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瑞莫拉宁(A16686或MDL62198)的体外评估。一种潜在可用于局部给药的新型缩酚酸肽复合物。

In vitro evaluation of ramoplanin (A16686 or MDL62198). A new depsipeptide complex for potential topical use.

作者信息

Jones R N, Barry A L

机构信息

Clinical Microbiology Institute, Tualatin, Oregon 97062.

出版信息

Diagn Microbiol Infect Dis. 1989 May-Jun;12(3):279-82. doi: 10.1016/0732-8893(89)90029-1.

Abstract

Ramoplanin, a new depsipeptide complex, was found to be 4- to 8-fold more active than vancomycin against all Gram-positive species (500 strains). Similarly, ramoplanin was both more active and had an additional spectrum compared to mupirocin (formerly pseudomonic acid) against Bacillus spp., Corynebacterium jeikeium, enterococci and Listeria monocytogenes. Mupirocin-resistant Staphylococcus spp. strains (less than 1%) were identified in these organisms collected from over 40 medical centers in the United States. These strains (S. capitis and S. saprophyticus) were susceptible to ramoplanin at 0.25 micrograms/ml or less. The three tested antimicrobial agents were not effective against Gram-negative organisms (20 species tested). Ramoplanin was bactericidal and MICs were not adversely influenced by high (greater than or equal to 10(7) CFU/ml) inoculum concentrations. Because ramoplanin has previously shown promise as a topical drug, these in vitro results further substantiate its wide spectrum, potency, and potential clinical usefulness as mupirocin-resistant staphylococci and other Gram-positive species become more prevalent.

摘要

雷莫拉宁是一种新型缩肽复合物,发现其对所有革兰氏阳性菌(500株)的活性比万古霉素高4至8倍。同样,与莫匹罗星(以前称为假单胞菌酸)相比,雷莫拉宁对芽孢杆菌属、杰氏棒状杆菌、肠球菌和单核细胞增生李斯特菌的活性更高且抗菌谱更广。在美国40多个医疗中心收集的这些微生物中,鉴定出了耐莫匹罗星的葡萄球菌属菌株(不到1%)。这些菌株(头状葡萄球菌和腐生葡萄球菌)对浓度为0.25微克/毫升或更低的雷莫拉宁敏感。这三种测试抗菌剂对革兰氏阴性菌(测试了20种)无效。雷莫拉宁具有杀菌作用,且高接种浓度(大于或等于10⁷CFU/毫升)对其最低抑菌浓度没有不利影响。由于雷莫拉宁以前已显示出作为局部用药的前景,随着耐莫匹罗星葡萄球菌和其他革兰氏阳性菌变得更加普遍,这些体外研究结果进一步证实了其广谱性、效力以及潜在的临床实用性。

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