Flavones from Heavenly Blue as modulators of Alzheimer's amyloid-beta peptide (Aβ) production
Flavones from Heavenly Blue as modulators of Alzheimer's amyloid-beta peptide (Aβ) production
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DOI：
10.1007/s00044-017-2100-x
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发表时间：
2018-03-01
影响因子：
2.6
通讯作者：
Abdalla, Mohamed M.
中科院分区：
文献类型：
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作者：
Awad, Hanem M.;Abd-Alla, Howaida I.;Abdalla, Mohamed M.
酚类成分是天蓝（Ipomoea）中存在的主要生物活性化合物。以往有关三色蕹菜植物化学和生物学研究的文献很少。从该植物的叶子中鉴定出六种化合物：大黄花苷 (1)、木犀草素-7-O-β-D-葡萄糖苷 (2)、5,7,4'-三羟基-6-甲氧基黄酮-7-O-β-d-葡萄糖苷 (3)、芹菜素 (4)、5,7-二羟基-3,3',4'-三甲氧基黄酮 (5) 和2-羟甲基氢醌-6-甲醛(6)。基于色谱、化学和光谱方法阐明了它们的结构。所有代谢物均为首次在番薯属中报道。黄酮 1、3 和 5 的体外和体内研究被评估为阿尔茨海默病淀粉样蛋白-β 肽 (Aβ) 生成的调节剂。结果表明，所有三种黄酮都能够在体外和体内调节 Aβ 浓度，而没有任何细胞毒性作用。观察到 Aβ42 分泌的剂量依赖性抑制。结果显示，这些黄酮在浓度高达 500 nM 时，对环氧合酶 (COX)-1 和 COX-2 没有抑制活性，并且伴随前列腺素合成的减少，表明 A β 42 水平的降低可能与 COX 活性无关。
Phenolic constituents are the principle bioactive compounds exist in Heavenly Blue (Ipomoea). Little was found in the literature concerning the previous phytochemical and biological studies of Ipomoea tricolor. From leaves of this plant, six compounds were identified: rhoifoloside (1), luteolin-7-O-beta-D-glucoside (2), 5,7,4'-trihydroxy-6-methoxyflavone-7-O-beta- d -glucoside (3), apigenin (4), 5,7-dihydroxy-3,3',4'-trimethoxyflavone (5), and 2-hydroxymethylhydroquinone-6-carbaldehyde (6). Their structures were elucidated on the basis of chromatographic, chemical, and spectroscopic methods. All metabolites were reported for the first time in the genus Ipomoea. In vitro and in vivo investigations of the flavones 1, 3, and 5 were assessed as modulators of Alzheimer's amyloid-beta peptide (A beta) production. The results indicated that all the three flavones were able to modulate the A beta concentration both in vitro and in vivo without any cytotoxic effect. A dose-dependent inhibition of A beta 42 secretion was observed. The results showed no inhibition activity of these flavones against cyclooxygenase (COX)-1 and COX-2 up to 500 nM concentration and concomitant reduction in prostaglandin synthesis, indicating that the reduction in A beta 42 levels may be independent of COX activity.