Diterpenoids from Euphorbia peplus possessing cytotoxic and anti-inflammatory activities
文献类型：期刊论文
| 作者 | Li, Ying3; Yu, Zhi-Pu2; Li, Yu-Peng3; Yu, Jin-Hai3; Yue, Jian-Min1,3
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| 刊名 | BIOORGANIC CHEMISTRY
 |
| 出版日期 | 2024-04-01 |
| 卷号 | 145页码:14 |
| 关键词 | Euphorbia peplus Diterpenoids Cytotoxic activity Anti-inflammatory activity NF-kappa B MAPK |
| ISSN号 | 0045-2068 |
| DOI | 10.1016/j.bioorg.2024.107194 |
| 通讯作者 | Yu, Jin-Hai(jhyu@baridd.ac.cn) ; Yue, Jian-Min(jmyue@simm.ac.cn) |
| 英文摘要 | Phytochemical investigation into the medium polar fraction of the ethanol extract of Euphorbia peplus led to the identification of 32 diterpenoids with five structural types. Compounds 1-5 and 7-11 are reported for the first time, while the configuration of 6,7-epoxy group of 6 was revised to be beta-oriented. Compounds 1-5 feature a rare structural variation of the double bond at Delta 1 migrating to Delta 1(10) in the tigliane-type diterpenoid family. Biologically, compound 21 was found to be the only one to show moderate cytotoxic activity, associated with the presence of a benzoyloxy residue at C-16. Besides, compounds 4, 8, 12, 13, 16, and 19 show significant inhibitory activities against NO production induced by LPS in RAW264.7 macrophage cells, with IC50 values within 2-5 mu M. Structure-activity relationship (SAR) analysis revealed that the ingenane-type diterpenoids have the best anti-inflammatory activity, and the esterification at 3-OH or 5-OH is crucial. Further biological researches demonstrated that 13, the predominant metabolite in this plant, exerts anti-inflammatory effects by blocking the activation of NF-kappa B and MAPK signaling pathways. |
| WOS关键词 | JATROPHANE DITERPENES ; MULTIDRUG-RESISTANCE ; MODULATORS ; LATEX ; ESTERS |
| 资助项目 | Shandong Laboratory Program[SYS202205] ; National Natural Science Foundation of China[22237007] ; National Natural Science Foundation of China[21807040] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001188700700001 |
| 出版者 | ACADEMIC PRESS INC ELSEVIER SCIENCE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/310375]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Yu, Jin-Hai; Yue, Jian-Min |
| 作者单位 | 1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China 2.Ocean Univ China, Sch Med & Pharm, Inst Evolut & Marine Biodivers, Minist Educ China,Key Lab Marine Drugs, Qingdao 266003, Peoples R China 3.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Ying,Yu, Zhi-Pu,Li, Yu-Peng,et al. Diterpenoids from Euphorbia peplus possessing cytotoxic and anti-inflammatory activities[J]. BIOORGANIC CHEMISTRY,2024,145:14. |
| APA | Li, Ying,Yu, Zhi-Pu,Li, Yu-Peng,Yu, Jin-Hai,&Yue, Jian-Min.(2024).Diterpenoids from Euphorbia peplus possessing cytotoxic and anti-inflammatory activities.BIOORGANIC CHEMISTRY,145,14. |
| MLA | Li, Ying,et al."Diterpenoids from Euphorbia peplus possessing cytotoxic and anti-inflammatory activities".BIOORGANIC CHEMISTRY 145(2024):14. |
入库方式： OAI收割
来源：上海药物研究所
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