Kamurai Bridget, Mombeshora Molly, Mukanganyama Stanley
Department of Biochemistry, University of Zimbabwe, P.O. Box MP 167 Mt. Pleasant, Harare, Zimbabwe.
Int J Microbiol. 2020 Sep 29;2020:8885338. doi: 10.1155/2020/8885338. eCollection 2020.
Increasing cases of multidrug-resistant pathogens have evolved into a global health crisis. ESKAPE group of bacteria are associated with antibiotic resistance, and infections caused by these pathogens result in high mortality and morbidity. However, synthesis of antibiotics is expensive and time-consuming since the development of a new drug has to go through several clinical trials. Repurposing of old drugs for the treatment of antimicrobial resistant pathogens has been explored as an alternative strategy in the field of antimicrobial drug discovery. Ten non-antimicrobial compounds were screened for antibacterial activity on two ESKAPE organisms, and . The drugs used in this study were amodiaquine an antimalarial drug, probenecid used to prevent gout, ibuprofen a painkiller, 2-amino-5-chlorobenzaxazole used as a tool for assessing hepatic cytochrome P450 activity in rodents, ellargic acid an antioxidant, quercetin an antioxidant and anti-inflammatory drug, N-N diacryloylpiperazine used to crosslink polyacrylamide gel in 2D-protein electrophoresis, epicatechin an antioxidant and antiviral drug, curcumin an anticancer drug, and quinine an antimalarial drug. Antibacterial susceptibility tests were carried out for the 10 compounds. Curcumin exhibited the most potent antimicrobial activity against both bacteria, with MICs of 50 g/ml and 100 g/ml for and , respectively. Ellargic acid was found to have an MIC of 100 g/ml against Curcumin caused protein and nucleic acid leakage from the bacterial cell membrane in both bacterial species. When curcumin was combined with ciprofloxacin, it was found to enhance the antibacterial effects of ciprofloxacin. The combination with ciprofloxacin reduced the MIC for ciprofloxacin from 0.5 g/ml to 0.0625 g/ml on and 0.25 g/ml to 0.0625 g/ml on . The results obtained show that curcumin has antibacterial activity against and and may enhance the antibacterial activity of ciprofloxacin.
多重耐药病原体病例的不断增加已演变成一场全球健康危机。ESKAPE 组细菌与抗生素耐药性有关,由这些病原体引起的感染会导致高死亡率和高发病率。然而,抗生素的合成既昂贵又耗时,因为一种新药的开发必须经过多项临床试验。在抗微生物药物发现领域,探索将旧药重新用于治疗抗微生物耐药病原体已成为一种替代策略。对十种非抗菌化合物进行了针对两种 ESKAPE 微生物的抗菌活性筛选。本研究中使用的药物有抗疟药阿莫地喹、用于预防痛风的丙磺舒、止痛药布洛芬、用作评估啮齿动物肝细胞色素 P450 活性工具的 2-氨基-5-氯苯并恶唑、抗氧化剂鞣花酸、抗氧化剂和抗炎药槲皮素、用于二维蛋白质电泳中交联聚丙烯酰胺凝胶的 N-N 二丙烯酰哌嗪、抗氧化剂和抗病毒药表儿茶素、抗癌药姜黄素以及抗疟药奎宁。对这 10 种化合物进行了抗菌药敏试验。姜黄素对两种细菌均表现出最有效的抗菌活性,对 [具体细菌 1] 和 [具体细菌 2] 的最低抑菌浓度分别为 50 μg/ml 和 100 μg/ml。发现鞣花酸对 [具体细菌 1] 的最低抑菌浓度为 100 μg/ml。姜黄素导致两种细菌的细菌细胞膜出现蛋白质和核酸泄漏。当姜黄素与环丙沙星联合使用时,发现它增强了环丙沙星的抗菌效果。与环丙沙星联合使用使环丙沙星对 [具体细菌 1] 的最低抑菌浓度从 0.5 μg/ml 降至