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大戟素A - D,来自泽漆的具有潜在抗炎活性的大环二萜类化合物。

Euphzycopins A - D, macrocyclic diterpenoids with potential anti-inflammatory activity from Euphorbia Helioscopia.

作者信息

Qiu Xiong, Zhang Yu, Xu Yao-Jun, Liang Zhong-Dan, Dai Xiao-Chang, Xiao Wei-Lie, Zhang Xing-Jie, Li Xiao-Li

机构信息

Key Laboratory of Medicinal Chemistry for Natural Resource of Ministry of Education, Yunnan Characteristic Plant Extraction Laboratory, Yunnan Research & Development Center for Natural Products, School of Chemical Science and Technology, and School of Pharmacy, State Key Laboratory for Conservation and Utilization of Bio-Resources in Yunnan, Yunnan University, Kunming 650500, People's Republic of China.

Key Laboratory of Medicinal Chemistry for Natural Resource of Ministry of Education, Yunnan Characteristic Plant Extraction Laboratory, Yunnan Research & Development Center for Natural Products, School of Chemical Science and Technology, and School of Pharmacy, State Key Laboratory for Conservation and Utilization of Bio-Resources in Yunnan, Yunnan University, Kunming 650500, People's Republic of China.

出版信息

Fitoterapia. 2024 Mar;173:105821. doi: 10.1016/j.fitote.2024.105821. Epub 2024 Jan 9.

DOI:10.1016/j.fitote.2024.105821
PMID:38211643
Abstract

Four new diterpenoids (1-4) and four known diterpenoids (5-8) were purified from the whole plant of Euphorbia helioscopia L. Compounds 1 and 2 were jathophanes diterpenoids with a 5/12 polycyclic systems, compound 3 was rhamofolane diterpenoid with a 5/10 bicyclic skeleton and compound 4 was a rare class of euphorbia diterpenes featuring an unusual 5/10 fused ring system. Anti-inflammatory activity tests were conducted on the separated compounds, indicating that compound 4 had significant inhibitory effect on NLRP3 inflammasome with an IC value of 7.75 μM. Further, the inhibitory effect of 4 was determined using immunofluorescence assays.

摘要

从泽漆全草中分离得到4个新的二萜类化合物(1-4)和4个已知的二萜类化合物(5-8)。化合物1和2是具有5/12多环系统的麻疯树型二萜类化合物,化合物3是具有5/10双环骨架的鼠李叶烷型二萜类化合物,化合物4是一类罕见的大戟属二萜类化合物,具有不寻常的5/10稠环系统。对分离得到的化合物进行了抗炎活性测试,结果表明化合物4对NLRP3炎性小体具有显著的抑制作用,IC值为7.75 μM。此外,通过免疫荧光测定法确定了化合物4的抑制作用。

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