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铜与生物活性配体的配合物。第二部分——抗真菌活性。

Copper complexes with bioactive ligands. Part II--Antifungal activity.

作者信息

Dudová B, Hudecová D, Pokorný R, Micková M, Palicová M, Segĺa P, Melník M

机构信息

Department of Biochemistry and Microbiology, Faculty of Chemical and Food Technology, Slovak University of Technology, 812 37 Bratislava, Slovakia.

出版信息

Folia Microbiol (Praha). 2002;47(3):225-9. doi: 10.1007/BF02817642.

Abstract

Antifungal activity of new copper(II) complexes of 2-methylthionicotinate (2-MeSNic) of the composition Cu(2-MeSNic)2(MeNia)(2).4H2O (where MeNia is N-methylnicotinamide), and Cu(2-MeSNic)2(Nia)(2).2H2O (where Nia is nicotinamide) and Cu(2-MeSNic)2L2 (where L is isonicotinamide, iNia, or ethyl nicotinate, EtNic) were tested on various strains of filamentous fungi by the macrodilution method. Most sensitive against copper(II) adducts with bioactive ligands were Rhizopus oryzae and Microsporum gypseum (IC50 1.5-2.3 mmol/L). The adducts with Nia, MeNia and EtNic at 5 mmol/L induced morphological changes in growing hyphae of Botrytis cinerea, mainly their intensive branching attached to release of cytoplasm with partial growth inhibition. Inhibition of sporulation (> 90%) of Alternaria alternata by Cu(2-MeSNic)2.H2O was observed as a change in the color of the colonies. The highest resistance was marked by B. cinerea and Fusarium moniliforme (average IC50 values 4.25 and 3.13 mmol/L, respectively). The presence of all bioactive ligands in copper(II) complexes caused an increase in the inhibition effect against model fungi (except significant inhibition activity of EtNic on R. oryzae).

摘要

采用微量稀释法对新型铜(II)-2-甲基硫代烟酸酯(2-MeSNic)配合物Cu(2-MeSNic)2(MeNia)(2).4H2O(其中MeNia为N-甲基烟酰胺)、Cu(2-MeSNic)2(Nia)(2).2H2O(其中Nia为烟酰胺)以及Cu(2-MeSNic)2L2(其中L为异烟酰胺、iNia或烟酸乙酯、EtNic)对多种丝状真菌菌株的抗真菌活性进行了测试。对带有生物活性配体的铜(II)加合物最敏感的是米根霉和石膏样小孢子菌(IC50为1.5 - 2.3 mmol/L)。5 mmol/L的Nia、MeNia和EtNic加合物在灰葡萄孢生长菌丝中诱导了形态变化,主要是其密集分支并伴有细胞质释放及部分生长抑制。观察到Cu(2-MeSNic)2.H2O对链格孢的孢子形成有抑制作用(> 90%),表现为菌落颜色变化。灰葡萄孢和串珠镰刀菌的抗性最强(平均IC50值分别为4.25和3.13 mmol/L)。铜(II)配合物中所有生物活性配体的存在导致对模式真菌的抑制作用增强(除EtNic对米根霉有显著抑制活性外)。

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