Chemical constituents of Aloe barbadensis Miller and their inhibitory effects on phosphodiesterase-4D
Chemical constituents of Aloe barbadensis Miller and their inhibitory effects on phosphodiesterase-4D
复制标题
库拉索芦荟的化学成分及其对磷酸二酯酶-4D的抑制作用
DOI：
10.1016/j.fitote.2013.08.027
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发表时间：
2013-12-01
期刊：
影响因子：
3.4
通讯作者：
Luo, Haibin
中科院分区：
文献类型：
--
作者：
Zhong, Jiasheng;Huang, Yiyou;Luo, Haibin
库拉索芦荟是一种药食两用的药用植物。为了研究海巴达的化学成分及其对磷酸二酯酶-4D(PDE4D)的抑制活性，用海巴达干粉的70%甲醇提取物进行了研究。通过植物化学研究，分离得到3个新的色酮：5-羟甲基-7-甲氧基-2-甲基色酮(4)、5-((4E)-2‘-oxo-pentenyl)-2-hydroxymethylchromone(6)和7-羟基-5-(羟甲基)-2-甲基色酮(7)，以及18个已知化合物。通过UV、IR、一维、二维核磁共振和高分辨质谱等波谱方法确定了它们的化学结构。此外，以氚标记的3‘，5’-环磷酸腺苷(H-3-cAMP)为底物评价了它们对PDE4D的抑制作用。根据反应后放射性变化计算抑制率，化合物1-4、10和21对PDE4D表现出一定的抑制活性，这可以解释海参作为抗炎药物的原因。(C)2013爱思唯尔B.V.保留所有权利。
Aloe barbadensis Mill has been used as food and medicine for a long time. In order to investigate the chemical constituents of A. barbadensis and their inhibitory activities towards phosphodiesterase-4D (PDE4D), 70% methanol extract of the dried A. barbadensis powder was employed. Phytochemical investigation has led to the isolation of three new chromones, 5-(hydroxymethyl)-7-methoxy-2-methylchromone (4), 5-((4E)-2'-oxo-pentenyl)-2-hydroxymethylchromone (6), and 7-hydroxy-5-(hydroxymethyl)-2-methylchromone (7), together with eighteen known compounds. Their chemical structures were determined based on spectroscopic methods including UV, IR, 1D and 2D NMR, and HRMS spectrometry. In addition, their inhibition against PDE4D was evaluated using tritium-labeled adenosine 3',5'-cyclic monophosphate (H-3-cAMP) as the substrate. Inhibition was calculated by the variation of radioactivity after the reaction, and compounds 1-4,10, and 21 exhibited certain inhibitory activities towards PDE4D, which can provide an explanation why A. barbadensis can serve as anti-inflammatory agents. (C) 2013 Elsevier B.V. All rights reserved.