Mastoparan X (trifluoroacetate

一种抗菌肽；对多种革兰氏阳性菌和革兰氏阴性菌均有活性（MIC分别为3-64和4-256µg/ml），6.4µg/ml时可诱导大肠杆菌细胞质膜通透性增加86%；通过Gi诱导GDP/GTP交换，并在无细胞测定中与钙调蛋白结合（Kd=~0.9nM）；20µM时可诱导T98G细胞坏死；128µg/ml时可诱导大鼠腹膜肥大细胞脱颗粒；诱导绵羊、鸡和人红细胞溶血；20mg/kg时可提高小鼠肠出血性大肠杆菌感染模型的存活率、降低疾病严重程度并防止空肠绒毛和隐窝受损。An antimicrobial peptide; active against several Gram-positive and Gram-negative bacteria (MICs = 3-64 and 4-256 µg/ml, respectively) and induces permeabilization of E. coli cytoplasmic membranes by 86% at 6.4 µg/ml; induces GDP/GTP exchange by Gi and binds to calmodulin (Kd = ~0.9 nM) in cell-free assays; induces necrosis in T98G cells at 20 µM; induces degranulation of isolated rat peritoneal mast cells at 128 µg/ml; induces hemolysis of isolated sheep, chicken, and human erythrocytes; increases survival, decreases disease severity, and prevents damage to jejunal villi and crypts in a mouse model of enterohemorrhagic E. coli infection at 20 mg/kg.分子式C73H126N20O15S • XCF3COOH分子量1556CC[C@H](C)[C@H](N)C(N[C@@H](CC(N)=O)C(N[C@H](C(N[C@@H](CCCCN)C(NCC(N[C@@H]([C@@H](C)CC)C(N[C@@H](C)C(N[C@@H](C)C(N[C@@H](CCSC)C(N[C@@H](C)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CC(C)C)C(N[C@H](C(N)=O)CC(C)C)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CC1=CNC2=CC=CC=C12)=O)=O.OC(C(F)(F)F)=O