Kennedy J F, Humphreys J D
Antimicrob Agents Chemother. 1976 May;9(5):766-70. doi: 10.1128/AAC.9.5.766.
The water-insoluble hydroxides of zirconium (IV), titanium (IV), titanium (III), iron (II), vanadium (III), and tin (II) have been used to prepare insoluble derivatives of a cyclic peptide antibiotic by a facile chelation process. Testing of the antibacterial activities of the products against two gram-positive and two gram-negative bacteria showed that in the majority of cases the water-insoluble antibiotics remained active against those bacteria susceptible to the parent antibiotic. The power of the assay system has been extended by the novel use of colored organisms to aid determinations where the growth of normal organisms could not be distinguished from the appearance of the supporting material. Insoluble derivatives of neomycin, polymyxin B, streptomycin, ampicillin, penicillin G, and chloramphenicol were prepared by chelation with zirconium hydroxide, and these derivatives similarly reflected the antibacterial activities of the parent compounds. Several of the metal hydroxides themselves possess antibacterial activity due to complex formation with the bacteria. However, the use of selected metal hydroxides can afford a simple, inexpensive, and inert matrix for antibiotic immobilization, resulting in an antibacterial product that may possess slow-release properties. The mechanisms by which the metal hydroxide-antibiotic association-dissociation may occur are discussed.
锆（IV）、钛（IV）、钛（III）、铁（II）、钒（III）和锡（II）的水不溶性氢氧化物已被用于通过简便的螯合过程制备环肽抗生素的不溶性衍生物。对产物针对两种革兰氏阳性菌和两种革兰氏阴性菌的抗菌活性测试表明，在大多数情况下，水不溶性抗生素对那些对母体抗生素敏感的细菌仍保持活性。通过新颖地使用有色生物体来辅助测定，扩展了检测系统的能力，在这些测定中，正常生物体的生长与支持材料的外观无法区分。通过与氢氧化锆螯合制备了新霉素、多粘菌素B、链霉素、氨苄青霉素、青霉素G和氯霉素的不溶性衍生物，这些衍生物同样反映了母体化合物的抗菌活性。几种金属氢氧化物本身由于与细菌形成络合物而具有抗菌活性。然而，使用选定的金属氢氧化物可为抗生素固定提供一种简单、廉价且惰性的基质，从而得到一种可能具有缓释特性的抗菌产品。讨论了金属氢氧化物 - 抗生素缔合 - 解离可能发生的机制。
