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多粘菌素B(PMB)是一种环十肽抗生素,它也结合和中和内毒素。不幸的是PMB的临床使用剂量可能被认为具有肾毒性,因此就限制了其用作治疗抗内毒素药物。作者试图通过将PMB共价联结于免疫球蛋白G携带者以改变其药代学和毒性。EDAC[1-乙基-3-(3-二苯胺丙基)碳化二酰亚胺]介导酰胺形成以制备PMB和IgG结合物。用有抗PMB单克隆抗体的斑点酶联免疫吸附试验显示纯化的结合物含结合的PMB。在蛋白质印迹试验中,结合物IgG-PMB与脂质A和脂多糖J5呈反应,同含抗脂质A的抗全血清反应比较,未结合的IgG不具此反
Polymyxin B (PMB) is a cyclic decapeptide antibiotic that also binds and neutralizes endotoxins. Unfortunately, the clinical dose of PMB may be considered nephrotoxic, thus limiting its use as an anti-endotoxin drug. The authors sought to alter their pharmacology and toxicity by covalently linking PMB to immunoglobulin G carriers. EDAC [l-ethyl-3- (3-diphenylaminopropyl) carbodiimide] mediates amide formation to make PMB and IgG conjugates. Dot-ELISA tests with anti-PMB monoclonal antibodies showed that the purified conjugates contained bound PMB. In the Western blotting assay, the conjugate IgG-PMB reacted with Lipid A and Lipopolysaccharide J5, and the unbound IgG did not have the reverse as compared to anti-full serum containing anti-lipid A