Hispidol
| 中文名称 | Hispidol |
|---|---|
| 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 |
| 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 |
|---|---|
| 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) |
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.