Preparation of AChE Inhibitors From Jujubogenin

A dammarane derivative dihydrojujubogenin-2-en-1-one, which possesses a skeleton and pharmacophore partially similar to those of Territrem B, a potent AChE inhibitor, was synthesized via three different paths. The anti-AChE activity of this compound and related analogue was measured.

Synthesis of 2-En-1-one-ebelactonyl Benzoates of Territrem B Analogues from Jujubogenin

Two series of territrem B analogues (10a-10c and 18) have been designed and synthesized from jujubogenin 5a which was prepared from jujubogenin glycosides 5b obtained from the leaves of Zizyphus jujuba. The structures of the new compounds were confirmed by H-, 1 13C-NMR and MS data. Compounds 10c and 18 showed weak inhibitory effect on AChE at 10-4 mol/L.

枳椇子促智活性成分研究

目的:研究枳椇子的促智活性成分。方法:从枳椇子中分离出6个皂苷类成分,以跳台法测试小鼠的记忆功能。实验装置为小鼠跳台反应箱,测试小鼠触电潜伏期及其3 min内错误次数作为记忆功能评价指标。将小鼠分为青年组、老年组、老年加吡拉西坦组(剂量0.3 g/kg)和老年加枳椇子总皂苷高、中、低3个剂量组(0.6、0.3、0.15 g/kg)等,研究皂苷类成分对老龄小鼠学习和记忆的影响。另将小鼠随机分为空白组、模型组、吡拉西坦组(剂量0.3 g/kg)和老年加化合物3、4、5、6(剂量均为0.3 g/kg)等,研究对由东莨菪碱、亚硝酸钠、40%乙醇分别所致记忆获得、巩固及再现障碍的影响。结果:6个皂苷类成分其化学结构经光谱鉴定分别为3-O-豆甾醇-(6-棕榈酰基)-β-D-吡喃葡萄糖苷(1)、β-胡萝卜苷(2)、hovenidulciosideA1(3)、hoduloside I(4)、hodulosideⅣ(5)、saponins C2(6)。其中,化合物1、2为首次从该植物中分离得到;化合物5、6能增强自然衰老小鼠的学习和记忆能力,并对由东莨菪碱、亚硝酸钠和40%乙醇分别引起的小鼠记忆获得、巩固及再现障碍病理模型有较明显的改善作用。结论:枳椇子酸枣仁皂苷元类皂苷可能是枳椇子总皂苷促智活性的物质基础。

A new tnterpenoid saponin from Bacopa monniera

A new triterpenoid saponin, bacopaside IX, was isolated from the whole plant of Bacopa monniera （L.） Wettst. and its structure was elucidated as 3-O-{β-d-glucopyranosyl（1 → 4）[α-1-arabinofuranosyl-（1 → 2）]-β-d-glucop-yranosyl}-20-O-α-1-arabinopyranosyljujubogenin by spectroscopic methods and some chemical transformations.