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来源于黄蝉 Tabebuia avellanedae 成分的抗菌萘醌类化合物的构效关系研究。

Structure-Activity Relationship Studies of Antimicrobial Naphthoquinones Derived from Constituents of Tabebuia avellanedae.

机构信息

School of Agriculture, Kindai University.

Research Center for Microorganism Control, Osaka Prefecture University.

出版信息

Chem Pharm Bull (Tokyo). 2021;69(7):661-673. doi: 10.1248/cpb.c21-00208.

Abstract

In this study, based on our previous study, derivatives of naphtho[2,3-b]furan-4,9-diones were synthesized and their antimicrobial activities were evaluated. The screening of these naphthoquinones revealed that the fluorine-containing NQ008 compound exhibited potent and broad antimicrobial activities against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA), Gram-negative bacteria, and fungi. The results of the ratio of the minimum bactericidal concentration (MBC) to the minimum inhibitory concentrations (MICs) and time-kill assays suggest that the mode of action of NQ008 is bactericidal. Additionally, the results of a drug resistance study revealed that NQ008 exhibited potent antibacterial activity and may delay the development of bacteria resistance. Furthermore, NQ008 exhibited preliminary antiviral activity against the swine influenza virus and Feline calicivirus.

摘要

在这项研究中,基于我们之前的研究,我们合成了萘并[2,3-b]呋喃-4,9-二酮的衍生物,并评估了它们的抗菌活性。这些萘醌的筛选结果表明,含氟的 NQ008 化合物对革兰氏阳性菌(包括耐甲氧西林金黄色葡萄球菌(MRSA))、革兰氏阴性菌和真菌具有强大而广泛的抗菌活性。最小杀菌浓度(MBC)与最小抑菌浓度(MIC)比值和时间杀伤试验的结果表明,NQ008 的作用模式是杀菌。此外,耐药性研究的结果表明,NQ008 具有强大的抗菌活性,并且可能延迟细菌耐药性的发展。此外,NQ008 对猪流感病毒和猫杯状病毒表现出初步的抗病毒活性。

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