用甲醇提取物抑制铜绿微囊桿菌的生长,并利用硅学研究鉴定其活性成分

IF 3.4 Q2 PHARMACOLOGY & PHARMACY
A. Sini, T. K. Bindu, Vinod P. Raphael, K. S. Shaju, Sherry Sebastian
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引用次数: 0

摘要

病原体的抗菌药耐药性是一个新出现的问题,近来已变得越来越重要。医药科学家正在不断探索创新和有效的抗菌剂。铜绿假单胞菌(P. aeruginosa)是一种主要导致肺炎和肝、肾及其他身体部位感染的细菌。它是一种革兰氏阴性细菌,可被环丙沙星和左氧氟沙星等抗生素控制。不过,这种病原体有时会对这些抗菌剂产生抗药性。众所周知,植物具有作为药用化合物来源的潜力,有鉴于此,我们的研究重点是利用井扩散法,研究铜绿微囊桿菌叶片的乙酸乙酯、丙酮和甲醇提取物及其对铜绿微囊桿菌生长的影响。为了深入了解提取物的成分,我们进行了气相色谱-质谱分析。在确定提取物中的成分后,我们评估了其药物相似性、吸收、分布、代谢和排泄(ADME),并进行了分子与铜绿假单胞菌选定结构受体的对接研究,以找出提取物中的活性成分。值得注意的是,只有铜绿微囊藻的甲醇提取物对这种病原体具有显著的抗菌活性。硅学研究显示,两种化合物(即异异胆酸乙酯和甲苯磺酰腙衍生物)具有很高的抑制效力。异胆酸乙酯对病原体的所有结构受体都有很好的抑制作用,而细菌的长效脂肪酶和青霉素结合蛋白等受体则与 4-苯基-3-戊烯-2-酮对甲苯磺酰腙结合良好。本研究的观察结果清楚地表明,马齿苋叶甲醇提取物中的两种植物化学物质,即异异胆酸乙酯和甲苯磺酰腙衍生物,对机会性病原体铜绿假单胞菌的生长具有很强的抑制作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Growth inhibition of P. aeruginosa by methanol extract of Bridelia stipularis and identification of active components using in silico studies

Background

Antimicrobial resistance among pathogens is an emerging problem, gaining significant importance recently. Pharmaceutical scientists are constantly exploring innovative and effective antibacterial agents. Pseudomonas aeruginosa (P. aeruginosa) is a bacterium primarily responsible for pneumonia and infections in the liver, kidneys, and other body parts. It is a Gram-negative bacterium that can be controlled by antibiotics such as ciprofloxacin and levofloxacin. However, this pathogen sometimes exhibits resistance to these antibacterial agents.

Methods

Recognizing the well-known potential of plants as sources of medicinal compounds, our study focused on the ethyl acetate, acetone and methanol extract of the leaves of Bridelia stipularis and its impact on the growth of P. aeruginosa using well diffusion method. To gain insight into the composition of the extract, we conducted GC–MS analysis. After identifying the components present in the extract, we assessed the drug-likeness, absorption, distribution, metabolism, and excretion (ADME) and conducted docking studies of the molecules with the selected structural receptors of P. aeruginosa to find out the active component present in the extract.

Results

Remarkably, only methanol extract of Bridelia stipularis demonstrated significant antibacterial activity against this pathogen. In silico investigations revealed that two compounds, namely ethyl iso-allocholate and toluene sulfonylhydrazone derivative, exhibited high inhibition potencies. All structural receptors of the pathogen taken for this study were well inhibited by ethyl iso-allocholate while the receptors such as laconizing lipase and penicillin-binding protein of the bacterium were bound well with the 4-phenyl-3-penten-2-one p-toluene sulfonylhydrazone.

Conclusions

Observations of this study clearly establish that the two phytochemicals present in the methanolic extract, i.e., ethyl iso-allocholate and toluene sulfonylhydrazone derivative of Bridelia stipularis leaves are highly active against the growth of the opportunistic pathogen P. aeruginosa.

Graphical abstract

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来源期刊
自引率
0.00%
发文量
44
审稿时长
23 weeks
期刊介绍: Future Journal of Pharmaceutical Sciences (FJPS) is the official journal of the Future University in Egypt. It is a peer-reviewed, open access journal which publishes original research articles, review articles and case studies on all aspects of pharmaceutical sciences and technologies, pharmacy practice and related clinical aspects, and pharmacy education. The journal publishes articles covering developments in drug absorption and metabolism, pharmacokinetics and dynamics, drug delivery systems, drug targeting and nano-technology. It also covers development of new systems, methods and techniques in pharmacy education and practice. The scope of the journal also extends to cover advancements in toxicology, cell and molecular biology, biomedical research, clinical and pharmaceutical microbiology, pharmaceutical biotechnology, medicinal chemistry, phytochemistry and nutraceuticals.
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