The unusual fused b-lactone vibralactone was isolated from cultures of the basidiomycete Boreostereum vibrans and has been shown to significantly inhibit pancreatic lipase.In this study,a structure-based lead optimiza...The unusual fused b-lactone vibralactone was isolated from cultures of the basidiomycete Boreostereum vibrans and has been shown to significantly inhibit pancreatic lipase.In this study,a structure-based lead optimization of vibralactone resulted in three series of 104 analogs,among which compound C1 exhibited the most potent inhibition of pancreatic lipase,with an IC50 value of 14 nM.This activity is more than 3000-fold higher than that of vibralactone.The effect of compound C1 on obesity was investigated using high-fat diet(HFD)-induced C57BL/6 J obese mice.Treatment with compound C1 at a dose of 100 mg/kg significantly decreased HFD-induced obesity,primarily through the improvement of metabolic parameters,such as triglyceride levels.展开更多
Objective:To evaluate the antioxidant potential and pancreatic lipase inhibitory action of optimized hydroethanolic extracts of Solanum nigrum.Methods:Optimized extraction for maximum recovery of metabolites was perfo...Objective:To evaluate the antioxidant potential and pancreatic lipase inhibitory action of optimized hydroethanolic extracts of Solanum nigrum.Methods:Optimized extraction for maximum recovery of metabolites was performed using a combination of freeze-drying and ultrasonication followed by determination of antioxidant and antiobesity properties.The ultra-high performance liquid chromatography equipped with mass spectrometry was used to analyze metabolite profiling of Solanum nigrum.Computational studies were performed using molecular docking and electrostatic potential analysis for individual compounds.The hypolipidemic potential of the most potent extract was assessed in the obese mice fed on fat rich diet.Results:The 80%hydroethanolic extract exhibited the highest extract yield,total phenolic contents,total flavonoid contents along with the strongest 2,2-diphenyl-1-picrylhydrazyl scavenging activity,total antioxidant power,and pancreatic lipase inhibitory properties.The 80%hydroethanolic extract not only regulated the lipid profile of obese mice but also restricted the weight gain in the liver,kidney,and heart.The 80%hydroethanolic extract also reduced alanine transaminase and aspartate transaminase concentrations in serum.The effects of plant extract at 300 mg/kg body weight were quite comparable with the standard drug orlistat.Conclusions:Solanum nigrum is proved as an excellent and potent source of secondary metabolites that might be responsible for obesity mitigation.展开更多
Background:Over the years,there has been research on the anti-obesity effect of the Allium cepa bulb,but a dearth of research was carried out on the leaves,which is consumed as vegetable salad and soup,hence this stud...Background:Over the years,there has been research on the anti-obesity effect of the Allium cepa bulb,but a dearth of research was carried out on the leaves,which is consumed as vegetable salad and soup,hence this study was proposed.Objective:This study aims at investigating the effect of A.cepa leaves on high fat diet(HFD)induced obesity in male Wistar rats.Methods:Twenty-eight male Wistar rats were divided into four groups with seven rats each.Apart from Group 1(normal control which received normal pelleted diet),obesity was induced in 21 rats of Group 2 to 4 with HFD.Group 2,the obese control was administered with 100%HFD,while the diet for group 3 and 4 was supplemented with 10%and 20%A.cepa powdered leaves,respectively,for 28 days.Results:In the rats treated with 10%and 20%A.cepa,body weight,fat mass,blood glucose,total cholesterol,triglycerides,aspartate amino transferase,alanine amino transferase,creatinine and urea levels were reduced significantly(P<0.05)in comparison with the obese control group.The liver of the rats treated with 10%and 20%A.cepa leaves revealed small and few amounts of fat deposits in comparison with the obese control group,which revealed numerous and large deposits of fat.The kidney of the rats treated with 10%and 20%A.cepa leaves showed moderate and mild inflammation,respectively,in comparison with the obese control group which showed acute inflammation.The leaves of A.cepa had antioxidant properties and the presence of volatile compounds with anti-obesity properties in A.cepa were identified using gas chromatography-mass spectrometry(GC-MS).Conclusion:A.cepa leaves had weight-loss effect in that it decreased body weight,fat mass,glucose and lipid levels including fat deposits in the liver.展开更多
基金The authors are grateful to the National Natural Science Foundation of China(81102348,U1132607,81373289).
文摘The unusual fused b-lactone vibralactone was isolated from cultures of the basidiomycete Boreostereum vibrans and has been shown to significantly inhibit pancreatic lipase.In this study,a structure-based lead optimization of vibralactone resulted in three series of 104 analogs,among which compound C1 exhibited the most potent inhibition of pancreatic lipase,with an IC50 value of 14 nM.This activity is more than 3000-fold higher than that of vibralactone.The effect of compound C1 on obesity was investigated using high-fat diet(HFD)-induced C57BL/6 J obese mice.Treatment with compound C1 at a dose of 100 mg/kg significantly decreased HFD-induced obesity,primarily through the improvement of metabolic parameters,such as triglyceride levels.
文摘Objective:To evaluate the antioxidant potential and pancreatic lipase inhibitory action of optimized hydroethanolic extracts of Solanum nigrum.Methods:Optimized extraction for maximum recovery of metabolites was performed using a combination of freeze-drying and ultrasonication followed by determination of antioxidant and antiobesity properties.The ultra-high performance liquid chromatography equipped with mass spectrometry was used to analyze metabolite profiling of Solanum nigrum.Computational studies were performed using molecular docking and electrostatic potential analysis for individual compounds.The hypolipidemic potential of the most potent extract was assessed in the obese mice fed on fat rich diet.Results:The 80%hydroethanolic extract exhibited the highest extract yield,total phenolic contents,total flavonoid contents along with the strongest 2,2-diphenyl-1-picrylhydrazyl scavenging activity,total antioxidant power,and pancreatic lipase inhibitory properties.The 80%hydroethanolic extract not only regulated the lipid profile of obese mice but also restricted the weight gain in the liver,kidney,and heart.The 80%hydroethanolic extract also reduced alanine transaminase and aspartate transaminase concentrations in serum.The effects of plant extract at 300 mg/kg body weight were quite comparable with the standard drug orlistat.Conclusions:Solanum nigrum is proved as an excellent and potent source of secondary metabolites that might be responsible for obesity mitigation.
文摘Background:Over the years,there has been research on the anti-obesity effect of the Allium cepa bulb,but a dearth of research was carried out on the leaves,which is consumed as vegetable salad and soup,hence this study was proposed.Objective:This study aims at investigating the effect of A.cepa leaves on high fat diet(HFD)induced obesity in male Wistar rats.Methods:Twenty-eight male Wistar rats were divided into four groups with seven rats each.Apart from Group 1(normal control which received normal pelleted diet),obesity was induced in 21 rats of Group 2 to 4 with HFD.Group 2,the obese control was administered with 100%HFD,while the diet for group 3 and 4 was supplemented with 10%and 20%A.cepa powdered leaves,respectively,for 28 days.Results:In the rats treated with 10%and 20%A.cepa,body weight,fat mass,blood glucose,total cholesterol,triglycerides,aspartate amino transferase,alanine amino transferase,creatinine and urea levels were reduced significantly(P<0.05)in comparison with the obese control group.The liver of the rats treated with 10%and 20%A.cepa leaves revealed small and few amounts of fat deposits in comparison with the obese control group,which revealed numerous and large deposits of fat.The kidney of the rats treated with 10%and 20%A.cepa leaves showed moderate and mild inflammation,respectively,in comparison with the obese control group which showed acute inflammation.The leaves of A.cepa had antioxidant properties and the presence of volatile compounds with anti-obesity properties in A.cepa were identified using gas chromatography-mass spectrometry(GC-MS).Conclusion:A.cepa leaves had weight-loss effect in that it decreased body weight,fat mass,glucose and lipid levels including fat deposits in the liver.
