产品
编 号:F465813
分子式:C43H51N3O11
分子量:785.88
产品类型
结构图
CAS No: 80621-81-4
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产品详情
生物活性:
Rifaximin, a gastrointestinal-selective antibiotic, binds the β-subunit of bacterial DNA-dependent RNA polymerase, resulting in inhibition of bacterial RNA synthesis. Rifaximin susceptibility is higher against Gram-positive strains (MIC: 0.03-5 mg/ml) compared to Gram-negative bacteria (MIC: 8-50 mg/mL).
体内研究:
Rifaximin administration (30 or 50 mg/kg/day) increases survival rates of colitic mice and reduces colitis severity by improvement of wasting syndrome, histologic scores, decrease in colon IL-2, IL-12, IFN-gamma and TNF-alpha (protein and mRNA) levels, and diminishes colon myeloperoxidase (MPO) activity.Animal Model:Balb/c mice (6–8 weeks old) bearing 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis
Dosage:10, 30 and 50 mg/kg/day
Administration:Orally, p.o. daily for 7 days
Result:Significantly reduced TNBS induced colitis at the dose of 30 and 50 mg/kg, but not 10 mg/kg. A 7-day course of 30 and 50 mg/kg resulted in an almost complete tissue protection.
体外研究:
Rifaximin has a good inhibitory activity against Staphylococcus, Streptococcus, Enterococcus, Escherichia coli, Shigella, Salmonella, Bacillus cereus, Moraxella catarrhalis, Haemophilus influenzae, Haemophilus ducreyi, Bacteroides bivius-disiens, Gardnerella vaginalis, Lactobacillus spp.,Mobiluncus spp.,Neisseria gonorrhoeae, Pseudomonas andAcinetobacter . Rifaximin rarely causes side effects.Rifaximin (0.1, 1.0 and 10.0 μM) causes significant and concentration-dependent reduction of cell proliferation, cell migration and PCNA expression in the Caco-2 cells vs. untreated cells. Rifaximin (0.1-10 μM) downregulates Akt/mTOR and p38MAPK/NF-κB pathways through a PXR-dependent mechanism.