Dow College of Biotechnology, Dow University of Health Sciences, Karachi, Pakistan / Department of Pharmacology, Dow College of Pharmacy, Dow University of Health Sciences, Karachi, Pakistan.
Dow College of Biotechnology, Dow University of Health Sciences, Karachi, Pakistan.
Pak J Pharm Sci. 2020 Sep;33(5(Supplementary)):2331-2339.
Emergence and spread of multidrug resistant (MDR) Staphylococcus aureus strains is becoming major challenge in treatment of soft tissue infections. This study aimed to explore antimicrobial and synergistic antimicrobial potential of three commercially available thiazoline derivatives (2-amino-2-thiazoline, 2-thiazoline-2-thiol and 2-acetyl-2-thiazoline) against MDR Staphylococcus aureus strains isolated from abscess drainage samples (n=20). MDR Staphylococcus aureus isolates were identified by Kirby-Bauer disk diffusion assay and were further subjected to molecular identification by 16srRNA amplification and DNA sequencing. Minimum Inhibitory Concentration (MIC) values of test compounds and antibiotics (0.25-512μg/mL) were measured and subsequently, synergism assay was performed to calculate Fractional Inhibitory Concentration (FIC) index. Out of twenty Staphylococcus aureus isolates, sixteen (80%) were found to be MDR whereas four (20%) were Non-MDR. Moxifloxacin and vancomycine were found most effective antibiotics, inhibiting 100% (n=20) and 95% (n=19) strains respectively. Antimicrobial activity of 2-amino-2-thiazoline (MIC: 32μg/mL), 2-thiazoline-2-thiol (MIC: 64μg/mL) and 2-acetyl-2-thiazoline (MIC: 32μg/mL) was found significant against all ten tested MDR strains. Synergistic combinations of thiazoline derivatives with test antibiotics reduced MIC values significantly. Therefore, combination of tested thiazoline derivatives with antibiotics could be used as alternative therapeutic approach to treat soft tissue infections caused by MDR Staphylococcus aureus after further pre-clinical and clinical studies.
多药耐药(MDR)金黄色葡萄球菌菌株的出现和传播对软组织感染的治疗构成了重大挑战。本研究旨在探索三种市售噻唑啉衍生物(2-氨基-2-噻唑啉、2-噻唑啉-2-硫醇和 2-乙酰基-2-噻唑啉)对从脓肿引流样本中分离的 MDR 金黄色葡萄球菌菌株的抗菌和协同抗菌潜力(n=20)。MDR 金黄色葡萄球菌分离株通过 Kirby-Bauer 圆盘扩散试验鉴定,并通过 16srRNA 扩增和 DNA 测序进一步进行分子鉴定。测试化合物和抗生素(0.25-512μg/mL)的最小抑菌浓度(MIC)值进行测量,随后进行协同作用测定以计算部分抑菌浓度(FIC)指数。在二十株金黄色葡萄球菌分离株中,有十六株(80%)被鉴定为 MDR,而有四株(20%)为非 MDR。莫西沙星和万古霉素被发现是最有效的抗生素,分别抑制了 100%(n=20)和 95%(n=19)的菌株。2-氨基-2-噻唑啉(MIC:32μg/mL)、2-噻唑啉-2-硫醇(MIC:64μg/mL)和 2-乙酰基-2-噻唑啉(MIC:32μg/mL)的抗菌活性对所有十株测试的 MDR 菌株均有显著作用。噻唑啉衍生物与测试抗生素的协同组合显著降低了 MIC 值。因此,在进一步进行临床前和临床研究后,测试噻唑啉衍生物与抗生素的联合使用可以作为治疗 MDR 金黄色葡萄球菌引起的软组织感染的替代治疗方法。