101. Euphzycopias A-I, macrocyclic diterpenes with NLRP3 inflammasome inhibitory activity from Euphorbia helioscopia L.
- Author
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Zhang Y, Xiong F, Zhang JJ, Yue CF, Bi DW, Cheng B, Wu XW, Li Q, Zhang XJ, Zhang RH, Dai XC, Shi QQ, Xiao WL, and Li XL
- Subjects
- Diterpenes chemistry, Diterpenes isolation & purification, Humans, Inflammasomes chemistry, Inflammasomes isolation & purification, Inhibitory Concentration 50, Magnetic Resonance Spectroscopy, Molecular Structure, NLR Family, Pyrin Domain-Containing 3 Protein antagonists & inhibitors, Optical Rotation, Plant Extracts chemistry, Plant Extracts isolation & purification, Plant Extracts pharmacology, Spectrophotometry, Infrared, Diterpenes pharmacology, Euphorbia chemistry, Inflammasomes pharmacology
- Abstract
A phytochemical investigation was conducted on Euphorbia helioscopia, resulting in the isolation of thirteen compounds, including nine undescribed diterpenoids, Euphzycopias A - I (1-9), of which the skeletons of compounds 1-4 were found in E. helioscopia L. Compounds 1-3 had 5/7/6 cyclic systems, while compound 4 had a 4/11 polycyclic system with a 4,7-cyclic ether between C-4 and C-7. The anti-inflammasome test using the isolated compounds (1-6, 8-13) showed that the diterpenes from E. helioscopia L. had a strong inhibitory effect on NLRP3 inflammasomes with IC
50 values of 3.34-14.92 μM., (Copyright © 2022 Elsevier B.V. All rights reserved.)- Published
- 2022
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