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

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

首页> 外文期刊>亚太热带生物医学杂志（英文版） >Antiplasmodial, cytotoxic activities and characterization of a new naturally occurring quinone methide pentacyclic triterpenoid derivative isolated from Salacia leptoclada Tul. (Celastraceae) originated from Madagascar

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

机译：分离自Salacia leptoclada Tul的一种新的天然存在的甲基苯醌甲基化物五环三萜衍生物的抗血浆，细胞毒活性和特征。（Celastraceae）起源于马达加斯加

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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 IC50 value of (0.041±0.020) µg/mL and an antiplasmodial activity against the chloroquine-resistant strain FC29 of Plasmodium falciparum with an IC50 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.

机译：目的：科学验证Salacia leptoclada Tul的传统用法。（Celastraceae）（S. leptoclada）并分离和阐明生物活性化合物的结构。方法：以恶性疟原虫和P388白血病细胞系为模型，结合色谱技术和体外生物学实验，通过生物学方法指导分离钩端螺旋体茎皮的丙酮提取物。通过1D和2D NMR光谱学和质谱法阐明了生物活性纯化合物的结构。结果：对S. leptoclada提取物进行生物学筛选，分离出五环三萜醌甲基化物。该纯化合物在体外对鼠P388白血病细胞表现出细胞毒性作用，IC50值为（0.041±0.020）µg / mL，并且对恶性疟原虫的耐氯喹菌株FC29具有抗血浆活性，IC50值为（0.052±0.030））µg / mL。尽管前导化合物具有这种有趣的抗疟疾特性，但治疗指数仍然很弱（0.788）。据我们所知，首次在鳞翅目沙门氏菌中报道了甲基苯醌五环三萜类化合物。结论：结果表明，涉及抗肿瘤活性的进一步研究对于开发这种作为抗癌药物的先导化合物是必要的。

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《亚太热带生物医学杂志（英文版）》 |2013年第10期|780-784|共5页
作者
Fatiany Pierre Ruphin; Robijaona Baholy; Randrianarivo Emmanuel; Raharisololalao Amelie; Marie-Therese Martin; Ngbolua Koto-te-Nyiwa;
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Department of 0rganic Chemistry, Faculty of Sciences, P.0. Box 187, University of Toliara, 601 Toliara Madagascar;

Malagasy Institute of Applied Research, Avarabohitra Itaosy lot AVB 77, P. 0. B0X 3833, 102 Antananarivo Madagascar;

Malagasy Institute of Applied Research, Avarabohitra Itaosy lot AVB 77, P. 0. B0X 3833, 102 Antananarivo Madagascar;

Department of 0rganic Chemistry, Faculty of Sciences, P.0. Box 906 University of Antananarivo, 101Antananarivo, Madagascar;

Institute of Natural Products Chemistry, National Centre for Scientific Research CNRS 91198, Gif Sur Yvette-Paris, France;

Department of Biology, Faculty of Science, University of Kinshasa, P.0. B0X 190 Kinshasa XI, Democratic Republic of the Congo;

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

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