一种季铵化硼二吡咯对葡萄球菌菌株的抗菌活性。

Antimicrobial activity of a quaternized BODIPY against Staphylococcus strains.

作者信息

Aydın Tekdaş Duygu, Viswanathan Geetha, Zehra Topal Sevinc, Looi Chung Yeng, Wong Won Fen, Min Yi Tan Grace, Zorlu Yunus, Gürek Ayşe Gül, Lee Hong Boon, Dumoulin Fabienne

机构信息

Gebze Technical University, Department of Chemistry, P.O Box 141, 41400 Gebze Kocaeli, Turkey.

Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia.

出版信息

Org Biomol Chem. 2016 Mar 7;14(9):2665-70. doi: 10.1039/c5ob02477c.

DOI:10.1039/c5ob02477c

PMID:26831779

Abstract

A novel BODIPY derivative was designed for biomedical applications. Its mono-quaternized structure ensured its water-solubility and suitable amphiphilicity. Showing no singlet oxygen generation to avoid damage to healthy cells, this new derivative proved to be an extremely promising antimicrobial agent, with activity equal or superior to ampicillin against MRS Staphylococcus strains with no short-term resistance issue. Its activity against MSS Staphylococcus strains was largely superior to those of ampicillin and reached the activity of vancomycin against MSS S. epidermidis. This latter result is in particular extremely promising for the treatment of hospital-acquired infections. Also the fluorescence properties of BODIPY allowed imaging of the uptake.

摘要

一种新型的BODIPY衍生物被设计用于生物医学应用。其单季铵化结构确保了它的水溶性和合适的两亲性。这种新衍生物不会产生单线态氧，从而避免对健康细胞造成损害，事实证明它是一种极有前景的抗菌剂，其活性与氨苄西林相当或优于氨苄西林，对耐甲氧西林葡萄球菌菌株无短期耐药问题。它对甲氧西林敏感葡萄球菌菌株的活性大大优于氨苄西林，达到了万古霉素对表皮葡萄球菌的活性。后一个结果对于医院获得性感染的治疗尤其有前景。此外，BODIPY的荧光特性有助于对摄取情况进行成像。