Suppr超能文献

植醇对多重耐药(MDR)菌株的抗生素增效活性、吸收、分布、代谢和排泄(ADME)及分子对接特性分析

Analysis of the Antibiotic-Potentiating Activity, Absorption, Distribution, Metabolism, and Excretion (ADME) and the Molecular Docking Properties of Phytol Against Multi-Drug-Resistant (MDR) Strains.

作者信息

Almeida-Bezerra José Weverton, Menezes Saulo Almeida, Silva José Thyálisson da Costa, de Sousa Simone Galdino, Alves Daniel Sampaio, Alencar Gabriel Gonçalves, Araújo Isaac Moura, Rodrigues Ewerton Yago de Sousa, Oliveira-Tintino Cícera Datiane de Morais, da Cruz Rafael Pereira, Rocha Janaína Esmeraldo, Tintino Saulo Relison, Barbosa-Filho José Maria, Morais-Braga Maria Flaviana Bezerra, de Menezes Irwin Rose Alencar, Raposo António, Coutinho Henrique Douglas Melo

机构信息

Department of Biological Chemistry, Regional University of Cariri-URCA, Crato 63105-000, CE, Brazil.

Biotechnology Center, Federal University of Rio Grande do Sul-UFRGS, Porto Alegre 91501-970, RS, Brazil.

出版信息

Antibiotics (Basel). 2024 Dec 4;13(12):1171. doi: 10.3390/antibiotics13121171.

Abstract

Phytol is a diterpene from the long-chain unsaturated acyclic alcohols, known for its diverse biological effects, including antimicrobial and anti-inflammatory activities. Present in essential oils, phytol is a promising candidate for various applications in the pharmaceutical and biotechnological sectors. This study aimed to evaluate the antibacterial and drug-potentiating effects of phytol against multidrug-resistant bacteria and to evaluate its properties: ADME and molecular docking. The antibacterial activity of phytol and the phytol combined with conventional drugs was evaluated by microdilution tests against standard and resistant bacterial strains. Finally, the SwissADME platform was employed to analyse the physicochemical and pharmacokinetic characteristics of phytol. Phytol significantly reduced the Minimum Inhibitory Concentration (MIC) of norfloxacin and gentamicin required to inhibit multidrug-resistant strains of and , respectively. Additionally, ADME analysis revealed that phytol exhibits low toxicity and favourable pharmacokinetic properties; in addition, it is revealed through molecular docking that phytol showed a relevant affinity with the proteins 6GJ1 and 5KDR, however, with values lower than the drugs gentamicin and ampicillin. Collectively, these findings suggest that phytol holds potential as an effective adjuvant in combating antimicrobial resistance.

摘要

叶绿醇是一种来自长链不饱和无环醇的二萜类化合物,以其多样的生物学效应而闻名,包括抗菌和抗炎活性。叶绿醇存在于香精油中,是制药和生物技术领域各种应用的有前景的候选物。本研究旨在评估叶绿醇对多重耐药菌的抗菌和药物增强作用,并评估其性质:药物代谢动力学和分子对接。通过针对标准和耐药细菌菌株的微量稀释试验评估了叶绿醇以及叶绿醇与传统药物联合使用时的抗菌活性。最后,利用瑞士ADME平台分析了叶绿醇的理化和药代动力学特征。叶绿醇分别显著降低了抑制多重耐药菌株和所需的诺氟沙星和庆大霉素的最低抑菌浓度(MIC)。此外,药物代谢动力学分析表明叶绿醇具有低毒性和良好的药代动力学性质;此外,通过分子对接发现叶绿醇与蛋白质6GJ1和5KDR具有相关亲和力,然而,其亲和力值低于药物庆大霉素和氨苄西林。总的来说,这些发现表明叶绿醇作为对抗抗菌耐药性的有效佐剂具有潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac58/11672802/2a07f709485c/antibiotics-13-01171-g001.jpg

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验