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利帕林 E 对细菌和酵母菌株的致死作用机制。

Mechanism of the lethal effect of Riparin E against bacterial and yeast strains.

机构信息

Department of Parasitology and Microbiology, Federal University of Piauí, Teresina, Piauí, Brazil.

Department of Pharmacy, Federal University of Piauí, Teresina, Piauí, Brazil.

出版信息

Microb Pathog. 2021 Aug;157:104968. doi: 10.1016/j.micpath.2021.104968. Epub 2021 May 21.

Abstract

Riparins are alkamides naturally found in the fruits of Aniba riparia (Nees) Mez, but currently synthetic molecules as Riparin E (Rip-E) can be obtained. Potential biological of Rip-E as schistosomicidal agent against Schistosoma mansoni worms, as well as against Staphylococcus aureus strains has already been described. However, the mechanism of action related to antimicrobial activity of Rip-E against bacterial or fungi species has not yet been reported. This study had as objective to evaluate the Rip-E antimicrobial activity against Gram-positive and Gram-negative bacteria, as well as against yeast species of clinical importance. Minimal inhibitory concentrations of the compound against bacterial and yeast strains were determined by microdilution method. To verify if a possible lethal effect caused by Rip-E were related to plasma membrane damage, microbial cells treated with Rip-E were stained with 7-aminoactinomycin D (7-AAD) and analyzed by flow cytometry. Rip-E showed a bactericide effect against Gram-positive species S. aureus and S. epidermidis, as well as, against Gram-negative species Escherichia coli and Salmonella enterica Typhimurium, but was inactive against Pseudomonas aeruginosa. Moreover, Rip-E showed activity against fungi species Candida albicans and C. tropicalis. S. aureus, E. coli and C. albicans cells treated with Rip-E were marked with 7-aminoactinomycin D (7-AAD) indicating that Rip-E can cause plasma membrane damage, acting as a potential microbicide agent for prevention or treatment of infectious diseases.

摘要

里帕林是一种天然存在于 Aniba riparia (Nees) Mez 果实中的酰胺,目前也可以合成里帕林 E(Rip-E)。Rip-E 作为一种杀血吸虫药物,不仅对曼氏血吸虫成虫有效,对金黄色葡萄球菌菌株也有一定的作用。然而,关于 Rip-E 对细菌或真菌的抗菌活性的作用机制尚未见报道。本研究旨在评估 Rip-E 对革兰氏阳性和革兰氏阴性细菌以及临床重要的酵母的抗菌活性。采用微量稀释法测定化合物对细菌和酵母菌株的最小抑菌浓度。为了验证 Rip-E 可能引起的致死作用是否与细胞膜损伤有关,用 Rip-E 处理微生物细胞并用 7-氨基放线菌素 D(7-AAD)染色,然后通过流式细胞术进行分析。Rip-E 对革兰氏阳性菌金黄色葡萄球菌和表皮葡萄球菌以及革兰氏阴性菌大肠杆菌和肠炎沙门氏菌 Typhimurium 具有杀菌作用,但对铜绿假单胞菌无效。此外,Rip-E 对真菌白色念珠菌和热带假丝酵母也具有活性。用 Rip-E 处理的金黄色葡萄球菌、大肠杆菌和白色念珠菌细胞用 7-氨基放线菌素 D(7-AAD)标记,表明 Rip-E 可引起细胞膜损伤,可作为预防或治疗感染性疾病的潜在杀菌剂。

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