Isolation and structural elucidation of cytotoxic compounds from the root bark of Diospyros quercina (Baill.) endemic to 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]Antananarivo Poly-technique High School,University of Antananarivo,101 Antananarivo,Madagascar [4]Department of Organic Chemistry,Faculty of Sciences,P.O.Box 906 University of Antananarivo,101 Antananarivo,Madagascar [5]Institute of Natural Products Chemistry,National Centre,for Scientific Research CNRS 91198,Gif Sur Yvette-Paris,France [6]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》2014年第3期169-175,共7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 (IFS,Stockholm,Sweden) and the Organizationfor the Prohibition of Chemical Weapons(OPCW)(IFS Research Grant No F/4921-2)

摘　　要：Objective:To isolate and characterize the cytotoxic compounds from Diospyros quercina(Baill.)G.E.Schatz&Lowry(Ebenaceae).Methods:An ethno-botanical survey was conducted in the south of Madagascar from July to August 2010.Bio-guided fractionation assay was carried out on the root bark of Diospyros quercina,using cytotoxicity bioassay on murine P388 leukemia cell lines as model.The structures of the cytotoxic compounds were elucidated by 1D and 2D NMR spectroscopy and mass spectrometry.Results:Biological experiments resulted in the isolation of three bioactive pure compounds(named TR-21,TR-22,and TR-23)which exhibited very good in vitro cytotoxic activities with the IC_(50)values of(0.017 5±0.0060)μg/mL,(0.089±0.005)μg/mL and(1.027±0.070)μg/mL respectively.Thus,they support the claims of traditional healers and suggest the possible correlation between the chemical composition of this plant and its wide use in Malagasy folk medicine to treat cancer.Conclusions:The ability of isolated compounds in this study to inhibit cell growth may represent a rational explanation for the use of Diospyros quercina root bark in treating cancer by Malagasy traditional healers.Further studies are,therefore,necessary to evaluate the in vivo antineoplastic activity of these cytotoxic compounds as effective anticancer drugs.Objective:To isolate and characterize the cytotoxic compounds from Diospyros quercina（Baill.）G.E.Schatz&Lowry（Ebenaceae）.Methods:An ethno-botanical survey was conducted in the south of Madagascar from July to August 2010.Bio-guided fractionation assay was carried out on the root bark of Diospyros quercina,using cytotoxicity bioassay on murine P388 leukemia cell lines as model.The structures of the cytotoxic compounds were elucidated by 1D and 2D NMR spectroscopy and mass spectrometry.Results:Biological experiments resulted in the isolation of three bioactive pure compounds（named TR-21,TR-22,and TR-23）which exhibited very good in vitro cytotoxic activities with the IC50values of（0.017 5±0.0060）μg/mL,（0.089±0.005）μg/mL and（1.027±0.070）μg/mL respectively.Thus,they support the claims of traditional healers and suggest the possible correlation between the chemical composition of this plant and its wide use in Malagasy folk medicine to treat cancer.Conclusions:The ability of isolated compounds in this study to inhibit cell growth may represent a rational explanation for the use of Diospyros quercina root bark in treating cancer by Malagasy traditional healers.Further studies are,therefore,necessary to evaluate the in vivo antineoplastic activity of these cytotoxic compounds as effective anticancer drugs.

关 键 词：DIOSPYROS quercinia Cytotoxic activities Isodiospyrin 6’-Ethoxy-1’ 3’-dihydroxy-4 6-dimethyl-1 2’-binaphthyl-2 5’3 8’tetraones (E)-5 6-Dimethyl-2-(2-methyl-3-(prop-1-enyl) phenyl)-2H-Chromene Madagascar 

分 类 号：S567.19[农业科学—中草药栽培]