Hispidol
中文名称 | Hispidol |
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中文同义词 | 化合物HISPIDOL |
英文名称 | 6,4''-DIHYDROXYAURONE |
英文同义词 | NSC356828;Hispidol, >98%;(Z)-Hispidol;3(2H)-Benzofuranone, 6-hydroxy-2-[(4-hydroxyphenyl)methylene]-, (2Z)-;inhibit,Hispidol,TNF Receptor,Tumor Necrosis Factor Receptor,TNFR,Inhibitor;6,4''-DIHYDROXYAURONE;(2Z)-6-hydroxy-2-[(4-hydroxyphenyl)methylidene]-2,3-dihydro-1-benzofuran-3-one |
CAS号 | 5786-54-9 |
分子式 | C15H10O4 |
分子量 | 254.24 |
EINECS号 | |
相关类别 | Aurones |
Mol文件 | 5786-54-9.mol |
结构式 |
Hispidol 性质
熔点 | 286-288 °C |
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沸点 | 523.8±50.0 °C(Predicted) |
密度 | 1.489±0.06 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | DMF:50mg/mL; DMSO:25mg/mL;乙醇:10mg/mL |
形态 | 固体 |
酸度系数(pKa) | 7.59±0.20(Predicted) |
颜色 | 浅黄至黄色 |
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.
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.