2. Academic Validation
  3. Bisorbicillinol inhibits Lyn tyrosine kinase for allergic response on RBL-2H3 cells

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

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: j1onose@nodai.ac.jp.
  • 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: abe@nodai.ac.jp.
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.

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