Studies On New Compounds Obtained From Psoralea Corylifolia And Their Biological Activities

Objective:Psoralea corylifolia,as a traditional Chinese folk medicine,has many pharmacological activities,including anti obesity,anti-tumor,anti-inflammatory,and antioxidant activities.The aim of this experiment is to isolate the active components of anti obesity from natural plant P.corylifolia.Determine the structure of the compound in the active site.Study the inhibitory activity of all compounds on obesity related target proteins,and discuss the impact of structural differences between different compounds on the inhibitory activity differences of target proteins.Methods:This experiment used 85.0%ethanol to preliminarily heat and reflux extract the seeds of P.corylifolia.The crude extracts of P.corylifolia seeds were extracted using n-hexane,n-butanol,ethyl acetate,and water,respectively.Detect the effects of four extracts on diacylglycerol transferase（DGAT）,protein tyrosine phosphatase 1B（PTP1B）,andα-glucosidase.By using column chromatography and semi preparative high-performance liquid chromatography,the ethyl acetate extract was further separated and purified to obtain natural anti obesity and anti hyperlipidemic compounds.Determine the structure of the compound through nuclear magnetic dat a and references.Detect the inhibitory activity of all compounds for DGAT,PTP1B,andα-glucosidase.Results:The anti obesity active ingredient PCE2 was isolated and purified.After analyzing data such as nuclear magnetic resonance(¹H-NMR,¹³C-NMR,HMBC,HMQC,NOESY,and ¹H-¹HCOSY),infrared,and ultraviolet,it is determinedas follows:4,2’,3’-trihydroxy-4’-（2’’β-hydroxy-3’’-methybult-3’’-enyl）chalcone（1）,4,2’,3’-trihydroxy-4’-（2’’α-hydroxy-3’’-methybult-3’’-enyl）chalcone（2）,4,2’-dihydroxy-4’-methoxy-5’-（2’’β-hydroxy-3’’-methybult-3’’-enyl）chalcone（3）,4,2’,4’-trihydroxy-3’-（2’’α-3’’-dihydroxy-3’’-dimethybult）chalcone（4）,4,2’,4’-trihydroxy-3’-（2’’β-3’’-dihydroxy-3’’-dimethybult）chalcone（5）,4-hydroxy-3’,4’-（2’’α-3’’-hydroxy-3’’-dimethybult）furano-chalcone（6）,4,2’,3’-trihydroxy-4’-methoxy-5’-（2’’β-hydroxy-3’’-methoxy-3’’-dimethybult）-chalcone（7）,4,2’,3’-trihydroxy-4’-prenyl-chalcone（8）,2（S）-4’-hydroxy-6-methoxy-7-（2’’-carbanyl-3’’-methybult-3’’enyl）Flavanone（9）,6-hydroxy-7-prenyl-coumarin（10）,7α,8α,12α-Psoracorylifol A（11）,7α,8α,12β-Psoracorylifol A（12）,7α,8β,12α-Psoracorylifol A（13）.Among them,compounds 1-4,7-13have a selective inhibitory effect on DGAT1(IC ₅₀:67.1±1.2～109.2±1.3μM)Compounds 1,8,and 10 have a good inhibitory effect on PTP1B(IC₅₀:13.8±1.1～19.1±1.6μM),Compound 1-10 pairsα-Glucosidase has a certain inhibitory effect(IC ₅₀:29.1±1.2～79.4±1.2μM)。Conclusion:A total of 13 new compounds were obtained,including 8 chalcone compounds,3 psoralen derivatives,1 dihydroflavone skeleton compound,and 1coumarin compound.All compounds were detected for DGAT,PTP1B,andα-Inhibitory activity of glucosidase.This study provides a potential guidance method for the rational development of psoralen and the industrialization of psoralen food and health products in the future,as well as a theoretical data basis for the subsequent modification and synthesis of targeted compounds.