从 L.中提取的一种新的四环三萜皂苷及其神经保护和 hMAO-B 抑制活性。
A new tetracyclic saponin from L. and its neuroprotective and hMAO-B inhibiting activity.
机构信息
Department of Pharmacognosy, Faculty of Pharmacy, Medical University of Sofia, Sofia, Bulgaria.
Department of Pharmacognosy, Institute of Pharmaceutical Sciences, University of Graz, Graz, Austria.
出版信息
Nat Prod Res. 2020 Feb;34(4):511-517. doi: 10.1080/14786419.2018.1491040. Epub 2018 Nov 23.
A new tetracyclic saponin, 17(),20()-3,6,16-trihydroxycycloartanyl-23-carboxylic acid 16-lactone 3-O--D-glucopyranoside () together with one known flavonoid, camelliaside A () were isolated from the aerial parts of L. Their structures were determined by chemical, HRESIMS and NMR methods. On 6-hydroxydopamine model on isolated rat brain synaptosomes, compounds - had statistically significant neuroprotective activity similar to that of Silibinin, tested at 100 μM. Saponin possessed the most prominent neuroprotective and antioxidant effects in this model. On human recombinant monoamine oxidase type B enzyme compound displayed strong inhibiting activity, compared to Selegiline (1 μM). It could be concluded that the new epoxycycloartane saponin could be a promising leading structure in respect of neurodegenerative diseases.
一种新的四环三萜皂苷，17（），20（）-3、6、16-三羟基环阿尔廷基-23-羧酸 16-内酯 3-O--D-吡喃葡萄糖苷（），以及一种已知的类黄酮，山茶花苷 A（），从 L. 的地上部分分离得到。通过化学、HRESIMS 和 NMR 方法确定了它们的结构。在 6-羟多巴胺离体大鼠脑突触体模型上，化合物-具有与水飞蓟素相似的统计学显著神经保护活性，在 100μM 下进行测试。在该模型中，皂苷具有最显著的神经保护和抗氧化作用。与 1μM 的Selegiline 相比，化合物在人重组单胺氧化酶 B 酶上显示出强烈的抑制活性。可以得出结论，新的环氧环阿尔廷烷皂苷可能是治疗神经退行性疾病的有前途的先导结构。
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