Screened And Conformational Relationship Study Of Active Ingredients Of Psoralea Corylifolia Based On Diacylglycerol Acyltransferase

Objective:Diacylglycerol acyltransferase（DGAT）enzyme,as the key enzyme in the Triacylglycerols（TG）synthesis pathway,plays a significant role in inhibiting obesity.Psoralea corylifolia,as a traditional Chinese medicine,not only has complex chemical components,but also has the pharmacological effects of eliminating wind and anti-freckle for external use,warming the spleen and tonifying the kidney,warming Yang and antidiarrheal and relieving asthma.The present experiment is a screened of the active ingredients of Psoralea corylifolia and their conformational relationship based on DGAT.Methods:The traditional reflux condensation technology was used to crude extract the dried seeds of Psoralea corylifolia.According to the identification of crude extract by thin layer chromatography（TLC）methods,the silica gel and RP-C18 column chromatography was selected to separate the dichloromethane layer extract with good biological activity.The obtained sub components were eluted by high performance liquid chromatograph（HPLC）with appropriate mobile phase to obtain monomer compounds.The structure of the compounds was identified by spectral analysis spectroscopic data(HRESIMS,UV,IR,~1H NMR,¹³C NMR,HMBC and NOESY).Results:Studies were obtained 10 compounds from Fr.6.3.The compounds were identified as 12α-psoracorylifol F（1）,7β,8α-hydroxy-12β-psoracorylifol F（2）,8-ketone-cyclobakuchiol C（3）,7α,8β-hydroxy-12β-cyclobakuchiol C（4）and8α-hydroxy-cyclobakuchiol C（5）,psoracorylifol F（6）,cyclobakuchiol C（7）,psoracorylifol A（8）,corypsoriol A（9）,psoracorylifol E（10）,by comparing references and spectroscopic data.Conclusion:In this experiment,ten meroterpenes were obtained from the seeds of Psoralea corylifolia,including five new meroterpenes and five known meroterpenes.All the isolates were assayed their inhibitory activity against DGAT1 using an in vitro assay with kuraridine as the positive control.Compounds 1–10 exhibited selective effects to DGAT1 in a dose-dependent manner with IC₅₀ values ranging from 61.5±1.1μM to 99.2±1.1μM.Moreover,all the isolates（1–10）were demonstrated that they have no inhibitory effects toward DGAT2 at levels of up to 200μM.