaminidase release and TNF-α secretion involved inhibition of Lyn, a tyrosine kinase. The inhibitory activities of bisorbicillinol indicate that this compound is a new candidate anti-allergic agent.

Keywords
Bisorbicillinol; Lyn; RBL-2H3 cells; TNF-α; β-Hexosaminidase.