Matijević-Sosa Julija, Cvetnić Zdenka
Department of Biochemistry and Molecular Biology, Faculty of Pharmacy and Biochemistry, University of Zagreb, Croatia.
Acta Pharm. 2005 Dec;55(4):387-99.
Antibacterial and antifungal activity of N-phthaloylamino acid hydroxamates [C6H4(CO)2N-X-CONHOH, X=amino acid residues of glycine, beta-alanine or D-phenylglycine], was examined against 44 strains of Gram-positive and Gram-negative bacteria, and 10 species of yeasts. The level of antimicrobial activity was established using the in vitro agar assay and the standard broth dilution susceptibility test. N-phthaloyl-D-phenylglycine-hydroxa- mic acid , the substance with the highest lipophilicity (log P), showed the best antibacterial activity, especially against Gram-negative bacteria. Minimum inhibitory concentration of was 0.008 mg mL-1 in the activity against Yersinia enterocolitica O3, confirmed by a large inhibition zone (30 mm) by the diffusion test. Hydroxamates inhibit growth by chelation of the PDF enzyme metal in both Gram-positive and Gram-negative bacteria, and LpxC enzyme in Gram-negative enzyme. Phthalimides appear to contribute to inhibition by destabilizing m-RNA. Antifungal activity of substances is not very expressed.
研究了N-邻苯二甲酰基氨基酸异羟肟酸酯[C6H4(CO)2N-X-CONHOH，X=甘氨酸、β-丙氨酸或D-苯甘氨酸的氨基酸残基]对44株革兰氏阳性菌和革兰氏阴性菌以及10种酵母的抗菌和抗真菌活性。采用体外琼脂试验和标准肉汤稀释药敏试验确定抗菌活性水平。N-邻苯二甲酰-D-苯甘氨酸异羟肟酸酯是亲脂性最高（log P）的物质，表现出最佳的抗菌活性，尤其是对革兰氏阴性菌。在针对小肠结肠炎耶尔森菌O3的活性中，其最低抑菌浓度为0.008 mg/mL，扩散试验显示出较大的抑菌圈（30 mm）证实了这一点。异羟肟酸酯通过螯合革兰氏阳性菌和革兰氏阴性菌中的PDF酶金属以及革兰氏阴性菌中的LpxC酶来抑制生长。邻苯二甲酰亚胺似乎通过使mRNA不稳定来促进抑制作用。这些物质的抗真菌活性不太明显。
