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异黄酮作为有效抗菌剂的结构先决条件。

Structure pre-requisites for isoflavones as effective antibacterial agents.

作者信息

Mukne Alka P, Viswanathan Vivek, Phadatare Avinash G

机构信息

Department of Pharmacognosy and Phytochemistry, Bombay College of Pharmacy, Mumbai - 400 098, Maharashtra, India.

出版信息

Pharmacogn Rev. 2011 Jan;5(9):13-8. doi: 10.4103/0973-7847.79095.

Abstract

Recent reports reveal that there is increasing incidence of infections of multidrug-resistant bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Flavonoids and related compounds have been shown to possess potent antimicrobial activities. Most of the flavonoids are considered as constitutive antimicrobial substances recently termed as "Phytoanticipins," especially those belonging to prenylated flavonoids and isoflavones. The current review highlights the structure prerequisites for isoflavones as antibacterial agents. Structure-activity relationship (SAR) conclusions have been drawn by comparing the reported minimum inhibitory concentration values for the various isoflavones against S. aureus and MRSA. There exists a significant co-relationship between the presence of certain functional groups (prenyl group, phenolic hydroxyl) at particular positions and antibacterial activity of the compounds. These trends have been postulated with a view of assisting better drug designing of future next-generation antiinfectives, particularly against the bothersome multidrug-resistant microbes. The SAR of these isoflavones has also proved to be a basis to explore the mechanism of antibacterial action. Thus, the study would prove extremely useful to synthesize antibacterial isoflavones in future, which would eventually be beneficial for optimizing the lead molecule for the antibacterial action.

摘要

近期报告显示,包括耐甲氧西林金黄色葡萄球菌(MRSA)和耐万古霉素肠球菌(VRE)在内的多重耐药菌感染的发生率正在上升。黄酮类化合物及相关化合物已被证明具有强大的抗菌活性。大多数黄酮类化合物被认为是最近被称为“植物抗毒素”的组成型抗菌物质,尤其是那些属于异戊烯基黄酮类化合物和异黄酮的物质。本综述重点介绍了异黄酮作为抗菌剂的结构前提条件。通过比较各种异黄酮对金黄色葡萄球菌和MRSA的报告最低抑菌浓度值,得出了构效关系(SAR)结论。特定位置上某些官能团(异戊烯基、酚羟基)的存在与化合物的抗菌活性之间存在显著的相关性。提出这些趋势是为了帮助更好地设计未来的下一代抗感染药物,特别是针对麻烦的多重耐药微生物。这些异黄酮的构效关系也被证明是探索抗菌作用机制的基础。因此,该研究对于未来合成抗菌异黄酮将被证明极其有用,这最终将有利于优化抗菌作用的先导分子。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5f62/3210004/da4569618c20/PRev-5-13-g001.jpg

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