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从丹参变种简毛鼠尾草中分离得到的两个新的倍半萜类化合物及其抗阿尔茨海默病活性。

Two Undescribed Germacrane-Type Sesquiterpenoids from Salvia cavaleriei var. simplicifolia Stib. and Their Anti-Alzheimer's Disease Activity.

机构信息

School of Pharmacy, State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou, 730000, P. R. China.

出版信息

Chem Biodivers. 2024 Jun;21(6):e202400511. doi: 10.1002/cbdv.202400511. Epub 2024 Apr 25.

Abstract

Two undescribed germacrane-type sesquiterpenoids, salcasins A (1) and B (2), together with three known compounds (3-5) were isolated and identified from the whole plant of Salvia cavaleriei var. simplicifolia Stib. The structures of the undescribed compounds were elucidated on the basis of spectroscopic methods, such as HR-ESI-MS, 1D and 2D NMR data. The relative configurations of 1 and 2 were established by analyzing their NOESY spectra as well as by C NMR calculations with DP4+ probability analyses. The absolute configurations of 1 and 2 were determined by comparing experimental and calculated ECD spectra. Furthermore, the in vivo anti-Alzheimer's disease activities of 1-5 were evaluated using Caenorhabditis elegans AD pathological model. Among all isolated compounds, salcasin A (1) significantly delayed AD-like symptoms of worm paralysis, which may be a potential anti-AD candidate agent.

摘要

从丹参变种的全植物中分离并鉴定出两种未被描述的倍半萜类化合物,salcasin A(1)和 B(2),以及三种已知化合物(3-5)。基于高分辨电喷雾电离质谱(HR-ESI-MS)、1D 和 2D NMR 数据等光谱方法阐明了未知化合物的结构。通过分析它们的 NOESY 光谱以及通过具有 DP4+概率分析的 C NMR 计算确定了 1 和 2 的相对构型。通过比较实验和计算的 ECD 光谱确定了 1 和 2 的绝对构型。此外,还使用秀丽隐杆线虫 AD 病理模型评估了 1-5 的体内抗阿尔茨海默病活性。在所分离的化合物中,salcasin A(1)显著延缓了蠕虫瘫痪的 AD 样症状,可能是一种有潜力的抗 AD 候选药物。

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