4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 29, Issue 6, Pages 832-835

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.01.019

Keywords

Bisorbicillinol; Lyn; beta-Hexosaminidase; TNF-alpha; RBL-2H3 cells

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

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