Synthesis and anti-fibrotic effects of santamarin derivatives as cytotoxic agents against hepatic stellate cell line LX2
文献类型：期刊论文
| 作者 | Wang,Jin-Ping; Li,Tian-Ze; Huang,Xiao-Yan; Geng,Chang-An; Shen,Cheng; Sun,Jin-Jin; Xue,Dong; Chen,Ji-Jun
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2021 |
| 卷号 | 41页码:127994 |
| 关键词 | Santamarin derivatives Anti-fibrotic effects HSC-LX2 Extracellular matrix NF-KAPPA-B SESQUITERPENE LACTONES LIVER FIBROSIS STRUCTURE REQUIREMENT BAY LEAF ACTIVATION |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2021.127994 |
| 英文摘要 | Liver fibrosis is a final result of extensive deposition of extracellular matrix (ECM) and starts with the activation and proliferation of hepatic stellate cells (HSCs). Our previous study showed that eudesmane sesquiterpenoid santamarin had cytotoxicity against hepatic stellate cell line LX2 (HSC-LX2) with IC50 values of 16.5 ? 0.7 ?M. To explore the structure?activity relationships, twenty-six derivatives were synthesized by modifying the hydroxyl group, double-bond and unsaturated lactone. Cytotoxicity evaluation suggested that eight derivatives (6, 9, 13, 17, 20 and 25?27) increased activity against HSC-LX2. Especially, derivatives 17, 20 and 25 displayed obvious cytotoxicity with IC50 values of 6.4 ? 0.4, 4.6 ? 0.1, and 3.5 ? 0.1 ?M, which were 3 to 5-fold higher than santamarin. Preliminary mechanisms study revealed that the active compound 20 exhibited more than 8fold and 6-fold enhancement of inhibitory effect on the deposition of human hyaluronic acid (HA) and human laminin (HL) with IC50 values of 7.6 ? 0.6 and 3.3 ? 1.2 ?M. |
| WOS记录号 | WOS:000651228800011 |
| 源URL | [http://ir.kib.ac.cn/handle/151853/73168]  |
| 专题 | 中国科学院昆明植物研究所 |
| 作者单位 | 1.Li, Tian-Ze 2.Shaanxi Normal Univ, Sch Chem & Chem Engn, Xian 710062, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 4.Huang, Xiao-Yan 5.Geng, Chang-An 6.Shen, Cheng 7.Sun, Jin-Jin 8.Chinese Acad Sci, Kunming Inst Bot, Yunnan Key Lab Nat Med Chem, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China 9.[Wang, Jin-Ping 10.Shaanxi Normal Univ, Minist Educ, Key Lab Appl Surface & Colloid Chem, Xian 710062, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang,Jin-Ping,Li,Tian-Ze,Huang,Xiao-Yan,et al. Synthesis and anti-fibrotic effects of santamarin derivatives as cytotoxic agents against hepatic stellate cell line LX2[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2021,41:127994. |
| APA | Wang,Jin-Ping.,Li,Tian-Ze.,Huang,Xiao-Yan.,Geng,Chang-An.,Shen,Cheng.,...&Chen,Ji-Jun.(2021).Synthesis and anti-fibrotic effects of santamarin derivatives as cytotoxic agents against hepatic stellate cell line LX2.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,41,127994. |
| MLA | Wang,Jin-Ping,et al."Synthesis and anti-fibrotic effects of santamarin derivatives as cytotoxic agents against hepatic stellate cell line LX2".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 41(2021):127994. |
入库方式： OAI收割
来源：昆明植物研究所
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