Isodon serra的两种新萜类化合物及其抗阿尔茨海默病活性

IF 2.5 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY
Li-Jia Ye, Miao Zhang, Mi-Na Yang, Xin Wang, Yi-Nan Yang, Hong-Fen Jiang, Jie Yang, Zhan-Xin Zhang, Dong-Qing Fei
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引用次数: 0

摘要

通过对山莨菪(Isodon serra, Lamiaceae)全株95%乙醇提取物的植物化学研究,分离出一种新的正戊烷二萜异serrone a(1)和一种新的2,3-叔熊烷型三萜异serrone a(2),以及四种已知化合物(3-6)。除化合物4外,其余化合物均为首次从该植物中分离得到。通过hresms、IR、1D和2D NMR数据分析,确定了新化合物的结构。用电子圆二色性(ECD)和单晶x射线衍射分析分别确定了1和2的绝对构型。据我们所知,本文首次报道了已知化合物4-6的单晶x射线衍射数据。此外,利用转基因秀丽隐杆线虫阿尔茨海默病(AD)病理模型,我们评估了化合物1-4和6的体内抗AD活性。生物学评价显示,在100µM浓度下,3和6延缓了CL4176线虫的麻痹过程,这表明它们可能是抗阿尔茨海默病的候选药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Two New Terpenoids From Isodon serra and Their Anti-Alzheimer's Disease Activity.

Phytochemical investigation of the 95% ethanol extract of the whole plants of Isodon serra (Lamiaceae) led to the isolation of a new ent-kaurane diterpenoid isoserrone A (1) and a new 2,3-seco-ursane-type triterpenoid isoserric acid A (2), along with four known compounds (3-6). Except for compound 4, the remaining compounds were obtained from I. serra for the first time. The structures of the new compounds were established based on the analysis of HRESIMS, IR, 1D, and 2D NMR spectroscopic data. The absolute configurations of 1 and 2 were elucidated by electronic circular dichroism (ECD) and single-crystal X-ray diffraction analysis, respectively. To our knowledge, this article provides the first reported single-crystal X-ray diffraction data of known compounds 4-6. Moreover, using a transgenic Caenorhabditis elegans Alzheimer's disease (AD) pathological model, we evaluated the in vivo anti-AD activities of compounds 1-4 and 6. The biological evaluation revealed that 3 and 6 delayed the paralysis process in CL4176 nematodes at the concentration of 100 µM, suggesting their potential as anti-AD therapeutic candidates.

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来源期刊
Chemistry & Biodiversity
Chemistry & Biodiversity 环境科学-化学综合
CiteScore
3.40
自引率
10.30%
发文量
475
审稿时长
2.6 months
期刊介绍: Chemistry & Biodiversity serves as a high-quality publishing forum covering a wide range of biorelevant topics for a truly international audience. This journal publishes both field-specific and interdisciplinary contributions on all aspects of biologically relevant chemistry research in the form of full-length original papers, short communications, invited reviews, and commentaries. It covers all research fields straddling the border between the chemical and biological sciences, with the ultimate goal of broadening our understanding of how nature works at a molecular level. Since 2017, Chemistry & Biodiversity is published in an online-only format.
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