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Synthesis and anti-fibrotic effects of santamarin derivatives as cytotoxic agents against hepatic stellate cell line LX2
Wang,Jin-Ping; Li,Tian-Ze; Huang,Xiao-Yan; Geng,Chang-An; Shen,Cheng; Sun,Jin-Jin; Xue,Dong; Chen,Ji-Jun
2021
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
卷号41页码:127994
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.
关键词Santamarin derivatives Anti-fibrotic effects HSC-LX2 Extracellular matrix NF-KAPPA-B SESQUITERPENE LACTONES LIVER FIBROSIS STRUCTURE REQUIREMENT BAY LEAF ACTIVATION
DOI10.1016/j.bmcl.2021.127994
WOS记录号WOS:000651228800011
引用统计
被引频次:5[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符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.[Wang, Jin-Ping
2.Li, Tian-Ze
3.Huang, Xiao-Yan
4.Geng, Chang-An
5.Shen, Cheng
6.Sun, Jin-Jin
7.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
8.Shaanxi Normal Univ, Minist Educ, Key Lab Appl Surface & Colloid Chem, Xian 710062, Peoples R China
9.Shaanxi Normal Univ, Sch Chem & Chem Engn, Xian 710062, Peoples R China
10.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
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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.
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