A new class of potent liver injury protective compounds: Structural elucidation, total synthesis and bioactivity study
文献类型：期刊论文
| 作者 | Ji, Kailong1; Liu, Wei1; Yin, Weihang1; Kong, Xiangrong2; Xu, Honghong1; Lai, Zeng-Wei1; Li, Jing-Ya1,2 ; Yue, Jian-Min1
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| 刊名 | ACTA PHARMACEUTICA SINICA B
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| 出版日期 | 2023-08-01 |
| 卷号 | 13期号:8页码:3414-3424 |
| ISSN号 | 2211-3835 |
| 关键词 | Phychetins Phyllanthus franchetianus Structural elucidation Total synthesis Liver injury protection Anti-inflammation |
| DOI | 10.1016/j.apsb.2023.05.001 |
| 通讯作者 | Lai, Zeng-Wei(2860879@sina.com) ; Li, Jing-Ya(jyli@simm.ac.cn) ; Yue, Jian-Min(jmyue@simm.ac.cn) |
| 英文摘要 | A new class of potent liver injury protective compounds, phychetins A -D (1-4) featuring an unique 6/6/5/6/5 pentacyclic framework, were isolated and structurally characterized from a Chinese me-dicinal plant Phyllanthus franchetianus. Compounds 2-4 are three pairs of enantiomers that were initially obtained in a racemic manner, and were further separated by chiral HPLC preparation. Com-pounds 1-4 were proposed to be originated biosynthetically from a coexisting lignan via an intramole-cular Friedel-Crafts reaction as the key step. A bioinspired total synthesis strategy was thus designated, and allowed the effective syntheses of compounds 2-4 in high yields. Some of compounds exhibited sig-nificant anti-inflammatory activities in vitro via suppressing the production of pro-inflammatory cytokine IL-1b. Notably, compound 4, the most active enantiomeric pair in vitro, displayed prominent potent pro-tecting activity against liver injury at a low dose of 3 mg/kg in mice, which could serve as a promising lead for the development of acute liver injury therapeutic agent. |
| WOS关键词 | LIGNANS |
| 资助项目 | National Natural Science Foundations of China[22177121] ; National Natural Science Foundations of China[92057116] ; National Natural Science Foundations of China[22237007] ; Science and Technology Commission of Shanghai Municipality (China)[19431908100] ; Science and Technology Commission of Shanghai Municipality (China)[20ZR1467800] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES |
| WOS记录号 | WOS:001060411700001 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/307058]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Lai, Zeng-Wei; Li, Jing-Ya; Yue, Jian-Min |
| 作者单位 | 1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ji, Kailong,Liu, Wei,Yin, Weihang,et al. A new class of potent liver injury protective compounds: Structural elucidation, total synthesis and bioactivity study[J]. ACTA PHARMACEUTICA SINICA B,2023,13(8):3414-3424. |
| APA | Ji, Kailong.,Liu, Wei.,Yin, Weihang.,Kong, Xiangrong.,Xu, Honghong.,...&Yue, Jian-Min.(2023).A new class of potent liver injury protective compounds: Structural elucidation, total synthesis and bioactivity study.ACTA PHARMACEUTICA SINICA B,13(8),3414-3424. |
| MLA | Ji, Kailong,et al."A new class of potent liver injury protective compounds: Structural elucidation, total synthesis and bioactivity study".ACTA PHARMACEUTICA SINICA B 13.8(2023):3414-3424. |
入库方式： OAI收割
来源：上海药物研究所
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