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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Polyphenolic compounds with anti-tumour potential from Corchorus olitorius (L.) Tiliaceae, a Nigerian leaf vegetable
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Polyphenolic compounds with anti-tumour potential from Corchorus olitorius (L.) Tiliaceae, a Nigerian leaf vegetable

机译：尼日利亚叶菜Corcorrus olitorius（L.）Tiliaceae的具有抗肿瘤潜力的多​​酚化合物

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摘要

Chromatographic fractionation of the methanolic extract of Corchorus olitorius (L.) (Tiliaceae), on silica gel yielded two polyphenolic compounds. The structures of the compounds were elucidated as Methyl-1,4,5-tri-O-caffeoyl quinate and trans-3-(4-Hydroxy-3-methoxyphenyl)acrylic anhydride, based on extensive use of spectroscopic techniques such as H-1 and C-13 NMR, DEPT and 2D NMR experiments (COSY, HSQC, HMBC), IR and MS. To establish an initial proof-of-concept for the biological relevance of these compounds, their cytotoxicity against the cancer cell lines HeLa, HL460 and PC3, which might indicate their anti-tumour potential, was assessed. The compounds when tested at a range of concentrations up to 1.6 mM were found to possess mild cytotoxic activity which was significant against HeLa cells at >= 800 mu M. The trans-3-(4-Hydroxy-3-methoxyl phenyl)acrylic anhydride was found to be related to curcumin, a compound known to have anti-cancer activity. Docking of each of the two compounds and also of curcumin into some molecular targets implicated in tumourigenesis revealed that the three compounds had binding affinities that were superior to those obtained for the co-crystallized inhibitors of metalloproteinase-9, fibroblast growth factor receptor 2 (FGFR2) and epidermal growth factor receptor (EGFR). The plant Corchorus olitorius therefore represents a potential source of natural 'lead' compounds with anti-tumour potential. (C) 2016 Elsevier Ltd. All rights reserved.
机译：在硅胶上色谱分离Corcorrus olitorius（L.）（Tiliaceae）的甲醇提取物，得到两种多酚化合物。基于广泛使用的光谱技术，例如H-，阐明了化合物的结构为-1,4,5-三-O-咖啡酰奎尼酸甲酯和反式-3-（4-羟基-3-甲氧基苯基）丙烯酸酐1和C-13 NMR，DEPT和2D NMR实验（COSY，HSQC，HMBC），IR和MS。为了建立这些化合物的生物学相关性的初步概念验证，评估了它们对癌细胞系HeLa，HL460和PC3的细胞毒性，这可能表明它们具有抗肿瘤潜力。当在高达1.6 mM的浓度范围内进行测试时，发现该化合物具有温和的细胞毒活性，在> = 800μM时对HeLa细胞具有显着的活性。反式3-（4-羟基-3-甲氧基苯基）丙烯酸酐被发现与姜黄素有关，姜黄素是一种已知具有抗癌活性的化合物。将这两种化合物以及姜黄素分别对接至一些涉及肿瘤发生的分子靶标中，发现这三种化合物的结合亲和力优于金属蛋白酶-9，成纤维细胞生长因子受体2（FGFR2）的共结晶抑制剂所获得的结合亲和力。 ）和表皮生长因子受体（EGFR）。因此，植物Corchorus olitorius代表了具有抗肿瘤潜力的天然“铅”化合物的潜在来源。 （C）2016 Elsevier Ltd.保留所有权利。

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