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纳米偶联万古霉素:开发抗耐万古霉素金黄色葡萄球菌(VRSA)药物的新机遇。

Nanoconjugated vancomycin: new opportunities for the development of anti-VRSA agents.

机构信息

Immunology and Microbiology Laboratory, Department of Human Physiology with Community Health, Vidyasagar University, Midnapore 721102, India.

出版信息

Nanotechnology. 2010 Mar 12;21(10):105103. doi: 10.1088/0957-4484/21/10/105103. Epub 2010 Feb 15.

DOI:10.1088/0957-4484/21/10/105103
PMID:20154376
Abstract

More than 90% of Staphylococcus strains are resistant to penicillin. In 1961 S. aureus developed resistance to methicillin (MRSA), invalidating almost all antibiotics, including the most potent beta-lactams. Vancomycin, a glycopeptide antibiotic, was used for the treatment of MRSA in 1980. Vancomycin inhibits the bio-synthesis of peptidoglycan and the assembly of NAM-NAG-polypeptide into the growing peptidoglycan chain. Vancomycin resistant S. aureus (VRSA) first appeared in the USA in 2002. Folic acid tagged chitosan nanoparticles are used as Trojan horses to deliver vancomycin into bacterial cells. These nanoparticles are biocompatible and biodegradable semisynthetic polymers. These nanosized vehicles enhance the transport of vancomycin across epithelial surfaces and show its efficient drug action, which has been understood from studies of the minimum inhibitory concentration and minimum bactericidal concentration of nanoparticles of a chitosan derivative loaded with vancomycin. Tolerance values distinctly show that vancomycin loaded into nanoconjugate is very effective and has a strong bactericidal effect on VRSA.

摘要

超过 90%的葡萄球菌菌株对青霉素具有耐药性。1961 年,金黄色葡萄球菌对甲氧西林(MRSA)产生了耐药性,几乎使所有抗生素(包括最有效的β-内酰胺类抗生素)失效。万古霉素,一种糖肽类抗生素,于 1980 年被用于治疗 MRSA。万古霉素抑制肽聚糖的生物合成以及 NAM-NAG-多肽组装到生长中的肽聚糖链中。耐万古霉素金黄色葡萄球菌(VRSA)于 2002 年首次在美国出现。叶酸标记壳聚糖纳米粒被用作运载万古霉素进入细菌细胞的特洛伊木马。这些纳米粒是生物相容和可生物降解的半合成聚合物。这些纳米尺寸的载体增强了万古霉素穿过上皮表面的运输,并显示出其有效的药物作用,这已通过研究载有万古霉素的壳聚糖衍生物纳米粒的最小抑菌浓度和最小杀菌浓度得到理解。耐受值明显表明,纳米共轭物中负载的万古霉素非常有效,对 VRSA 具有强烈的杀菌作用。

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