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来自婆罗洲特有植物的生物活性化合物

Bioactive Compounds from the Bornean Endemic Plant .

作者信息

Teo Stephen P, Bhakta Sanjib, Stapleton Paul, Gibbons Simon

机构信息

Research Department of Pharmaceutical and Biological Chemistry, School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK.

Department of Biological Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, Malet Street, London WC1E 7HX, UK.

出版信息

Antibiotics (Basel). 2020 Dec 16;9(12):913. doi: 10.3390/antibiotics9120913.

Abstract

The present study aimed to screen plants for bioactive compounds with potential antibacterial activities. In our efforts to evaluate plants from Borneo, we isolated and elucidated the structures of four natural products from the bioactive fraction of a chloroform extract of using various chromatographic and spectroscopic techniques. The bioactive compounds were identified as a known styryllactone, (+)-altholactone ((2,3,3a,7a)-3-hydroxy-2-phenyl-2,3,3a,7a-tetrahydrobenzo-5(4)-5-one) (), a new styryllactone, (2,3,3a,7a)-3-hydroxy-2-phenyl-2,3,3a,7a-tetrahydrobenzo-5(4)-5-one) () as well as a new alkaloid, 2,6-dimethoxyisonicotinaldehyde () and a new alkenyl-5-hydroxyl-phenyl benzoic acid (). and showed broad-spectrum anti-bacterial activities against Gram-positive and Gram-negative bacteria as well as acid-fast model selected for this study. Compound only demonstrated activities against Gram-positive bacteria whilst displayed selective inhibitory activities against Gram-positive bacterial strains. Additionally, their mechanisms of anti-bacterial action were also investigated. Using as a fast-growing model of tubercle bacilli, compounds , and demonstrated inhibitory activities against whole-cell drug efflux and biofilm formation; two key intrinsic mechanisms of antibiotic resistance. Interestingly, the amphiphilic compound exhibited inhibitory activity against the conjugation of plasmid pKM101 in using a plate conjugation assay. Plasmid conjugation is a mechanism by which Gram-positive and Gram-negative-bacteria acquire drug resistance and virulence. These results indicated that bioactive compounds isolated from can be potential candidates as 'hits' for further optimisation.

摘要

本研究旨在筛选具有潜在抗菌活性生物活性化合物的植物。在评估婆罗洲植物的过程中,我们采用各种色谱和光谱技术,从一种氯仿提取物的生物活性部分中分离并阐明了四种天然产物的结构。这些生物活性化合物被鉴定为一种已知的苯乙烯基内酯,(+)-阿尔托内酯((2,3,3a,7a)-3-羟基-2-苯基-2,3,3a,7a-四氢苯并-5(4)-5-酮)(),一种新的苯乙烯基内酯,(2,3,3a,7a)-3-羟基-2-苯基-2,3,3a,7a-四氢苯并-5(4)-5-酮(),以及一种新的生物碱,2,6-二甲氧基异烟酸醛()和一种新的烯基-5-羟基-苯基苯甲酸()。 和 对革兰氏阳性菌、革兰氏阴性菌以及本研究中选择的抗酸模型均表现出广谱抗菌活性。化合物 仅对革兰氏阳性菌有活性,而 对革兰氏阳性菌菌株表现出选择性抑制活性。此外,还研究了它们的抗菌作用机制。以 作为结核杆菌快速生长模型,化合物 、 和 对全细胞药物外排和生物膜形成表现出抑制活性;这是抗生素耐药性的两个关键内在机制。有趣的是,两亲性化合物 在平板接合试验中对 中质粒pKM101的接合表现出抑制活性。质粒接合是革兰氏阳性菌和革兰氏阴性菌获得耐药性和毒力的一种机制。这些结果表明,从 中分离出的生物活性化合物可能是进一步优化的潜在“命中”候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e240/7767169/640c50081a0f/antibiotics-09-00913-g001.jpg

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