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石杉生物碱及其抗乙酰胆碱酯酶活性。

Lycopodium Alkaloids from Huperzia serrata and Their Anti-acetylcholinesterase Activities.

机构信息

Institute of Traditional Chinese Medicine & Natural Products, Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, 510632, P. R. China.

Guangdong Clinical Translational Center for Targeted Drug, Department of Pharmacology, School of Medicine, Jinan University, Guangzhou, 510632, P. R. China.

出版信息

Chem Biodivers. 2023 Sep;20(9):e202301024. doi: 10.1002/cbdv.202301024. Epub 2023 Aug 8.

Abstract

One new fawcettimine-type alkaloid (1), one new miscellaneous-type alkaloid (2), four new lycodine-type alkaloids (3-6), and eight known ones (7-14) were isolated from the whole plants of Huperzia serrata. Their structures and absolute configurations were elucidated based on spectroscopic data, X-ray diffraction, ECD calculation and Mosher's method. Compound 1 was a rare C N -type Lycopodium alkaloid, possessing serratinine skeleton with an amide side chain in C-5. The absolute configuration of the 18-OH of compounds 4-6 were first determined by Mosher's method. Moreover, compounds 1-14 were assayed anti-acetylcholinesterase effect in vitro, and compound 7 showed significant anti-acetylcholinesterase activity with an IC value of 16.18±1.64 μM.

摘要

从蛇足石杉全株中分离得到 1 个新的石杉堿型生物碱(1)、1 个新的杂环型生物碱(2)、4 个新的石松堿型生物碱(3-6)和 8 个已知化合物(7-14)。基于光谱数据、X 射线衍射、ECD 计算和 Mosher 方法,解析了它们的结构和绝对构型。化合物 1 是一种罕见的 C N -型石松生物碱,具有蛇足石杉骨架,并在 C-5 位带有酰胺侧链。化合物 4-6 的 18-OH 的绝对构型首次通过 Mosher 方法确定。此外,还对化合物 1-14 进行了体外抗乙酰胆碱酯酶活性测定,化合物 7 表现出显著的抗乙酰胆碱酯酶活性,IC 值为 16.18±1.64 μM。

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