Bulgakova V G, Petrykina Z M, Korolev P N, Sazykina S Iu, Polin A N
Mikrobiologiia. 1985 Jul-Aug;54(4):621-7.
The work was concerned with studying the effect of gramicidin S derivatives with modified free amino groups of ornithine residues on bacterial cells and protoplasts. The substitution of the amino groups with neutral or carboxyl-containing groups eliminated or sharply decreased the antibacterial activity of gramicidin S, its binding to the cells, and the ability to change the permeability of the cytoplasmic membranes of the intact cells. However, the neutral derivatives and the derivative with acidic properties showed a considerable lytic activity when they were incubated with the protoplasts of Micrococcus lysodeikticus, Bacillus megaterium and Bacillus subtilis. Hence, these compounds preserved a certain membranotropic level. Those gramicidin S derivatives with modified ornithine amino groups which possessed basic properties were similar to gramicidin S in the antibiotic activity, the modified permeability of the membranes, the ability to bind with the cells, and the lytic action on the protoplasts.
该研究工作旨在探讨鸟氨酸残基游离氨基被修饰的短杆菌肽S衍生物对细菌细胞和原生质体的影响。用中性或含羧基的基团取代氨基后，短杆菌肽S的抗菌活性、与细胞的结合能力以及改变完整细胞细胞质膜通透性的能力均被消除或大幅降低。然而，当这些中性衍生物和具有酸性性质的衍生物与溶壁微球菌、巨大芽孢杆菌和枯草芽孢杆菌的原生质体一起孵育时，它们表现出相当强的裂解活性。因此，这些化合物保留了一定的膜作用水平。那些具有碱性性质的鸟氨酸氨基被修饰的短杆菌肽S衍生物在抗生素活性、膜通透性改变、与细胞结合的能力以及对原生质体的裂解作用方面与短杆菌肽S相似。
