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姜黄素在血清白蛋白、血浆和全血存在时抗菌活性的改变。

Altered antibacterial activity of Curcumin in the presence of serum albumin, plasma and whole blood.

作者信息

Teow Sin Yeang, Ali Syed A

机构信息

Cluster of Oncological and Radiological Sciences, Advanced Medical and Dental Institute (AMDI), University Sains Malaysia (USM), Bertam, Kepala Batas, Pulau Pinang, Malaysia.

出版信息

Pak J Pharm Sci. 2017 Mar;30(2):449-457.

Abstract

Antibacterial effect is one of the major therapeutic activities of plant-derived Curcumin. This work evaluated the effect of serum albumin, human plasma, and whole blood on the in vitro activity of Curcumin against eight clinical bacterial isolates by standard broth microdilution and plate-counting methods. Toxicological effects of Curcumin towards human red blood cells (RBCs) and peripheral blood mononuclear cells (PBMCs) were also investigated. Curcumin exhibited weak activity against gram-negative bacteria, except Escherichia coli and Shigella flexneri were susceptible and was most active against gram-positive bacteria: Staphylococcus aureus, Streptococcus pyogenes and Enterococcus faecalis. The antibacterial activity was impaired in the presence of bovine serum albumin (BSA), human plasma and whole blood. Curcumin was not toxic to PBMCs and RBCs at 200μg/mL. Furthermore, Curcumin showed synergistic activity in combination with antibiotics: Ciprofloxacin, Gentamicin, Vancomycin and Amikacin against Staphylococcus aureus. This study demonstrated that the interaction of Curcumin with plasma proteins diminishes its in vitro antibacterial activity. Curcumin derivatives with reduced affinity for plasma protein may improve the bioavailability and antibacterial activities.

摘要

抗菌作用是植物来源的姜黄素的主要治疗活性之一。本研究通过标准肉汤微量稀释法和平板计数法,评估了血清白蛋白、人血浆和全血对姜黄素体外抗8种临床分离细菌活性的影响。还研究了姜黄素对人红细胞(RBC)和外周血单个核细胞(PBMC)的毒理学作用。姜黄素对革兰氏阴性菌表现出较弱的活性,除了大肠杆菌和弗氏志贺菌敏感外,对革兰氏阳性菌:金黄色葡萄球菌、化脓性链球菌和粪肠球菌最具活性。在牛血清白蛋白(BSA)、人血浆和全血存在的情况下,抗菌活性受到损害。姜黄素在200μg/mL时对PBMC和RBC无毒。此外,姜黄素与抗生素:环丙沙星、庆大霉素、万古霉素和阿米卡星联合使用时,对金黄色葡萄球菌表现出协同活性。本研究表明,姜黄素与血浆蛋白的相互作用会降低其体外抗菌活性。对血浆蛋白亲和力降低的姜黄素衍生物可能会提高其生物利用度和抗菌活性。

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