肉豆蔻酸抑制细菌 ABC 转运蛋白 BmrA 的活性。

Department of Chemistry, Johannes Gutenberg-University, 55128 Mainz, Germany.

Institut für Biotechnologie und Wirkstoff-Forschung gGmbH (IBWF), 55128 Mainz, Germany.

Int J Mol Sci. 2021 Dec 17;22(24):13565. doi: 10.3390/ijms222413565.

ATP-binding cassette (ABC) transporters are conserved in all kingdoms of life, where they transport substrates against a concentration gradient across membranes. Some ABC transporters are known to cause multidrug resistances in humans and are able to transport chemotherapeutics across cellular membranes. Similarly, BmrA, the ABC transporter of is involved in excretion of certain antibiotics out of bacterial cells. Screening of extract libraries isolated from fungi revealed that the C14 fatty acid myristic acid has an inhibitory effect on the BmrA ATPase as well as the transport activity. Thus, a natural membrane constituent inhibits the BmrA activity, a finding with physiological consequences as to the activity and regulation of ABC transporter activities in biological membranes.

三磷酸腺苷结合盒（ABC）转运蛋白存在于所有生命领域中，它们在跨膜过程中逆浓度梯度运输底物。一些 ABC 转运蛋白已知会导致人类的多药耐药性，并能够将化疗药物穿过细胞膜。同样，是 ABC 转运蛋白 BmrA 将某些抗生素从细菌细胞中排出。从真菌中分离的提取物文库筛选显示，C14 脂肪酸肉豆蔻酸对 BmrA 的 ATP 酶以及运输活性具有抑制作用。因此，一种天然的膜成分抑制了 BmrA 的活性，这一发现对于 ABC 转运蛋白在生物膜中的活性和调节具有生理意义。