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编 号:F749363
分子式:C103H177N35O27S3
分子量:2433.92
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生物活性:
Thanatin is an inducible cationic antimicrobial peptide. Thanatin is a pathogen-inducible single-disulfide-bond-containing β-hairpin AMP. Thanatin displays broad-spectrum activity against both Gram-negative and Gram-positive bacteria as well as against various species of fungi with MICs of 0.3-40 μM, 0.6-40 μM and 0.6-20 μM, respectively. Thanatin has the property of competitive replacement of divalent cations from bacterial outer membrane (OM), leading to OM disruption.

体内研究:
Thanatin (1、3、6mg/kg;腹腔注射;1 小时和 6 小时) 可保护感染 NDM-1 产生的大肠杆菌的小鼠。Animal Model:Male BALB/c mice aged 8-10 weeks and weighing 18-22?g with CFU E. coli XJ141026
Dosage:1, 3, 6?mg/kg
Administration:Intraperitoneally injected; at 1 and 6?h
Result:1, 3, and 6?mg/kg markedly increased the survival rate from 0 to 30%, 70%, and 100%, respectively. Showed that the bacterial titers decreased with increasing drug dose. Rescued the pathological damages (large amounts of inflammatory cell infiltration, alveolar fusion, congestion in the spleen red pulp area, hepatic sinusoidal dilation and congestion) in a dose-dependent manner.

体外研究:
Thanatin 具有强阳离子性 (pI 为 10.48),并包含一个独特的短八残基碱性环,该环是通过 C 末端残基 Cys11 和 Cys18 之间形成二硫键而形成的。Thanatin 在 0.4-3.2 μM 的最低抑制浓度 (MIC) 值下对所有 New Delhi metallo-β-lactamase-1 (NDM-1) 产生的大肠杆菌和肺炎克雷伯菌菌株的生长表现出有效的抑制作用。
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