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用于复发性败血症感染的抗菌肽模拟物:针对免疫功能低下疾病靶点的体外研究

Antimicrobial Peptidomimetics for Recurrent Septicemia Infections: In Vitro Study for Immuno Compromised Disease Target.

作者信息

Sharma Priyanka, Nagarajan Kandasamy, Panda Bihu Prasad

机构信息

P.G Research Scholar, Department of Pharmacology, KIET School of Pharmacy, Ghaziabad, Delhi-NCR, India.

Professor & Head, Department of Pharmaceutical Chemistry, KIET School of Pharmacy, Ghaziabad, Delhi-NCR, India.

出版信息

Drug Res (Stuttg). 2018 Sep;68(9):499-503. doi: 10.1055/s-0043-119069. Epub 2018 Apr 16.

Abstract

The frequency of Bacillus subtilis infection such as pneumonia pan-opthalmitis, visceral abscess or musculoskeletal infection etc. complications following bacteremia, meningitis in children & the infection associated with majority of motor vehicle accidents associated with trauma & gun shoot injury. Antibiotics which appear especially useful in the treatment of Bacillus. infection are clindamycin and vancomycin to which vast majority of strains are susceptible in vitro. Our objective is to test the synthesized peptidomimetics with the efforts mainly directed towards the identification of antibacterial compounds against recurrent septicemia infection. Six peptidomimetics namely G-A-L-D (C-soot Glu-ala-leu-Asp), D-P-F (C-soot Asp-pro-Phe), I-R (C-soot Ile-Arg), L-R (C-soot leu-Arg), E-R (C-soot Glu-Arg), D-E (C-soot Asp-Glu), the column eluted compounds were tested for disc diffusion using gram positive Bacillus Subtilis strains at different concentrations predicted by pH and inhibitory concentrations. I-R (C-soot Ile-Arg), & D-E (C-soot Asp-Glu) was found to be very effective along with 5 compounds against Bacillus Subtilis strain tested. Maximum activity 100 µg/ml for synthesized peptidomimetics with the corresponding zonal inhibition diameter (11 mm; 11 mm; 14 mm; 11 mm; 11 mm; 14 mm) against Bacillus subtilis strain. This is the first evidence based report that proves I-R (C-soot Ile-Arg) & D-E (C-soot Asp-Glu) has shown antibacterial action against gram positive strains of Bacillus Subtilis against recurrent septicemia infection.

摘要

儿童菌血症、脑膜炎后诸如肺炎、全眼球炎、内脏脓肿或肌肉骨骼感染等并发症的枯草芽孢杆菌感染频率,以及与大多数机动车事故相关的创伤和枪伤相关的感染。在治疗枯草芽孢杆菌感染方面似乎特别有用的抗生素是克林霉素和万古霉素,绝大多数菌株在体外对其敏感。我们的目标是测试合成的拟肽,主要致力于鉴定针对复发性败血症感染的抗菌化合物。六种拟肽,即G-A-L-D(C-烟炱Glu-ala-leu-Asp)、D-P-F(C-烟炱Asp-pro-Phe)、I-R(C-烟炱Ile-Arg)、L-R(C-烟炱leu-Arg)、E-R(C-烟炱Glu-Arg)、D-E(C-烟炱Asp-Glu),对柱洗脱化合物使用革兰氏阳性枯草芽孢杆菌菌株在由pH值和抑制浓度预测的不同浓度下进行纸片扩散试验。发现I-R(C-烟炱Ile-Arg)和D-E(C-烟炱Asp-Glu)与其他5种化合物对测试的枯草芽孢杆菌菌株非常有效。合成拟肽在100μg/ml时具有最大活性,对枯草芽孢杆菌菌株的相应抑菌圈直径为(11mm;11mm;14mm;11mm;11mm;14mm)。这是第一份基于证据的报告,证明I-R(C-烟炱Ile-Arg)和D-E(C-烟炱Asp-Glu)对复发性败血症感染的革兰氏阳性枯草芽孢杆菌菌株显示出抗菌作用。

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