首页> 美国卫生研究院文献>Annals of Tropical Medicine and Parasitology >In vitro antileishmanial activity of fisetin flavonoid via inhibition of glutathione biosynthesis and arginase activity in Leishmania infantum
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In vitro antileishmanial activity of fisetin flavonoid via inhibition of glutathione biosynthesis and arginase activity in Leishmania infantum

机译:通过抑制婴儿利什曼原虫中谷胱甘肽的生物合成和精氨酸酶活性菲西汀类黄酮的体外抗疟药活性

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摘要

With the increasing emergence of drug resistant Leishmania sp. in recent years, combination therapy has been considered as a useful way to treat and control of Leishmaniasis. The present study was designed to evaluate the antileishmanial effects of the fisetin alone and combination of fisetin plus Meglumine antimoniate (Fi-MA) against Leishmania infantum. The IC50 values for fisetin were obtained 0.283 and 0.102 μM against promastigotes and amastigote forms, respectively. Meglumine antimoniate (MA, Glucantime) as control drug also revealed IC50 values of 0.247 and 0.105 μM for promastigotes and amastigotes of L. infantum, respectively. In order to determine the mode of action of fisetin and Meglumine antimoniate (MA, Glucantime), the activities of arginase (ARG), catalase (CAT), glutathione peroxidase (GPx) and superoxide dismutase (SOD) were measured. Moreover, intracellular glutathione (GSH) and nitric oxide (NO) levels in L. infantum-infected macrophages and L. infantum promastigotes which were treated with IC50 concentrations of fisetin, MA and Fi-MA were investigated. Our results showed that MA decreased CAT and SOD activity and increased NO levels in L. infantum-infected macrophages. In promastigotes, MA inhibited parasite SOD activity and reduced parasite NO production. The decreased levels of most of the antioxidant enzymes, accompanying by the raised level of NO in treated macrophages with MA, were observed to regain their normal profiles due to Fi-MA treatment. Furthermore, fisetin could prevent the growth of promastigotes by inhibition of ARG activity and reduction of GSH levels and NO production. In conclusion, these findings showed that fisetin improves MA side effects.
机译:随着耐药性利什曼原虫的出现。近年来,组合疗法已被认为是治疗和控制利什曼病的有用方法。本研究旨在评估单独使用非瑟汀和非瑟汀加葡甲胺锑酸盐(Fi-MA)组合对婴儿利什曼原虫的抗疟疾作用。针对前鞭毛体和鞭毛体形式的非瑟定的IC50值分别为0.283和0.102μM。葡甲胺溴酸盐(MA,Glucantime)作为对照药物也显示婴儿乳杆菌的前鞭毛体和变形虫的IC50值分别为0.247和0.105μM。为了确定非瑟酮和葡甲胺铝酸盐(MA,Glucantime)的作用方式,测定了精氨酸酶(ARG),过氧化氢酶(CAT),谷胱甘肽过氧化物酶(GPx)和超氧化物歧化酶(SOD)的活性。此外,还研究了用IC50浓度的非瑟酮,MA和Fi-MA处理过的婴儿被乳杆菌感染的巨噬细胞和婴儿乳杆菌前体细胞中的谷胱甘肽(GSH)和一氧化氮(NO)水平。我们的结果表明,MA降低了感染小infant乳杆菌的巨噬细胞的CAT和SOD活性,并增加了NO水平。在前鞭毛体中,MA抑制了寄生虫的SOD活性并减少了寄生虫NO的产生。通过Fi-MA处理,观察到大多数抗氧化酶的水平降低,伴随着用MA处理的巨噬细胞中NO水平的升高,恢复了它们的正常分布。此外,非瑟酮可通过抑制ARG活性和降低GSH水平和NO产生来阻止前鞭毛体的生长。总之,这些发现表明,非瑟酮可改善MA的副作用。

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