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Hispidol

CAS No. : 5786-54-9

MCE 国际站：Hispidol

产品活性：Hispidol ((Z)-Hispidol) 具有研究炎症性肠病的潜力，能够抑制 TNF-α 诱导的单核细胞对结肠上皮细胞的粘附，IC₅₀ 值为 0.50 µM。

研究领域：Apoptosis

作用靶点：TNF Receptor

In Vitro: Hispidol shows potent inhibitory effect (>70%) on the TNF-α-induced adhesion of monocytes to colon epithelial cells, which is one of the hallmark events leading to inflammatory bowel disease (IBD). Hispidol shows strong inhibitory activities against TNF-α-induced monocytic-colonic epithelial cell adhesion as well as LPS-induced TNF-α expression, is as an excellent candidate for IBD drug development. This inhibition of TNF-α expression by hispidol corresponds to the additional inhibitory activity against AP-1 transcriptional activity, which is another transcription factor required for high level TNF-α expression.

In Vivo: The oral administration of hispidol suppresses significantly and dose-dependently TNBS-induced rat colitis. Oral administration of hispidol suppresses TNBS-induced colitis in a dose-dependent manner. There is a significant recovery in body weight decrease and colon tissue edematous inflammation. A higher dose (30 mg/kg) of hispidol shows a similar recovery effect to that of 300 mg/kg sulfasalazine. In the colon tissues, TNBS induces a dramatic increase in the level of MPO, a biochemical marker of inflammation, which is suppressed significantly by hispidol in a dose-dependent manner.

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