A sesquiterpene quinone, dysidine, from the sponge Dysidea villosa, activates the insulin pathway through inhibition of PTPases
文献类型:期刊论文
作者 | Zhang, Yu; Li, Yan; Guo, Yue-wei![]() ![]() ![]() |
刊名 | ACTA PHARMACOLOGICA SINICA
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出版日期 | 2009-03 |
卷号 | 30期号:3页码:333-345 |
关键词 | sesquiterpene quinone dysidine PTP1B inhibitor insulin |
ISSN号 | 1671-4083 |
DOI | 10.1038/aps.2009.5 |
文献子类 | Article |
英文摘要 | Aim: The sesquiterpene hydroquinones/quinones belong to one class of marine sponge metabolites, and they have received considerable attention due to their varied biological activities, including anti-tumor, anti-HIV, and anti-inflammatory action. In order to probe the potential anti-diabetic effect of the sesquiterpene hydroquinones/quinones, the effect of dysidine on the insulin pathway was studied. Methods: The promotion of glucose uptake by dysidine was studied in differentiated 3T3-L1 cells. The increase in membrane-located GLUT4 by dysidine was studied in CHO-K1/GLUT4 and 3T3-L1 cells by immuno-staining. The activation of the insulin signaling pathway by dysidine was probed by Western blotting. The inhibition of PTPases by dysidine was detected in vitro. Results: Dysidine, found in the Hainan sponge Dysidea villosa in the Chinese South Sea, effectively activated the insulin signaling pathway, greatly promoted glucose uptake in 3T3-L1 cells, and showed strong insulin-sensitizing activities. The potential targets of action for dysidine were probed, and the results indicated that dysidine exhibited its cellular effects through activation of the insulin pathway, possibly through the inhibition of protein tyrosine phosphatases, with more specific inhibition against protein tyrosine phosphatase 1B (PTP1B). Conclusion: Our findings are expected to expand understanding of the biological activities of sesquiterpene hydroquinones/quinones, and they show that dysidine could be a potential lead compound in the development of an alternative adjuvant in insulin therapy. |
WOS关键词 | TYROSINE-PHOSPHATASE 1B ; STIMULATES GLUCOSE-UPTAKE ; PROTEIN-KINASE INHIBITOR ; 3T3-L1 ADIPOCYTES ; SELECTIVE INHIBITORS ; GLUT4 TRANSLOCATION ; PHOSPHOLIPASE A(2) ; PLASMA-MEMBRANE ; LEPTIN ACTION ; SENSITIVITY |
资助项目 | State Key Program of Basic Research of China[2004CB518905] ; State Key Program of Basic Research of China[2007CB914304] ; National Natural Science Foundation of China[30525024] ; National Natural Science Foundation of China[90713046] ; National Natural Science Foundation of China[20721003] ; National Natural Science Foundation of China[20772136] ; Foundation of Chinese Academy of Sciences[KSCX2-YW-R-18] |
WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
语种 | 英语 |
CSCD记录号 | CSCD:3628633 |
WOS记录号 | WOS:000264239600008 |
出版者 | ACTA PHARMACOLOGICA SINICA |
源URL | [http://119.78.100.183/handle/2S10ELR8/279295] ![]() |
专题 | 天然药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物化学研究室 药理学第三研究室 |
通讯作者 | Guo, Yue-wei |
作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai 210203, Peoples R China |
推荐引用方式 GB/T 7714 | Zhang, Yu,Li, Yan,Guo, Yue-wei,et al. A sesquiterpene quinone, dysidine, from the sponge Dysidea villosa, activates the insulin pathway through inhibition of PTPases[J]. ACTA PHARMACOLOGICA SINICA,2009,30(3):333-345. |
APA | Zhang, Yu,Li, Yan,Guo, Yue-wei,Jiang, Hua-liang,&Shen, Xu.(2009).A sesquiterpene quinone, dysidine, from the sponge Dysidea villosa, activates the insulin pathway through inhibition of PTPases.ACTA PHARMACOLOGICA SINICA,30(3),333-345. |
MLA | Zhang, Yu,et al."A sesquiterpene quinone, dysidine, from the sponge Dysidea villosa, activates the insulin pathway through inhibition of PTPases".ACTA PHARMACOLOGICA SINICA 30.3(2009):333-345. |
入库方式: OAI收割
来源:上海药物研究所
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