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通过将皮肤抗菌肽固定在藻酸盐纳米颗粒上增强其抗菌活性——薄荷醇和乳酸对其增效作用的影响

Enhanced Antibacterial Activity of Dermaseptin through Its Immobilization on Alginate Nanoparticles-Effects of Menthol and Lactic Acid on Its Potentialization.

作者信息

Hazime Noura, Belguesmia Yanath, Barras Alexandre, Amiche Mohamed, Boukherroub Rabah, Drider Djamel

机构信息

Univ. Lille, CNRS, Centrale Lille, Univ. Polytechnique Hauts-de-France, UMR 8520, IEMN, F-59000 Lille, France.

UMR Transfrontalière BioEcoAgro1158, Univ. Lille, INRAE, Univ. Liège, UPJV, JUNIA, Univ. Artois, Univ. Littoral Côte D'Opale, ICV-Institut Charles Viollette, F-59000 Lille, France.

出版信息

Antibiotics (Basel). 2022 Jun 9;11(6):787. doi: 10.3390/antibiotics11060787.

Abstract

Dermaseptin B2 (DRS-B2) is an antimicrobial peptide secreted by , which is an Amazonian tree frog. Here, we show that the adsorption of DRS-B2 on alginate nanoparticles (Alg NPs) results in a formulation (Alg NPs + DRS-B2) with a remarkable antibacterial activity against ATCC 8739 and 184 strains, which are sensitive and resistant, respectively, to colistin. The antibacterial activity, obtained with this new formulation, is higher than that obtained with DRS-B2 alone. Of note, the addition of lactic acid or menthol to this new formulation augments its antibacterial activity against the aforementioned Gram-negative bacilli. The safety of DRS-B2, and also that of the new formulation supplemented or not with a small molecule such as lactic acid or menthol has been proven on the human erythrocytes and the eukaryotic cell line types HT29 (human) and IPEC-1 (animal). Similarly, their stability was determined under the conditions mimicking the gastrointestinal tract with different conditions: pH, temperature, and the presence of digestive enzymes. Based on all the obtained data, we assume that these new formulations are promising and could be suggested, after approval and completing regulation aspects, as alternatives to antibiotics to fight infections caused by Gram-negative bacilli such as .

摘要

皮肤防御素B2(DRS - B2)是由亚马逊树蛙分泌的一种抗菌肽。在此,我们表明DRS - B2吸附在海藻酸钠纳米颗粒(Alg NPs)上会形成一种制剂(Alg NPs + DRS - B2),该制剂对分别对黏菌素敏感和耐药的ATCC 8739和184菌株具有显著的抗菌活性。用这种新制剂获得的抗菌活性高于单独使用DRS - B2时的抗菌活性。值得注意的是,向这种新制剂中添加乳酸或薄荷醇可增强其对上述革兰氏阴性杆菌的抗菌活性。DRS - B2以及添加或未添加乳酸或薄荷醇等小分子的新制剂在人红细胞以及HT29(人)和IPEC - 1(动物)等真核细胞系类型上的安全性已得到证实。同样,在模拟胃肠道不同条件(pH、温度和消化酶存在情况)下测定了它们的稳定性。基于所有获得的数据,我们认为这些新制剂很有前景,在获得批准并完成监管方面后,可作为对抗由革兰氏阴性杆菌如[此处原文缺失相关杆菌名称]引起的感染的抗生素替代品被推荐。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/517e/9220408/42c5d070579a/antibiotics-11-00787-g001.jpg

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