SODIUM SULPHOMETHYL DERIVATIVES OF POLYMYXINS
SODIUM SULPHOMETHYL DERIVATIVES OF POLYMYXINS
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DOI：
10.1111/j.1476-5381.1967.tb01946.x
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发表时间：
1967-01-01
期刊：
影响因子：
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通讯作者：
MARTIN, AJ
中科院分区：
文献类型：
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作者：
BEVERIDGE, EG;MARTIN, AJ
电泳显示商用粘菌素磺酸钠 (CSMS) 和多粘菌素 B 甲磺酸钠 (SPBMS) 由各种组分组成，其游离氨基的磺甲基化程度可能不同。在体外，CSMS 和 SPBMS 的活性重量低于母体抗生素，但当加热中性 pH 值的溶液时，活性增加，增加与温度和加热时间有关。电泳表明磺甲基的选择性水解导致了活性的增加。这种水解在 37°C 的人血浆中发生得更快，对尿液中排泄的抗生素组分的检查表明，这种水解在体内也发生得比简单的水溶液更大程度。与 CSMS 相比，注射 SPBMS 引起严重局部疼痛和其他不良副作用的发生率很高。
Commercial colistin sulphomethate sodium (CSMS) and sodium polymyxin B methanesulfphonate (SPBMS) were shown by electrophoresis to be composed of various fractions probably differing in the degree of sulphomethylation of the free amino groups. CSMS and SPBMS were less active weight for weight than the parent antibiotics in vitro but activity increased when solutions at neutral pH were heated, the increases being related to the temperature and length of heating. Electrophoresis suggested that selective hydrolysis of sulphomethyl groups had taken place to cause these increases in activity. This hydrolysis occurred more rapidly in human plasma at 37[degree] and examination of the antibiotic fractions excreted in the urine suggested that this hydrolysis also took place in the body to a greater extent than in simple aqueous solutions. In contrast to CSMS, injection of SPBMS caused a high incidence of severe localized pain and other undesirable side effects.