产品
编 号:F548210
分子式:C26H44CaO9
分子量:520.66
产品类型
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CAS No: 104486-81-9
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生物活性:
Mupirocin (BRL-4910A, Pseudomonic acid) calcium is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin calcium apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis.
体内研究:
MRSA: Meticillin-resistant Staphylococcus aureusMupirocin (BRL-4910A, Pseudomonic acid) calcium is well absorbed after oral and parenteral administration but serum antibiotic concentrations were short-lived as a result of extensive degradation to the antibacterially inactive metabolite, monic acid A.Mupirocin calcium (2% ointment; external administration; twice daily; 3-6 d) decreases the total bacterial loads in the skin lesions with either topical treatment.Mupirocin calcium (2% ointment; external administration; 4 d) alleviates MRSA-infected pressure ulcers in mice.Mupirocin calcium (100 mg/mL; s.c.; 7 d) exerts prevention efficacy against vascular prosthetic graft infection due to Staphylococcus epidermidis.Animal Model:MRSA skin infection model in mice (10-12 weeks old)
Dosage:2% ointment
Administration:External administration; twice daily; 3-6 days
Result:Reduced the total bacterial loads in the skin lesions, and decreased by 2.0, 5.1 log10 CFU on day 3 and 6, respectively.
Animal Model:Diabetic pressure ulcer mouse model (33.2-39.2 g)
Dosage:2% ointment
Administration:External administration; 4 days
Result:Resulted less superficial mats of bacterial colonies, and improved histopathology evaluation.
Animal Model:Adult male Wistar rats (weight 275-325 g)
Dosage:Impregnated with 100 μg of mupirocin/mL; segments:1.5 cm *1 cm2
Administration:Subcutaneous implantation; 7 days
Result:Resulted in preventing S. epidermidis infection of the graft in a rat model with spontaneously bound to collagen-sealed Dacron grafts.
体外研究:
Mupirocin (BRL-4910A, Pseudomonic acid) calcium (0-100 μM; 48 h) shows antibacterial effect against staphylococci, streptococci and certain gram-negative bacteria, with MIC values range from 0.06-0.25 μg/mL (MIC50 =0.12 μg/mL, MIC90 =0.25 μg/mL).Mupirocin calcium is highly bound (95% bound) to human serum protein, thus results in activity inhibition in the presence of human serum.Mupirocin calcium apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis.Mupirocin calcium (2% ointment) reduces pro-inflammatory cytokines IL-1β and IL-17 level, decreases tumor necrosis factor-alpha (TNF-α) expression, and increases the leavel of vascular endothelial growth factor (VEGF).Mupirocin calcium inhibits MS (S. epidermidis ATCC 12228), MR (S. epidermidis (Se56-99)), and VIR (S. epidermidis (Se43-98)) with MICs of 0.25, 1.26, 1.59 mg/L.Note: MIC, the minimum inhibition concentration.