首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Metabolite profile and in vitro activities of Phagnalon saxatile (L.) Cass. relevant to treatment of Alzheimer's disease
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Metabolite profile and in vitro activities of Phagnalon saxatile (L.) Cass. relevant to treatment of Alzheimer's disease

机译:Phagnalon saxatile(L.)Cass的代谢产物概况和体外活性。与阿尔茨海默氏病的治疗有关

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The present study describes for the first time the in vitro properties (inhibition of NO production and anticholinesterase) of Phagnalon saxatile (L.) Cass. (Asteraceae). The methanolic extract showed antioxidant activity that was measured by DPPH assay and β-carotene bleaching test. The same extract inhibited NO production in the murine monocytic macrophage cell line RAW 264.7. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition was assessed by modifications of Ellman's method. Purification of the MeOH extract of P. saxatile allowed the isolation of phenolic compounds. Among them, the compounds that most effectively inhibited lipopolysaccharide-induced NO production were caffeic acid and methylchlorogenic acid, with IC50 values of 7μg/mL and 12μg/mL, respectively. Luteolin and 3,5-dicaffeoylquinic acid exhibited the most promising activity against AChE with an IC50 of 25.2 and 54.5μg/mL, respectively, while caffeic acid and luteolin exhibited higher activity against BChE with an IC50 of 32.2 and 37.2μg/mL, respectively.
机译:本研究首次描述了Phagnalon saxatile(L.)Cass的体外特性(抑制NO产生和抗胆碱酯酶)。 (菊科)。该甲醇提取物显示出抗氧化剂活性,该活性通过DPPH测定法和β-胡萝卜素漂白试验测定。同一提取物可抑制鼠单核巨噬细胞RAW 264.7中NO的产生。乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)抑制作用通过改良Ellman方法进行评估。虎尾草的MeOH萃取物的纯化允许分离酚类化合物。其中,最有效抑制脂多糖诱导的NO生成的化合物是咖啡酸和甲基绿原酸,IC50值分别为7μg/ mL和12μg/ mL。木犀草素和3,5-二咖啡酰奎宁酸对AChE表现出最有希望的活性,IC50分别为25.2和54.5μg/ mL,而咖啡酸和木犀草素对BChE表现出更高的活性,对IC50的IC50分别为32.2和37.2μg/ mL。 。

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