Si Lifang, Li Pan, Liu Xiong, Luo Lixin
a School of Bioscience & Bioengineering, South China University of Technology, Guangzhou University Town , Panyu , Guangzhou , China.
J Enzyme Inhib Med Chem. 2016;31(sup1):184-196. doi: 10.1080/14756366.2016.1178639. Epub 2016 May 10.
Many Gram-positive bacteria can anchor their surface proteins to the cell wall peptidoglycan covalently by a common mechanism with Sortase A (SrtA), thus escaping from the host's identification of immune cells. SrtA can complete this anchoring process by cleaving LPXTG motif conserved among these surface proteins and thus these proteins anchor on the cell wall. Moreover, those SrtA mutants lose this capability to anchor these relative proteins, with these bacteria no longer infectious. Therefore, SrtA inhibitors can be promising anti-infective agents to cure bacterial infections. Chinese herb medicines (CHMs) (chosen from Science Citation Index) have exhibited inhibition on SrtA of Gram-positive pathogens irreversibly or reversibly. In general, CHMs are likely to have important long-term impact as new antibacterial compounds and sought after by academia and the pharmaceutical industry. This review mainly focuses on SrtA inhibitors from CHMs and the potential inhibiting mechanism related to chemical structures of compounds in CHMs.
许多革兰氏阳性菌可通过与分选酶A（SrtA）的共同机制将其表面蛋白共价锚定到细胞壁肽聚糖上，从而逃避宿主免疫细胞的识别。SrtA可通过切割这些表面蛋白中保守的LPXTG基序来完成这一锚定过程，进而使这些蛋白锚定在细胞壁上。此外，那些SrtA突变体失去了锚定这些相关蛋白的能力，这些细菌也不再具有传染性。因此，SrtA抑制剂有望成为治疗细菌感染的抗感染药物。中草药（选自科学引文索引）已表现出对革兰氏阳性病原体的SrtA具有不可逆或可逆的抑制作用。总体而言，中草药作为新型抗菌化合物可能具有重要的长期影响，并受到学术界和制药行业的追捧。本综述主要关注中草药中的SrtA抑制剂以及与中草药中化合物化学结构相关的潜在抑制机制。
