Study On The Inhibition Activity Of Lipase In Six Chinese Medicine Activity Components

Objective:obesity has gradually become one of the biggest threats to human health in this century,it is high blood pressure,coronary heart disease,stroke and cancer?thymic carcinoma,colon?and blood lipid abnormalities disease leading cause of the disease,inhibit the activity of digestive enzymes in the digestive tract,is currently the most common method used for the prevention and treatment of obesity,pancreatic lipase plays a key role in the fat hydrolysis,natural source of traditional Chinese medicine?TCM?pancreatic lipase inhibitor has the characteristics of low toxicity,high efficiency,less side effects,so from natural Chinese medicine screening has inhibition of pancreatic lipase,the active ingredient,and through structural modification to improve its bioavailability,has been becoming the current hot direction of the drug to lose weight.In this paper,study on several different types of traditional Chinese medicine monomer compounds pancreatic lipase inhibition rate,and the inhibition effect of ursolic acid good triterpene compounds studied the modification of structure and lipase inhibitory activity,hope that this study on weight loss drug development to lay a certain foundation.Methods:using the nitrophenol method with orlistat for positive reference substance,with pancreatic lipase model selection has the inhibitory activity of monomer compounds,respectively,to join the corresponding amount,reaction substrates?p-nitrophenyl palmitate solution?,inhibitors?This study is to select curcumin,double hydrogen arbutus element,mangiferin,rhein,trans ferulic acid,vanillic acid,vanillin,ursolic acid and oleanolic acid and ursolic acid product ursolic acid methyl ester,the modified version of ursolic acid ethyl ester,ursolic acid,n-propyl,ursolic acid isopropyl ester,ursolic acid benzyl ester,ursolic acid sodium salt,2-acetyl ursolic acid methyl ester,ethyl 2-acetyl ursolic acid mixture inhibitor solution,respectively?,Tris HCl,pig pancreatic lipase solution reaction buffer in 96-well plates,and in 37?,under the absorption wavelength of 405 nm measure its absorbance value,calculate the pancreatic lipase inhibition rate.Results:orlistat had a strong inhibitory activity of pancreatic lipase with an IC₅₀ value of 65.23nM,and curcumin and arbutin had a strong inhibitory activity of pancreatic lipase,with an IC₅₀ value of 61.95?M and142.76?M.The inhibitory activity of oleanolic acid and dihydromyricetin was not obvious,and the inhibition rate of pancreatic lipase was less than 30%at high concentration.Mangiferin,rhubarb,antiferulic acid,vanillin and vanillin have little inhibitory activity on pancreatic lipase,and the inhibition rate of pancreatic lipase is less than 10%at high concentration.The inhibitory effect of each monomer compound on pancreatic lipase was the best at pH8.0,and the inhibition rate stabilized after 10min.Ursolic acid methyl ethyl,ursolic acid,ursolic acid,acrylic ester,ursolic acid isopropyl ester,ursolic acid sodium salt of inhibition of pancreatic lipase activity and ursolic acid,the IC₅₀alue concentration of 142.05?M,respectively,138.95?M,139.33?mol,138.19?M,140.08?M,2-acetyl ursolic acid methyl ester,ethyl 2-acetyl ursolic acid on inhibition of pancreatic lipase activity weaker than ursolic acid,the IC₅₀ alue concentration of 185.57?M,respectively,186.6?M,ursolic acid benzyl ester on the inhibition of pancreatic lipase activity stronger than ursolic acid,the IC₅₀ alue concentration of 79.9?M.The inhibitory effect of ursolic acid derivatives on pancreatic lipase was the best at pH8.0,and the inhibition rate stabilized after 10min.Conclusion:curcumin is a basic heating under the condition of easy to decompose compounds,ursolic acid is a kind of structure stability of pentacyclic triterpene compound,the inhibition of pancreatic lipase has a significant effect of IC₅₀ were 61.95?M,142.76?M,.Though ursolic acid structure modification and testing the lipase inhibited activity,the results show that ursolic acid C-28 introduction of straight chain derivative inhibition rate of pancreatic lipase there won't be promoted,C-3 a certain degree of acyl inhibition rate was lower,The inhibition rate of pancreatic lipase was increased by the introduction of C-28 side chains with benzene ring.