大戟烷二萜类化合物作为自噬激活剂和 Tau 病理抑制剂的研究进展。
Jatrophane Diterpenoids from Linn. as Activators of Autophagy and Inhibitors of Tau Pathology.
机构信息
State Key Laboratory of Functions and Applications of Medicinal Plants & College of Pharmacy, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Medical University, Guiyang 550014, China.
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China.
出版信息
Int J Mol Sci. 2023 Jan 6;24(2):1088. doi: 10.3390/ijms24021088.
Ten jatrophane diterpenoids were isolated from the whole plant Linn. including seven new ones, named euphjatrophanes A-G (labeled compounds , , -). Their structures were elucidated with a combination of spectroscopic and single-crystal X-ray crystallography, enabling the identification of compounds , , and as the previously published euphpepluones G, K, and L, respectively. All compounds were evaluated for their bioactivity with flow cytometry in assays of autophagic flux in HM Cherry-GFP-LC3 (human microglia cells stably expressing the tandem monomeric mCherry-GFP-tagged LC3) cells. Euphpepluone K () significantly activated autophagic flux, an effect that was verified with confocal analysis. Moreover, cellular assays showed that euphpepluone K () induced autophagy and inhibited Tau pathology.
从 Linn 的全植物中分离得到了 10 种吉普烷二萜类化合物，包括 7 种新化合物，命名为 euphjatrophanes A-G（标记化合物、、-）。通过光谱和单晶 X 射线晶体学的组合，阐明了它们的结构，使化合物、和确定为以前公布的 euphpepluones G、K 和 L。所有化合物都通过流式细胞术在 HM Cherry-GFP-LC3（稳定表达串联单体 mCherry-GFP 标记 LC3 的人小胶质细胞）细胞中的自噬通量测定中进行了生物活性评估。Euphpepluone K () 显著激活自噬通量，这一效应通过共聚焦分析得到了验证。此外，细胞实验表明 euphpepluone K () 诱导自噬并抑制 Tau 病理。
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