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Bioactivity-guided fractionation to identify β-glucuronidase inhibitors in Nymphaea pubescens flower extract

机译:生物活性指导分级分离以鉴定睡莲花提取物中的β-葡萄糖醛酸苷酶抑制剂

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The plant Nymphaea pubescens Willd. (Family: Nymphaeaceae) is edible having medicinal importance. The objective of the study was to analyze the potential hepatoprotective properties of the flowers and pedicels of N. pubescens by inhibiting the enzyme β-glucuronidase. Crude methanol extracts of flower and pedicel as well as chloroform, ethyl acetate, and aqueous fractions of the flower extract were tested for their activities against the enzyme in vitro . The extracts and the fractions were analyzed by GC–MS to identify metabolites present in them. Flower (IC_(50) value?=?270.27?±?4.67?μg/ml) and pedicel (IC_(50) value?=?868.46?±?28.21?μg/ml) extracts have shown to inhibit the β-glucuronidase activity. Chloroform (IC_(50) value?=?147.16?±?6.68?μg/ml), ethyl acetate (IC_(50) value?=?183.94?±?2.37?μg/ml), and aqueous (IC_(50) value?=?339.43?±?5.34?μg/ml) fractions showed significantly stronger activity than that of silymarin (IC_(50) value?=?792.62?±?10.01?μg/ml), the known inhibitor of the enzyme. GC–MS-based analysis of the flower extract and solvent fractions led to the identification of kaempferol having 79-fold stronger activity than that of silymarin, IC_(50) value of kaempferol being 10.44?±?0.084?μg/ml or 0.0037?mM?±?0.0001.
机译:睡莲(Nymphaea pubescens Willd)。 (家庭:睡莲科)是可食用的,具有药用价值。该研究的目的是分析i的花和花梗的潜在肝保护特性。通过抑制酶β-葡萄糖醛酸苷酶。在体外测试了花和花梗的粗甲醇提取物以及氯仿,乙酸乙酯和花提取物的水相部分对酶的活性。通过GC-MS分析提取物和馏分,以鉴定其中存在的代谢物。花(IC_(50)值?=?270.27?±?4.67?μg/ ml)和花梗(IC_(50)值?=?868.46?±?28.21?μg/ ml)提取物显示出可抑制β-葡萄糖醛酸酶的作用。活动。氯仿(IC_(50)值?=?147.16?±?6.68?μg/ ml),乙酸乙酯(IC_(50)值?=?183.94?±?2.37?μg/ ml)和水溶液(IC_(50)值λ=≥339.43±±5.34μg/ ml)级分显示出比水飞蓟素(IC_(50)值== 792.62±±10.01μg/ ml)强的活性。基于GC-MS的花提取物和溶剂组分分析鉴定出山竹酚的活性比水飞蓟素强79倍,山竹酚的IC_(50)值为10.44?±?0.084?μg/ ml或0.0037?。 mM±±0.0001。

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