Resistance modulatory and efflux-inhibitory activities of capsaicinoids and capsinoids

被引：19

作者：

Prasch, Sandra ^{[1
]}

Duran, Alexandra G. ^{[2
]}

Chinchilla, Nuria ^{[2
]}

Molinillo, Jose M. G. ^{[2
]}

Macias, Francisco A. ^{[2
]}

Bucar, Franz ^{[1
]}

机构：

[1] Karl Franzens Univ Graz, Inst Pharmaceut Sci, Dept Pharmacognosy, Univ Pl 4, A-48010 Graz, Austria

[2] Univ Cadiz, Sch Sci, Inst Biomol INBIO, Dept Organ Chem,Allelopathy Grp, Campus Excelencia Int ceiA3,C Repub Saharaui 7, Cadiz 11510, Spain

来源：

BIOORGANIC CHEMISTRY | 2019年 / 82卷

关键词：

Capsaicinoids; Capsinoids; Efflux pump inhibitor; Resistance; Mycobacteria; ETHIDIUM-BROMIDE EFFLUX; CAPSICUM; CYTOTOXICITY; CHANNEL; FRUITS; CELLS;

D O I：

10.1016/j.bioorg.2018.10.062

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Capsaicinoids are reported to have a bunch of promising pharmacological activities, among them antibacterial effects against various strains of bacteria. In this study the effect on efflux pumps of mycobacteria was investigated. The importance of efflux pumps, and the inhibition of these, is rising due to their involvement in antibiotic resistance development. In order to draw structure and activity relationships we tested natural and synthetical capsaicinoids as well as synthetical capsinoids. In an accumulation assay these compounds were evaluated for their ability to accumulate ethidium bromide into mycobacterial cells, a well-known substrate for efflux pumps. Capsaicin and dihydrocapsaicin, the two most abundant capsaicinoids in Capsicum species, proved to be superior efflux pump inhibitors compared to the standard verapamil. A dilution series showed dose dependency of both compounds. The compound class of less pungent capsinoids qualified for further investigation as antibacterials against Mycobacterium smegmatis.

引用

页码：378 / 384

页数：7

共 28 条

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