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一种来自番石榴(Psidium guajava (Linn.))叶的新型抗菌二苯甲酮糖苷。

A new antibacterial benzophenone glycoside from Psidium guajava (Linn.) leaves.

作者信息

Ukwueze Stanley E, Osadebe Patience O, Okoye Festus B C

机构信息

a Department of Pharmaceutical and Medicinal Chemistry , Faculty of Pharmaceutical Sciences, University of Port Harcourt , Port Harcourt , Nigeria.

出版信息

Nat Prod Res. 2015;29(18):1728-34. doi: 10.1080/14786419.2014.1003188. Epub 2015 Jan 29.

Abstract

Bioactivity-guided fractionation of methanol extract from the leaves of Psidium guajava L. (Myrtaceae) yielded a new benzophenone glycoside, Guajaphenone A (2) together with two known compounds, Garcimangosone D (1) and Guaijaverin (3). Their structures were elucidated by analysis of spectroscopic data including 1D and 2D NMR and electrospray ionisation mass spectrometry (ESI-MS). The isolated compounds were screened against standard strains of Gram-positive and Gram-negative bacteria using broth dilution assay method, and the MIC values determined and compared with reference antibiotic ceftriaxone. They were found to have significant antibacterial activities against Escherichia coli and Staphylococcus aureus with all of them showing better activities against S. aureus, but displaying weaker activities, in comparison to ceftriaxone. However, despite reduced effect of these compounds against the organisms, this work opens the perspective to use these molecules as 'leads' for the design of novel and selective drug candidates for some tropical infectious diseases.

摘要

对番石榴(桃金娘科)叶片甲醇提取物进行生物活性导向分离,得到一种新的二苯甲酮糖苷——番石榴苯酮A(2),以及两种已知化合物——藤黄芒果酮D(1)和番石榴苷(3)。通过分析包括一维和二维核磁共振以及电喷雾电离质谱(ESI-MS)在内的光谱数据,阐明了它们的结构。使用肉汤稀释法对分离出的化合物针对革兰氏阳性和革兰氏阴性细菌的标准菌株进行筛选,测定最小抑菌浓度(MIC)值,并与参考抗生素头孢曲松进行比较。发现它们对大肠杆菌和金黄色葡萄球菌具有显著的抗菌活性,所有化合物对金黄色葡萄球菌的活性均更好,但与头孢曲松相比,活性较弱。然而,尽管这些化合物对这些生物体的作用有所降低,但这项工作为将这些分子用作设计针对某些热带传染病的新型选择性候选药物的“先导物”开辟了前景。

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