Colistin Methanesulfonate (sodium salt) is a polypeptide antibiotic that inhibits susceptible strains of Pseudomonas aeruginosa, with MICs of 4-16mg/l [1]. In aqueous solution, Colistin Methanesulfonate undergoes hydrolysis, forming a complex mixture of partially sulfomethylated derivatives as well as colistin, which interferes with the structure and function of the bacterial outer membrane and cytoplasmic membrane[2]. Colistin Methanesulfonate has been widely used to inhibit the growth of various multi-drug resistant bacteria both in vitro and in vivo[3].
In vitro, Colistin Methanesulfonate treatment at 0.3mM for 48 hours resulted in a significant decrease in the viability of SH-SY5Y cells, along with changes in cell morphology and the aggregation of cell debris[4]. Treatment with 256mg/l Colistin Methanesulfonate for 24 hours led to an increase in the number of mesosomes in M. tuberculosis H37Ra, accompanied by a large number of cell lysis and cell debris[5].
References:
[1] Li J, Turnidge J, Milne R, et al. In vitro pharmacodynamic properties of colistin and colistin methanesulfonate against Pseudomonas aeruginosa isolates from patients with cystic fibrosis[J]. Antimicrobial agents and chemotherapy, 2001, 45(3): 781-785.
[2] Bergen P J, Li J, Rayner C R, et al. Colistin methanesulfonate is an inactive prodrug of colistin against Pseudomonas aeruginosa[J]. Antimicrobial agents and chemotherapy, 2006, 50(6): 1953-1958.
[3] Karaiskos I, Gkoufa A, Polyzou E, et al. High-dose nebulized colistin methanesulfonate and the role in hospital-acquired pneumonia caused by gram-negative bacteria with difficult-to-treat resistance: a review[J]. Microorganisms, 2023, 11(6): 1459.
[4] Lu J, Zhu Y, Li M, et al. In Vitro Neurotoxicity Comparison: Colistimethate Induces Higher Toxicity Than Colistin via Formaldehyde Accumulation[J]. International Journal of Antimicrobial Agents, 2025: 107626.
[5] Van Breda S V, Buys A, Apostolides Z, et al. The antimicrobial effect of colistin methanesulfonate on Mycobacterium tuberculosis in vitro[J]. Tuberculosis, 2015, 95(4): 440-446.
Colistin Methanesulfonate (sodium salt)是一种多肽类抗生素，对铜绿假单胞菌敏感菌株具有抑制作用，MIC范围为4-16mg/l[1]。Colistin Methanesulfonate在水溶液中会发生水解，形成包括多粘菌素E在内的多种部分磺甲基化衍生物的复杂混合物，从而干扰细菌外膜和细胞质膜的结构与功能[2]。Colistin Methanesulfonate已广泛应用于体外和体内实验中，用于抑制多种多重耐药菌的生长[3]。
在体外，使用0.3mM的Colistin Methanesulfonate处理SH-SY5Y细胞48小时，可导致细胞活力显著下降，并伴随细胞形态改变和细胞碎片聚集[4]。用256mg/l的Colistin Methanesulfonate处理结核分枝杆菌H37Ra菌株24小时后，细菌中膜样结构数量增加，同时出现大量细胞裂解和细胞碎片[5]。