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Lipase Inhibitor from Fruits of Solanum stramonifolium Jacq.

机译:茄茄果实中的脂肪酶抑制剂。

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Obesity is usually considered as an overweight or excess body fat, leading to increased health problems. Obesity is a major risk factor for a number of serious diseases. Decreasing dietary fat absorption, through inhibition of pancreatic lipase activity, has been reported to be one of the most effective ways for managing obesity. The present study was aimed at investigating lipase inhibitors from edible plants. A lipase inhibitor was isolated from n-hexane and ethyl acetate extracts of the ripe fruits of Solanum stramonifolium Jacq. by column chromatography and identified by spectral analysis. Its structure was elucidated as (22R)-3β-benzoyloxy-22-hydroxy-4α-methyl-5α-stigmast-7-en-6-one or carpesterol (1). Carpesterol exhibited moderate lipase inhibition activity with IC50 value of 56.0 μg/mL while orlistat, a well- know pancreatic lipase inhibitor, had IC50 value of 3.5 ng/mL. Moreover, the kinetic properties of carpesterol on pancreatic lipase were evaluated. Carpesterol is a competitive inhibitor and exhibited antagonistic interaction when combined with orlistat on lipase inhibition activity.
机译:肥胖通常被认为是超重或体内多余的脂肪,导致健康问题增加。肥胖是许多严重疾病的主要危险因素。据报道,通过抑制胰腺脂肪酶的活性来减少饮食中的脂肪吸收是控制肥胖的最有效方法之一。本研究旨在研究可食用植物中的脂肪酶抑制剂。从Solanum stramonifolium Jacq成熟果实的正己烷和乙酸乙酯提取物中分离出脂肪酶抑制剂。通过柱色谱法和通过光谱分析鉴定。阐明其结构为(22R)-3β-苯甲酰氧基-22-羟基-4α-甲基-5α-stigmast-7-en-6-one或carpesterol(1)。胆固醇显示出中等的脂肪酶抑制活性,IC50值为56.0μg/ mL,而众所周知的胰腺脂肪酶抑制剂奥利司他的IC50值为3.5 ng / mL。此外,评估了鲤鱼甾醇对胰腺脂肪酶的动力学性质。胆固醇是一种竞争性抑制剂,与奥利司他联用对脂肪酶的抑制活性表现出拮抗作用。

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