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[富勒烯氨基酸衍生物在巨细胞病毒感染中的体外抗病毒活性]

[In vitro antiviral activity of fullerene amino acid derivatives in cytomegalovirus infection].

作者信息

Medzhidova M G, Abdullaeva M V, Fedorova N E, Romanova V S, Kushch A A

出版信息

Antibiot Khimioter. 2004;49(8-9):13-20.

PMID:15727140
Abstract

The in vitro effect of 5 water soluble fullerene C60 amino acid derivatives (FAD) on the development of cytomegalovirus infection was studied in the schemes of the therapeutic, prophylactic and virucidal action. The following compounds as FAD were used: fullerene conjugated with Na salt of gamma-aminobutyric acid (C60-ABA-Na), 2 derivatives based on Na salts of fullerene-gamma-aminobutyric acid and fullerene-omega-caproic acid (C60-ABA-OH-Na and C60-ACA-OH-Na respectively) and 2 derivatives based on methyl ethers of the above mentioned fullerene amino acids (C60-ABA-OH-CH3 and C60-ACA-OH-CH3). All the FAD were able to inhibit the development of the virus cytopathogenic action in the cell culture. However, the compounds had different antiviral properties. C60-ABA-OH-Na, C60-ABA-CH3 and C60-ACA-CH3 showed marked antiviral activity in the prophylactic scheme. 50-Percent inhibition of the virus cytopathogenic action (ID50) was observed when concentrations of the compounds were 0.31, 5 and 25 mcg/ml respectively. C60-ACA-OH-Na inhibited the development of cytomegalovirus infection in the cell culture only in the scheme of the therapeutic action (ID50 4 mcg/ml). C60-ABA-Na had the highest antiviral effect. In a concentration of 0.22 mcg/ml it inhibited the cytomegalovirus plague-forming capacity by 50% in both the prophylactic and the virucidal schemes. The chemotherapeutic index of the compound was within the limits of 2500 to 5450.

摘要

研究了5种水溶性富勒烯C60氨基酸衍生物(FAD)在治疗、预防和杀病毒作用方案中对巨细胞病毒感染发展的体外作用。使用了以下作为FAD的化合物:与γ-氨基丁酸钠共轭的富勒烯(C60-ABA-Na)、基于富勒烯-γ-氨基丁酸和富勒烯-ω-己酸的钠盐的2种衍生物(分别为C60-ABA-OH-Na和C60-ACA-OH-Na)以及基于上述富勒烯氨基酸甲酯的2种衍生物(C60-ABA-OH-CH3和C60-ACA-OH-CH3)。所有FAD均能抑制细胞培养中病毒细胞病变作用的发展。然而,这些化合物具有不同的抗病毒特性。C60-ABA-OH-Na、C60-ABA-CH3和C60-ACA-CH3在预防方案中表现出显著的抗病毒活性。当化合物浓度分别为0.31、5和25 mcg/ml时,观察到病毒细胞病变作用的50%抑制(ID50)。C60-ACA-OH-Na仅在治疗作用方案中抑制细胞培养中巨细胞病毒感染的发展(ID50为4 mcg/ml)。C60-ABA-Na具有最高的抗病毒效果。在0.22 mcg/ml的浓度下,它在预防和杀病毒方案中均能将巨细胞病毒蚀斑形成能力抑制50%。该化合物的化疗指数在2500至5450范围内。

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