In vitro antileishmanial activity of nicotinamide
In vitro antileishmanial activity of nicotinamide
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DOI：
10.1128/aac.49.2.808-812.2005
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发表时间：
2005-02-01
影响因子：
4.9
通讯作者：
Ouaissi, A
中科院分区：
文献类型：
--
作者：
Sereno, D;Alegre, AM;Ouaissi, A
我们的研究代表了第一份证明烟酰胺（NAm）（维生素B-3的一种形式）抗利什曼原虫活性的报告。5 mM浓度的NAm显著抑制利什曼原虫无鞭毛体的细胞内生长和过表达硕大利什曼原虫SIR 2（LmSIR 2）的寄生虫携带的NAD依赖性脱乙酰酶活性。然而，转基因寄生虫与野生型寄生虫一样容易受到NAm诱导的细胞生长停滞的影响。因此，我们得出结论，NAm抑制利什曼原虫生长，LmSIR 2的过表达不能克服这种抑制。抑制机制尚未确定，但可能包括其他体内靶点。因此，NAm可能代表一种新的抗利什曼原虫药物，可能在治疗过程中与其他药物联合使用。
Our study represents the first report demonstrating the antileishmanial activity of nicotinamide (NAm), a form of vitamin B-3. A 5 mM concentration of NAm significantly inhibited the intracellular growth of Leishmania amastigotes and the NAD-dependent deacetylase activity carried by parasites overexpressing Leishmania major SIR2 (LmSIR2). However, the transgenic parasites were as susceptible as the wild-type parasites to NAm-induced cell growth arrest. Therefore, we conclude that NAm inhibits leishmanial growth and that overexpression of LmSIR2 does not overcome this inhibition. The mechanism of the inhibition is not defined but may include other in vivo targets. NAm may thus represent a new antileishmanial agent which could potentially be used in combination with other drugs during therapy.