Department of Chemistry, Obafemi Awolowo University, Ile-Ife, Nigeria; Department of Chemistry, University of Botswana, Gaborone, Botswana.
Department of Chemistry, Obafemi Awolowo University, Ile-Ife, Nigeria.
J Ethnopharmacol. 2019 Mar 1;231:503-506. doi: 10.1016/j.jep.2018.11.009. Epub 2018 Nov 8.
Anthocleista vogelii (Planch) is used in folk medicine in conditions related to inflammation and oxidative stress. This suggests that some of its constituents could possess ability to reduce oxidative damage to cells and ameliorate inflammatory conditions which are two prominent features in the brain of a person suffering from Alzheimer's disease.
The leaf extracts were investigated for their bioactive constituents in our quest for novel compounds for the management of Alzheimer's disease.
Anthocleista vogelii crude leaf extract obtained from 80% methanol was successively partitioned with n-hexane, dichloromethane (DCM), ethyl acetate (EtOAc) and n-butanol. This gave four solvent fractions of the crude extract. These fractions and isolated compound were subjected to acetylcholinesterase (AChE) inhibitory activity test using the microplate assay method. The structure of the isolated compound was determined using spectroscopic methods (1D and 2D NMR, and MS).
The results of the acetylcholinesterase inhibitory assay revealed that n-BuOH and ethyl acetate fractions had the best activity with IC of 564.58 and 727.63 µg/mL respectively. Activity directed fractionation of each of these fractions led to the isolation of the same compound identified as a C-glucosylflavone; isovitexin-7-O-methyl ether (swertisin). This rare C-glucosylflavone co-exist as two rotamers and exhibited duplication of NMR signals. It is reported from this plant for the first time. Swertisin displayed better acetylcholinesterase inhibitory activity with IC of 32.09 µg/mL than physostigmine (eserine) with IC of 56.09 µg/mL used as a standard.
This study reports isolation and characterization of a rare C-glycosylflavone; isovitexin-7-O-methyl ether (swertisin). Isolated compound exhibited duplication of NMR signals and better acetylcholinesterase inhibitory activity than eserine used as a standard. The activity exhibited by this compound suggests that it could be useful in the management of Alzheimer's disease.
鸡骨常山（Planch）在民间医学中用于与炎症和氧化应激有关的病症。这表明其某些成分可能具有减少细胞氧化损伤和改善炎症的能力，这是阿尔茨海默病患者大脑的两个突出特征。
本研究旨在寻找治疗阿尔茨海默病的新型化合物，因此对叶片提取物进行了生物活性成分的研究。
从 80%甲醇中获得的鸡骨常山粗叶提取物，用正己烷、二氯甲烷（DCM）、乙酸乙酯（EtOAc）和正丁醇依次萃取，得到粗提取物的四个溶剂级分。将这些级分和分离的化合物用微量板法进行乙酰胆碱酯酶（AChE）抑制活性测试。通过光谱方法（1D 和 2D NMR 和 MS）确定分离化合物的结构。
乙酰胆碱酯酶抑制活性测定结果表明，n-BuOH 和 EtOAc 级分的活性最好，IC 分别为 564.58 和 727.63µg/mL。对这些级分的每一级分进行活性导向分离，得到了相同的化合物，鉴定为 C-葡萄糖基黄酮；异荭草苷-7-O-甲醚（swertisin）。这是该植物中首次报道的罕见 C-葡萄糖基黄酮，它以两种构象体存在并显示出 NMR 信号的重复。它显示出比用作标准的毒扁豆碱（依色林）更好的乙酰胆碱酯酶抑制活性，IC 为 32.09µg/mL。
本研究报告了一种罕见的 C-糖苷黄酮；异荭草苷-7-O-甲醚（swertisin）的分离和鉴定。分离得到的化合物显示出 NMR 信号的重复，并且比用作标准的毒扁豆碱的乙酰胆碱酯酶抑制活性更好。该化合物的活性表明它可能对阿尔茨海默病的治疗有用。
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