Rifampin|13292-46-1|安捷凯

Background

Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens.

Rifampicin (100 mg/mL) can block the functional activity of P-glycoprotein. Rifampicin is not a substract for P-glycoprotein. The mechanism of rifampicin resistance is unassociated with the functional activity of P-glycoprotein[3].

Rifampicin (200, 400 mg/kg) can induce fatty liver at high concentration[1]. Rifampicin (30 mg/kg, i.p.) treatment of S464P biofilms in vivo results in a slight decline, but earlier rebinds in bioluminescence from these catheters compared with the parental signal, whereas rifampicin has no affect on bioluminescence in mice infected with mutant H481Y[2].

利福平是一种对细菌病原体具有强大和广谱抗生素作用的药物。

利福平（100 mg/mL）可阻断P-糖蛋白的功能活性。利福平不是P-糖蛋白的底物。利福平耐药机制与P-糖蛋白的功能活性无关[3]。

利福平（200，400 mg/kg）可以诱导高浓度脂肪肝[1]。利福平（30 mg/kg，i.p.）处理S464P生物膜后，这些导管中的生物荧光信号略有下降，但比父母信号更早地重新绑定，而利福平对感染突变体H481Y的小鼠的生物荧光信号没有影响[2]。

参考文献:
[1]. Piriou A, et al. Fatty liver induced by high doses of rifampicin in the rat: possible relation with an inhibition of RNA polymerases in eukariotic cells. Arch Toxicol Suppl. 1979;(2):333-7.
[2]. Yu J, et al. Monitoring in vivo fitness of rifampicin-resistant Staphylococcus aureus mutants in a mouse biofilm infection model. J Antimicrob Chemother. 2005 Apr;55(4):528-34. Epub 2005 Mar 2.
[3]. Erokhina MV, et al. [In vitro development of rifampicin resistance in the epithelial cells]. Probl Tuberk Bolezn Legk. 2006;(8):58-61.

Protocol

Animal experiment:

Briefly, 1 cm Teflon catheter (14-gauge) carrying 104 cfu S. aureus, either the parental strain Xen 29 or the RifR mutants S464P or H481Y, are implanted subcutaneously in groups of nine mice per strain. One catheter segment is inserted on each side of each animal. Six days after the implantation of the catheters, five mice from each group are treated with rifampicin at 30 mg/kg intraperitoneally in 0.1 mL saline, twice daily for four consecutive days. The remaining four mice in each group are left untreated as controls. At various time points during the infection, the mice are anaesthetized using a constant flow of 1.5% isoflurane from the IVIS? manifold, and imaged using an IVIS? Image System 100 Series. The bioluminescent signals (photons/s) emitted from the mice are analysed using LivingImage? software and plotted over the course of infection. The mice are sacrificed 20 days after infection (11 days after final rifampicin treatment). The catheters are surgically removed and the bacteria are detached by sonication for determination of bacterial burdens on the catheters.

参考文献:

[1]. Piriou A, et al. Fatty liver induced by high doses of rifampicin in the rat: possible relation with an inhibition of RNA polymerases in eukariotic cells. Arch Toxicol Suppl. 1979;(2):333-7.
[2]. Yu J, et al. Monitoring in vivo fitness of rifampicin-resistant Staphylococcus aureus mutants in a mouse biofilm infection model. J Antimicrob Chemother. 2005 Apr;55(4):528-34. Epub 2005 Mar 2.
[3]. Erokhina MV, et al. [In vitro development of rifampicin resistance in the epithelial cells]. Probl Tuberk Bolezn Legk. 2006;(8):58-61.

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Rifampin

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Background

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