Antiplasmodial,cytotoxic activities and characterization of a new naturally occurring quinone methide pentacyclic triterpenoid derivative isolated from Salacia leptoclada Tul.(Celastraceae)originated from Madagascar  

作　　者：Fatiany Pierre Ruphin Robijaona Baholy Randrianarivo Emmanuel Raharisololalao Amelie Marie-Therese Martin Ngbolua Koto-te-Nyiwa 

机构地区：[1]Department of Organic Chemistry,Faculty of Sciences,P.O.Box 187.University of Toliara,601 Toliara Madagascar [2]Malagasy Institute of Applied Research,Avarabohitra Itaosy lot AVB 77.P.O.BOX 3833,102 Antananarivo Madagascar [3]Department of Organic Chemistry,Faculty of Sciences,P.O.Box 906 University of Antananarivo,101 Antananarivo,Madagascar [4]Institute of Natural Products Chemistry,National Centre for Scientific Research CNRS 91198,Gif Sur Yvette-Paris,France [5]Department of Biology,Faculty of Science,University of Kinshasa,P.O.BOX 190 Kinshasa XI,Democratic.Republic of the Congo

出　　处：《Asian Pacific Journal of Tropical Biomedicine》2013年第10期780-784,共5页亚太热带生物医学杂志（英文版）

基　　金：Supported by the Third World Academy of Science(TWAS)Fellowship for Research and Advanced Training FR number:Grant No.3240224121;the International Foundation for Science dFS,Stockholm.Swedem and the Organization for the Prohibition of Chemical Weapons(OPCW)dFS Research Grant No.F/4921-2)

摘　　要：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.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 IC50value of（0.041±0.020）μg/mL and an antiplasmodial activity against the chloroquine-resistant strain FC29 of Plasmodium falciparum with an IC50value 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.

关 键 词：Salacia leptoclada QUINONE methide MALARIA THERAPEUTIC index Cancer Madagascar 

分 类 号：R285[医药卫生—中药学]