The Renaissance of Polymyxins
The Renaissance of Polymyxins
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DOI：
10.2174/09298673113209990185
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发表时间：
2013-10-01
影响因子：
4.1
通讯作者：
Szabo, D.
中科院分区：
文献类型：
--
作者：
Kadar, B.;Kocsis, B.;Szabo, D.
多粘菌素是多肽抗生素，由于其选择性结合革兰氏阴性菌的脂多糖，因此具有膜损伤的主要作用。它们的肾毒性和神经毒性副作用限制了它们的使用，然而，在过去十年中，多重耐药革兰氏阴性细菌的出现导致多粘菌素重新引入临床实践。本综述概述了多粘菌素的历史和最新发展。我们描述了抗菌作用、药效学、药代动力学和不同的给药途径。我们重点介绍天然经典多粘菌素，即多粘菌素B和E，非经典药物多粘菌素M、S和T。将列出新型多粘菌素化学结构衍生物，包括NAB739、NAB740、NAB741和NAB7061，这些衍生物在未来可能具有重要的治疗作用。
Polymyxins are polypeptide antibiotics, with a primary effect of membrane damaging due to their selective binding to the lipopolysaccharide of Gram-negative bacteria. Their nephro- and neurotoxic side effects limited their use, however, in the last decade the emergence of multidrug-resistant Gram-negative bacteria led to the reintroduction of polymyxins into clinical practice. This review provides an overview about the history and the latest developments of polymyxins. We describe the antimicrobial effects, pharmacodynamics, pharmacokinetics and different routes of administration. We highlight natural classic polymyxins, namely polymyxin B and E, the non-classic agents polymyxin M, S and T. Novel polymyxin chemical structure derivatives will be listed including NAB739, NAB740, NAB741 and NAB7061, that can have important therapeutical role in the future.