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在沙特阿拉伯生长的苦瓜中的葫芦素型三萜糖苷的体外和体内研究对肝癌的作用。

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

机构信息

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

出版信息

Environ Toxicol Pharmacol. 2012 Mar;33(2):245-51. doi: 10.1016/j.etap.2011.12.010. Epub 2011 Dec 16.

Abstract

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 Cucurbitacin I glucoside (Cu I, 2). The chemical structures of 1 and 2, were elucidated by spectroscopic analyses include; 1D ((1)H 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 2.8 nmol/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.

摘要

对在沙特阿拉伯生长的苦瓜果实进行色谱分析,导致分离出两种化合物;葫芦素 E 苷(CuE,1)和葫芦素 I 苷(CuI,2)。通过光谱分析,包括 1D((1)H 和(13)C)和 2D(COSY、HMQC 和 HMBC)NMR 和 ESI-MS 光谱,阐明了 1 和 2 的化学结构。测定了化合物对肝癌细胞系(HepG2)和艾氏腹水癌(EAC)荷瘤小鼠的体外细胞毒性活性。两种化合物对 HepG2 均具有较强的抑制活性,IC50 分别为 3.5 和 2.8 nmol/mL。除了这些活性之外,体内研究采用 EAC 表明,两种化合物均能够延长感染 EAC 的小鼠的存活时间、寿命并使感染小鼠的生化参数正常化。

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