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林恩:抗菌活性、植物化学与增强的抗生素联合策略。

Linn.: Antibacterial Activity, Phytochemistry, and Enhanced Antibiotic Combinatorial Strategies.

作者信息

Tiwana Gagan, Cock Ian E, Cheesman Matthew J

机构信息

School of Pharmacy and Medical Sciences, Gold Coast Campus, Griffith University, Gold Coast 4222, Australia.

School of Environment and Science, Nathan Campus, Griffith University, Brisbane 4111, Australia.

出版信息

Antibiotics (Basel). 2024 Jul 16;13(7):654. doi: 10.3390/antibiotics13070654.

Abstract

Antimicrobial resistance (AMR) is a global public health threat caused by the misuse and overuse of antibiotics. It leads to infections becoming difficult to treat, causing serious illness, disability, and death. Current antibiotic development is slow, with only 25% of current antibiotics exhibiting novel mechanisms against critical pathogens. Traditional medicinal plants' secondary metabolites offer potential for developing novel antibacterial compounds. These compounds, often with strong antimicrobial activity, can be used to develop safe and effective antibacterial chemotherapies. This study investigated the antibacterial activity of Linn. extracts against a panel of bacterial pathogens using disc diffusion and microdilution assays and quantified by calculation of minimum inhibition concentration (MIC). Additionally, the effects of combinations of the extracts and selected conventional antibiotics were examined by sum of fractional inhibition concentration (ƩFIC) calculation and isobologram analysis. Liquid chromatography-mass spectrometry (LC-MS) phytochemistry analysis was used to identify noteworthy compounds in the active extracts and the nauplii bioassay was used to evaluate toxicity. The aqueous and methanolic extracts exhibited notable antibacterial activity in the broth microdilution assay against and methicillin-resistant (MRSA) (MIC = 669 µg/mL and 738 µg/mL, respectively). The methanolic extract also showed noteworthy antibacterial action in the broth assay against (MIC = 738 µg/mL). The aqueous extract had noteworthy growth inhibitory activity against (MIC = 669 µg/mL), whilst the methanolic extract demonstrated good antibacterial activity against that bacterium (MIC = 184 µg/mL). The aqueous and methanol extracts showed minimal antibacterial action against and . The extracts were subjected to LC-MS analysis, which revealed several interesting phytochemicals, including a variety of flavonoids and tannins. The antibacterial activity and lack of toxicity of the extracts indicates that they may be worthwhile targets for antibiotic development and further mechanistic and phytochemistry studies are required.

摘要

抗菌耐药性(AMR)是一种由抗生素滥用和过度使用导致的全球公共卫生威胁。它使感染变得难以治疗,引发严重疾病、残疾和死亡。当前抗生素研发进展缓慢,目前仅有25%的抗生素对关键病原体具有新的作用机制。传统药用植物的次生代谢产物为开发新型抗菌化合物提供了潜力。这些化合物通常具有强大的抗菌活性,可用于开发安全有效的抗菌化疗药物。本研究使用纸片扩散法和微量稀释法研究了[植物名称] Linn.提取物对一组细菌病原体的抗菌活性,并通过计算最低抑菌浓度(MIC)进行量化。此外,通过计算分数抑菌浓度总和(ƩFIC)和等效线图分析,研究了提取物与选定的传统抗生素组合的效果。采用液相色谱 - 质谱(LC - MS)植物化学分析来鉴定活性提取物中的重要化合物,并使用无节幼体生物测定法评估毒性。水提取物和甲醇提取物在肉汤微量稀释试验中对[细菌名称1]和耐甲氧西林金黄色葡萄球菌(MRSA)表现出显著的抗菌活性(MIC分别为669 µg/mL和738 µg/mL)。甲醇提取物在肉汤试验中对[细菌名称2]也显示出显著的抗菌作用(MIC = 738 µg/mL)。水提取物对[细菌名称3]具有显著的生长抑制活性(MIC = 669 µg/mL),而甲醇提取物对该细菌表现出良好的抗菌活性(MIC = 184 µg/mL)。水提取物和甲醇提取物对[细菌名称4]和[细菌名称5]的抗菌作用最小。对提取物进行LC - MS分析,发现了几种有趣的植物化学物质,包括多种黄酮类化合物和单宁。[植物名称] Linn.提取物的抗菌活性和无毒性表明它们可能是抗生素开发的有价值目标,需要进一步进行机制和植物化学研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb42/11273511/058dd88fe1b7/antibiotics-13-00654-g001.jpg

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