Studies On The Chemical Constituents And Pharmacological Activities Of The Fruits Of Xanthium Italicum Moretti

Objective:Xanthium italicum Moretti is a genus of（Xanthium L.）.As an alien invasive plant,it has been widely distributed in China.To clarify active substance basis of Xanthium italicum Moretti and further develop of its potential effective medicinal constituents.Base on our early stage of the research study,we continue analysis and research Xanthium italicum Moretti ethyl acetate extract of fruit.Chemical composition and pharmacological activities of monomer compounds were isolated from research in order to provide theoretical base of the plant resources development and utilization.Methods:The traditional column chromatography method（chromatographic packing:hydroxypropyl glucangel,polyamide,silica,etc.）and half prepared HPLC separation method（chromatographic column:YMC Pack ODS-A columns and Chiral CD-Ph S5 Chiral chromatographic column）for Xanthium italicum Moretti and through isolation and purification of ethyl acetate extracts of spectroscopy method.We use chemical methods and spectroscopic analysis to determine the structure of the compound,and test their cytotoxic,anti-inflammatory and analgesic activity.Results:A total of 53 compounds were isolated from the ethyl acetate extract of Xanthium italicum Moretti fruit,including 10 new compounds,5 sesquiterpenes,3 glycosides and 2phenylpropanoids.The compounds were sesquiterpenes,phenylpropanoids and phenolic acids.The new compounds CRZ-11 and CRZ-39 showed analgesic activity through acetic acid writhing test in mice.The writhing inhibition rates of CRZ-11 and CRZ-39 were 80.53%and 67.89%,respectively,at 20mg/kg dose.The IC₅₀（μmol/L）values of compound CRZ-98 on human gastric cancer cell HGC27,human liver cancer cell Hep G2,human lung cancer cell A549 and human colorectal cancer cell HCT-116 for 72h were 2.06,0.72,0.1,0.87,respectively.Compound CRZ-31,CRZ-55,CRZ-63,CRZ-89 and CRZ-107inhibited LPS-induced NO production in primary mouse peritoneal macrophages at concentrations of 10^-5 M,respectively,46.53%,9.59%,4.56%,92.28%and22.32%.Conclusions:In this study,the chemical constituents of the ethyl acetate extract of Xanthium italicum Moretti fruit were studied.53 compounds were isolated and identified,among which 10 new compounds.It was speculated that Xanthiane-type sesquiterpenes were the characteristic constituents.In order to provide a theoretical basis for the study of Xanthium italicum Moretti,the pharmacological activity of the compound was screened and the material basis of its tumor suppressive,anti-inflammatory and analgesic activities was preliminary explored.