cholinesterase inhibitory activities

  • 文章类型: Journal Article
    翼龙属包括26种,其中一半是关于化学成分的植物化学研究,香豆素被认为是该属中的化学分类学标记。这里是紫茎叶翅目DC(菊科),一种来自巴西的本地植物,这是第一次被调查。26个化合物从沙棘DC的地上部分分离。,是5种三萜,4种植物甾醇,9类黄酮,3酚酸,5香豆素此外,通过UHPLC-HRMS/MS使用去复制技术推定鉴定了总共177个化合物,超过50%对应于类黄酮和香豆素。尽管已经在Pterocaulon属中报道了41种不同的香豆素,在这项研究中首次发现了16个。还进行了生物学研究,二氯甲烷部分是抗增殖评价中最活跃的部分,抗氧化剂,抗菌和胆碱酯酶抑制活性。
    Pterocaulon genus comprises 26 species, half of them have been phytochemical investigations regarding the chemical composition, and coumarins have been considered the chemotaxonomic markers in the genus. Herein Pterocaulon angustifolium DC (Asteraceae), a native plant from Brazil, is investigated for the first time. Twenty-six compounds were isolated from aerial parts of P. angustifolium DC., being 5 triterpenes, 4 phytosterols, 9 flavonoids, 3 phenolic acids, and 5 coumarins. Moreover, a total of 177 compounds were putatively identified using the dereplication technique by UHPLC-HRMS/MS, more than 50% correspond to flavonoids and coumarins. Although 41 different coumarins have already been reported in Pterocaulon genus, 16 were identified for the first time in this study. Crude ethanolic extract and fractions of P. angustifolium were also biologically investigates, and dichloromethane fraction was the most active fraction in the evaluation of antiproliferative, antioxidant, antimicrobial and cholinesterase inhibitory activities.
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  • 文章类型: Journal Article
    在这项研究中,从Picrasmaquassioides的叶子中分离出八种新的天然产物。光谱技术用于阐明其平面结构。根据电子圆二色性(ECD)技术结合2,3-二氢苯并呋喃发色团的P/M螺旋度规则,阐明了它们的绝对构型,和糖水解。胆碱酯酶抑制剂通常用作阿尔茨海默病抑制剂。因此,对这8个化合物的乙酰胆碱酯酶和丁酰胆碱酯酶抑制活性进行了测试,结果表明,只有化合物6显示出弱的乙酰胆碱酯酶抑制活性。特别是,分子对接用于说明化合物6与AChE活性位点之间的结合。
    In this study, eight new natural products were isolated from the leaves of Picrasma quassioides. Spectroscopic techniques were used for the elucidation of their planar structures. Their absolute configurations were elucidated on the basis of electron circular dichroism (ECD) techniques combined with the P/M helicity rule for the 2,3-dihydrobenzofuran chromophore, and saccharide hydrolysis. Cholinesterase inhibitors are often used as Alzheimer\'s disease inhibitors.Thus, acetylcholinesterase and butyrylcholinesterase inhibitory activity of these eight compounds were tested, and results showed that only compound 6 showed weakly acetylcholinesterase inhibitory activity. In particular, molecular docking was used to illustrate the bindings between compound 6 and the active sites of AChE.
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