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具有重要医学意义的多重耐药菌的利帕林 I、II 和 III 的抗菌活性和生物膜抑制作用及超微结构变化。

Antimicrobial activity and biofilm inhibition of riparins I, II and III and ultrastructural changes in multidrug-resistant bacteria of medical importance.

机构信息

Laboratory of Molecular and Cellular Biology, Department of Parasitology, Institute Aggeu Magalhães - FIOCRUZ/PE (Av. Prof. Moraes Rego, S/n - Cidade Universitária, Recife/PE, 50670-420, Brazil.

Laboratory of Molecular and Cellular Biology, Department of Parasitology, Institute Aggeu Magalhães - FIOCRUZ/PE (Av. Prof. Moraes Rego, S/n - Cidade Universitária, Recife/PE, 50670-420, Brazil.

出版信息

Microb Pathog. 2020 Dec;149:104529. doi: 10.1016/j.micpath.2020.104529. Epub 2020 Sep 30.

Abstract

Natural products have been used to treat various infections; however, the development of antimicrobials has made natural products in disuse. Riparin I, II and III are natural alkamide isolated from Aniba riparia (Ness) Mez (Lauraceae), that exhibit economic importance and it is used in traditional medicine, and popularly known as "louro". This study investigated the cytotoxicity, antimicrobial and antibiofilm activity, and ultrastructural changes in vitro by riparins I, II and III in Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii and Pseudomonas aeruginosa. We analyzed the cytotoxicity by MTT assay in Vero cells and hemolytic action verified in human erythrocytes. The antimicrobial activity was determined by microdilution in broth against ATCC strains, identifying the susceptible species. Subsequently, only the MDR isolates of sensitive bacterial species were evaluated regarding its biofilm formation and ultrastructural changes. Riparin I presented low cytotoxicity and hemolytic percentage ranging from of 9.01%-12.97%. Only the riparin III that showed antimicrobial activity against MDR clinical isolates, and significant reduction in biofilm formation in S. aureus. Moreover, the riparin III promoted ultrastructural changes in bacterial cells, such as elongated cellular without bacterial septum, cells with a rugged appearance on the cell surface and cytoplasmic material extravasation. As has been noted riparin III has an inhibitory potential against biofilm formation in S. aureus, besides having antimicrobial activity and promoting ultrastructural changes in MDR clinical isolates. Thus, riparin III is an interesting alternative for further studies aiming to develop new therapeutic options.

摘要

天然产物一直被用于治疗各种感染;然而,由于抗菌药物的发展,天然产物已经不再被使用。Riparin I、II 和 III 是从 Aniba riparia(Ness)Mez(Lauraceae)中分离出来的天然酰胺,具有经济重要性,用于传统医学,俗称“劳罗”。本研究调查了 riparins I、II 和 III 对金黄色葡萄球菌、肺炎克雷伯菌、鲍曼不动杆菌和铜绿假单胞菌的体外细胞毒性、抗菌和抗生物膜活性以及超微结构变化。我们通过 MTT 测定法在 Vero 细胞中分析细胞毒性,并在人红细胞中验证溶血作用。通过肉汤微量稀释法测定抗菌活性,以确定对 ATCC 株的敏感物种。随后,仅对敏感细菌种的 MDR 分离株评估其生物膜形成和超微结构变化。Riparin I 的细胞毒性和溶血百分比范围为 9.01%-12.97%,均较低。只有 riparin III 对 MDR 临床分离株表现出抗菌活性,并显著降低了金黄色葡萄球菌的生物膜形成。此外,riparin III 还导致细菌细胞的超微结构发生变化,例如细胞伸长但没有细菌隔膜、细胞表面粗糙和细胞质物质外渗。正如所指出的,riparin III 对金黄色葡萄球菌生物膜形成具有抑制潜力,此外还具有抗菌活性并促进 MDR 临床分离株的超微结构变化。因此,riparin III 是进一步研究开发新治疗方法的有趣选择。

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