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In vitro and in vivo study of cucurbitacins-type triterpene glucoside from Citrullus colocynthis growing in Saudi Arabia against hepatocellular carcinoma

机译:在沙特阿拉伯生长的西葫芦瓜中葫芦素型三萜糖苷的抗肝细胞癌的体内外研究

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摘要

Chromatographic investigation of fruits obtained from Citrullus colocynthis, growing in Saudi Arabia, led to isolation of two compounds; Cucurbitacin E glucoside (Cu E, 1), and Cucur-bitacin I glucoside (Cu I, 2). The chemical structures of 1 and 2, were elucidated by spectroscopic analyses include; 1D (~1H and ~(13)C) and 2D (COSY, HMQC and HMBC) NMR and ESI-MS spectroscopy. The in vitro cytotoxic activity against Hepatoma Cell Line (HepG2) and mice-bearing tumor of Ehrlich's ascites carcinoma (EAC) of the compounds were estimated. Both compounds had potent inhibitory activity on HepG2 with IC_(50) 3.5 and 2.8nmol/mL, respectively. In addition to these activities, the in vivo study employing EAC, showed the capability of both compounds to prolong the survival time, life span and normalize the biochemical parameters of the infected mice with EAC.
机译:对从沙特阿拉伯生长的柑桔(Citrullus colocynthis)获得的果实进行色谱分析,结果分离出两种化合物。葫芦素E糖苷(Cu E,1)和葫芦素B糖苷I(Cu I,2)。通过光谱分析阐明了1和2的化学结构,包括: 1D(〜1H和〜(13)C)和2D(COSY,HMQC和HMBC)NMR和ESI-MS光谱。估计了该化合物对肝癌细胞系(HepG2)和荷瘤小鼠腹水癌(EAC)的体外细胞毒活性。两种化合物均具有对HepG2的有效抑制活性,分别为IC_(50)3.5和2.8nmol / mL。除这些活性外,采用EAC的体内研究表明,这两种化合物都能延长被EAC感染的小鼠的存活时间,寿命并使其生化参数正常化。

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  • 来源
    《Environmental toxicology and pharmacology》 |2012年第2期|p.245-251|共7页
  • 作者单位

    Department of Chemistry, Faculty of Science, King Abdulaziz University, P.O. Box 80203, Jeddah 21589, Saudi Arabia,Department of Chemistry, Faculty of Science, Mansoura University, New Damietta, Egypt;

    Department of Health Information Technology, Jeddah Community College, King AbdulAziz University, P.O. Box 80283, Jeddah 21589,Saudi Arabia,Department of Pharmacognosy, Faculty of Pharmacy, Minia University, Minia 61519, Egypt;

    Department of Marine Chemistry, Faculty of Marine Sciences, King Abdulaziz University, P.O. 80207, Jeddah 21589, Saudi Arabia;

    Department of Physiology and Pharmacology 'V. Erspamer', Sapienza University of Rome, Rome, Italy;

    Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt;

    Department of Chemistry, Faculty of Science, King Abdulaziz University, P.O. Box 80203, Jeddah 21589, Saudi Arabia;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

    cucurbitacins; citrullus colocynthis; cucurbitaceae HepG2; EAC; anticancer;

    机译:葫芦素;柑桔葫芦科HepG2;EAC;抗癌药;

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