Journal
BIOORGANIC CHEMISTRY
Volume 112, Issue -, Pages -Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2021.104944
Keywords
Euphorbia lathyris; Lathyrane; Premyrsinane; Anti-inflammatory activity
Funding
- National Natural Science Foundation of China (NSFC) [81773594, 81773637, U1803122, U1703111]
- Chunhui Program-Cooperative Research Project of the Ministry of Education, Liaoning Revitalization Talents Program [XLYC1807182]
- Liaoning Province Natural Science Foundation [2019-MS-299, 2020-MZLH-31]
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Twelve new diterpenoids were isolated from the seeds of Euphorbia lathyris, with compound 1 showing the most remarkable anti-inflammatory effect by inhibiting the generation of inflammatory cytokines. The study also discussed the structure-activity relationships of these diterpenoids.
Twelve previously undescribed diterpenoids, euplarisans A-L (1-12), including one premyrsinane and eleven lathyranes, along with ten known analogues 13-22 were isolated from the seeds of Euphorbia lathyris. Their chemical structures were delineated by spectroscopic analysis and single-crystal X-ray diffraction. Interestingly, both 5 and 6 possessed an unusual trans-gem-dimethylcyclopropane as structural features and compound 8 was elucidated as premyrsinane-type diterpenoid. Meanwhile, a plausible biogenetic pathway for compounds 1-12 was proposed. In the anti-inflammatory bioassay, compounds 1, 2, 4, 13, 16, and 18 markedly inhibited the nitric oxide production in LPS-induced RAW264.7 macrophage cells. Compound 1 showed a more remarkable anti-inflammatory effect than others. It inhibited the generation of inflammatory cytokines (IL-1 beta, IL-6, and TNF alpha) and also obviously decreased the expression of iNOS, COX-2, and p-IKB alpha in a dose-dependent manner. The structure-activity relationships (SARs) of these diterpenoids were also discussed.
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