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 inhi...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.展开更多
文摘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.
