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AMXT-1501 针对革兰氏阳性菌和革兰氏阴性菌的多药耐药菌靶向细胞膜磷脂。

AMXT-1501 targets membrane phospholipids against Gram-positive and -negative multidrug-resistant bacteria.

机构信息

Department of Infectious Diseases and Shenzhen Key Lab of Endogenous Infection, Shenzhen Nanshan People's Hospital and the 6th Affiliated Hospital of Shenzhen University Medical School, Shenzhen, People's Republic of China.

Department of Tuberculosis, Shenzhen Nanshan Center for Chronic Disease Control, Shenzhen, People's Republic of China.

出版信息

Emerg Microbes Infect. 2024 Dec;13(1):2321981. doi: 10.1080/22221751.2024.2321981. Epub 2024 Feb 29.

DOI:10.1080/22221751.2024.2321981
PMID:38422452
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10906134/
Abstract

The rapid proliferation of multidrug-resistant (MDR) bacterial pathogens poses a serious threat to healthcare worldwide. Carbapenem-resistant (CR) Enterobacteriaceae, which have near-universal resistance to available antimicrobials, represent a particularly concerning issue. Herein, we report the identification of AMXT-1501, a polyamine transport system inhibitor with antibacterial activity against Gram-positive and -negative MDR bacteria. We observed minimum inhibitory concentration (MIC)/MIC values for AMXT-1501 in the range of 3.13-12.5 μM (2.24-8.93 μg /mL), including for methicillin-resistant (MRSA), CR , , and . AMXT-1501 was more effective against MRSA and CR than vancomycin and tigecycline, respectively. Subinhibitory concentrations of AMXT-1501 reduced the biofilm formation of and . Mechanistically, AMXT-1501 exposure damaged microbial membranes and increased membrane permeability and membrane potential by binding to cardiolipin (CL) and phosphatidylglycerol (PG). Importantly, AMXT-1501 pressure did not induce resistance readily in the tested pathogens.

摘要

多药耐药（MDR）细菌病原体的迅速增殖对全球的医疗保健构成了严重威胁。碳青霉烯耐药（CR）肠杆菌科对现有抗菌药物具有近乎普遍的耐药性，这是一个特别令人关注的问题。在此，我们报告了 AMXT-1501 的鉴定，这是一种多胺转运系统抑制剂，对革兰氏阳性和阴性 MDR 细菌具有抗菌活性。我们观察到 AMXT-1501 的最小抑菌浓度（MIC）/MIC 值在 3.13-12.5 μM（2.24-8.93 μg/ml）范围内，包括耐甲氧西林金黄色葡萄球菌（MRSA）、CR 、 和 。与万古霉素和替加环素相比，AMXT-1501 对 MRSA 和 CR 更为有效。亚抑菌浓度的 AMXT-1501 减少了 和 的生物膜形成。在机制上，AMXT-1501 暴露通过与心磷脂（CL）和磷脂酰甘油（PG）结合来破坏微生物膜并增加膜通透性和膜电位。重要的是，在测试的病原体中，AMXT-1501 压力不易诱导耐药性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/108bc4d4ee05/TEMI_A_2321981_F0007_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/a79c8b61d3d6/TEMI_A_2321981_F0001_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/725f1e8eb53f/TEMI_A_2321981_F0002_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/8eac2518c97d/TEMI_A_2321981_F0003_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/b0ae46e51191/TEMI_A_2321981_F0004_OB.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/bda8b1dfa392/TEMI_A_2321981_F0005_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/02671c6dbe65/TEMI_A_2321981_F0006_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/108bc4d4ee05/TEMI_A_2321981_F0007_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/a79c8b61d3d6/TEMI_A_2321981_F0001_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/725f1e8eb53f/TEMI_A_2321981_F0002_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/8eac2518c97d/TEMI_A_2321981_F0003_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/b0ae46e51191/TEMI_A_2321981_F0004_OB.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/bda8b1dfa392/TEMI_A_2321981_F0005_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/02671c6dbe65/TEMI_A_2321981_F0006_OC.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc2c/10906134/108bc4d4ee05/TEMI_A_2321981_F0007_OC.jpg

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