Objective:To validate scientifically the traditional use of Salacia leptoclada Tul.(Celastraceae)(S.leptoclada)and to isolate and elucidate the structure of the biologically active compound.Methods:Bioassay-guided fra...Objective:To validate scientifically the traditional use of Salacia leptoclada Tul.(Celastraceae)(S.leptoclada)and to isolate and elucidate the structure of the biologically active compound.Methods:Bioassay-guided fractionation of the acetonic extract of the stem barks of S.leptoclada was carried out by a combination of chromatography technique and biological experiments in viro using Plasmodium falciparum and P388 leukemia cell lines as models.The structure of the biologically active pure compound was elucidated by 1D and 2D NMR spectroscopy and mass spectrometry.Results:Biological screening of S.leptoclada extracts resulted in the isolation of a pentacyclic triterpenic quinone methide.The pure compound exhibited both in vitro a cytotoxic effect on murine P388 leukemia cells with IC_(50)value of(0.041±0.020)μg/mL and an antiplasmodial activity against the chloroquine-resistant strain FC29 of Plasmodium falciparum with an IC_(50)value of(0.052±0.030)μg/mL.Despite this interesting anti-malarial property of the lead compound,the therapeutic index was weak(0.788).In the best of our knowledge,the quinone methide pentacyclic triterpenoid derivative compound is reported for the first time in S.leptoclada.Conclusions:The results suggest that furthers studies involving antineoplastic activity is needed for the development of this lead compound as anticancer drug.展开更多
基金Supported by the Third World Academy of Science(TWAS)Fellowship for Research and Advanced Training FR number:Grant No.3240224121the International Foundation for Science dFS,Stockholm.Swedem and the Organization for the Prohibition of Chemical Weapons(OPCW)dFS Research Grant No.F/4921-2)
文摘Objective:To validate scientifically the traditional use of Salacia leptoclada Tul.(Celastraceae)(S.leptoclada)and to isolate and elucidate the structure of the biologically active compound.Methods:Bioassay-guided fractionation of the acetonic extract of the stem barks of S.leptoclada was carried out by a combination of chromatography technique and biological experiments in viro using Plasmodium falciparum and P388 leukemia cell lines as models.The structure of the biologically active pure compound was elucidated by 1D and 2D NMR spectroscopy and mass spectrometry.Results:Biological screening of S.leptoclada extracts resulted in the isolation of a pentacyclic triterpenic quinone methide.The pure compound exhibited both in vitro a cytotoxic effect on murine P388 leukemia cells with IC_(50)value of(0.041±0.020)μg/mL and an antiplasmodial activity against the chloroquine-resistant strain FC29 of Plasmodium falciparum with an IC_(50)value of(0.052±0.030)μg/mL.Despite this interesting anti-malarial property of the lead compound,the therapeutic index was weak(0.788).In the best of our knowledge,the quinone methide pentacyclic triterpenoid derivative compound is reported for the first time in S.leptoclada.Conclusions:The results suggest that furthers studies involving antineoplastic activity is needed for the development of this lead compound as anticancer drug.
