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通过生物测定法从[具体来源未给出]中分离出对[具体对象未给出]具有杀菌活性的季铵型苄基异喹啉。

Bioassay-directed isolation of quaternary benzylisoquinolines from with bactericidal activity against .

作者信息

Azimi Gholamhassan, Hakakian Ali, Ghanadian Mustafa, Joumaa Ali, Alamian Saeed

机构信息

Department of Chemistry, University of Isfahan, Isfahan, I.R. Iran.

Department of Research and Development, Production and Research Complex, Pasteur Institute, I.R. Iran.

出版信息

Res Pharm Sci. 2018 Apr;13(2):149-158. doi: 10.4103/1735-5362.223797.

DOI:10.4103/1735-5362.223797
PMID:29606969
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5842486/
Abstract

Bonge. (Syn: Boiss. & Buhse) is a shrub widely distributed in Middle East and central part of Asia. An ethnobotanical study revealed that indigenous and tribal people in Iran use root decoction for treatment of brucellosis. Therefore, the aim of this study was bioassay directed isolation of antibacterial compounds from this plant based on their bactericidal activity against . Briefly, the ethanol extract of was fractioned and subjected to preliminary antibacterial screening tests against Brucella. The more active fraction (Fr.3) was subjected to purification by repeated chromatography systems. Quaternary benzylisoquinoline alkaloids including columbamine, palmatine, berberine, and jatrorhizine were four main components identified in the selected active fraction. Except for berberine which is reported before, palmatine, columbamine and jatrorhizine are isolated for the first time from this plant. Anti-brucellosis properties of isolated compounds were studied against under different test conditions. In minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) results, jatrorhizine () showed more antibacterial activity with MIC and MBC of 0.78 and 1.56 μg/mL, respectively. In both agar well diffusion and disk diffusion ANOVA results showed that there were statistically significant differences between compounds versus placebo in all of the tested concentration ( <0.001). In conclusion, all of four alkaloids showed potent antibacterial activity against but jatrorhizine and columbamine with free hydroxyl group on C-3 or C-2 showed more activity than palmatine and berberine without any free hydroxyl group on their structures. The antibacterial effects of columbamine (15 μg/mL) and jatrorhizine (15 μg/mL) were comparative to streptomycin (10 μg/mL) as standard drug which candidate them for more pharmacological researches to find new antibacterial agents against brucellosis.

摘要

邦吉(同义词:布瓦西埃和布斯)是一种广泛分布于中东和亚洲中部的灌木。一项民族植物学研究表明,伊朗的原住民和部落居民使用其根煎剂治疗布鲁氏菌病。因此,本研究的目的是基于其对布鲁氏菌的杀菌活性,对该植物中的抗菌化合物进行生物测定导向分离。简要地说,将该植物的乙醇提取物进行分馏,并对布鲁氏菌进行初步抗菌筛选试验。活性较高的馏分(馏分3)通过反复色谱系统进行纯化。在选定的活性馏分中鉴定出的四种主要成分是季铵型苄基异喹啉生物碱,包括黄连碱、巴马汀、小檗碱和药根碱。除之前报道过的小檗碱外,巴马汀、黄连碱和药根碱首次从该植物中分离得到。在不同测试条件下,研究了分离出的化合物对布鲁氏菌的抗布鲁氏菌病特性。在最低抑菌浓度(MIC)和最低杀菌浓度(MBC)结果中,药根碱()显示出更强的抗菌活性,MIC和MBC分别为0.78和1.56μg/mL。在琼脂孔扩散和纸片扩散试验中,方差分析结果表明,在所有测试浓度下,化合物与安慰剂之间存在统计学显著差异(<0.001)。总之,所有四种生物碱对布鲁氏菌均显示出强大的抗菌活性,但在C-3或C-2上带有游离羟基的药根碱和黄连碱比结构上没有任何游离羟基的巴马汀和小檗碱表现出更强的活性。黄连碱(15μg/mL)和药根碱(15μg/mL)的抗菌效果与作为标准药物的链霉素(10μg/mL)相当,这使它们有资格进行更多的药理学研究,以寻找新的抗布鲁氏菌病抗菌剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d45/5842486/c812c2a24973/RPS-13-149-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d45/5842486/384ceaa7b4a6/RPS-13-149-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d45/5842486/ccbc07dda4d7/RPS-13-149-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d45/5842486/f82593b56512/RPS-13-149-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d45/5842486/c812c2a24973/RPS-13-149-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d45/5842486/384ceaa7b4a6/RPS-13-149-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d45/5842486/ccbc07dda4d7/RPS-13-149-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d45/5842486/f82593b56512/RPS-13-149-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d45/5842486/c812c2a24973/RPS-13-149-g006.jpg

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