HPN, a Synthetic Analogue of Bromophenol from Red Alga Rhodomela confervoides: Synthesis and Anti-Diabetic Effects in C57BL/KsJ-db/db Mice
文献类型：期刊论文
| 作者 | Shi, Dayong1,4; Guo, Shuju1,4; Jiang, Bo1,4; Guo, Chao1,4; Wang, Tao2; Zhang, Luyong2; Li, Jingya3
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| 刊名 | MARINE DRUGS
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| 出版日期 | 2013-02 |
| 卷号 | 11期号:2页码:350-362 |
| 关键词 | bromophenol protein tyrosine phosphatase 1B inhibitor db/db mouse model anti-diabetes properties |
| ISSN号 | 1660-3397 |
| DOI | 10.3390/md11020350 |
| 文献子类 | Article |
| 英文摘要 | 3,4-Dibromo-5-(2-bromo-3,4-dihydroxy-6-(isopropoxymethyl)benzyl)benzene-1,2-diol (HPN) is a synthetic analogue of 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(ethoxymethyl) benzyl)benzene-1,2-diol (BPN), which is isolated from marine red alga Rhodomela confervoides with potent protein tyrosine phosphatase 1B (PTP1B) inhibition (IC50 = 0.84 mu mol/L). The in vitro assay showed that HPN exhibited enhanced inhibitory activity against PTP1B with IC50 0.63 mu mol/L and high selectivity against other PTPs (T cell protein tyrosine phosphatase (TCPTP), leucocyte antigen-related tyrosine phosphatase (LAR), Src homology 2-containing protein tyrosine phosphatase-1 (SHP-1) and SHP-2). The results of antihyperglycemic activity using db/db mouse model demonstrated that HPN significantly decreased plasma glucose (P < 0.01) after eight weeks treatment period. HPN lowered serum triglycerides and total cholesterol concentration in a dose-dependent manner. Besides, both of the high and medium dose groups of HPN remarkably decreased HbA1c levels (P < 0.05). HPN in the high dose group markedly lowered the insulin level compared to the model group (P < 0.05), whereas the effects were less potent than the positive drug rosiglitazone. Western blotting results showed that HPN decreased PTP1B levels in pancreatic tissue. Last but not least, the results of an intraperitoneal glucose tolerance test in Sprague-Dawley rats indicate that HPN have a similar antihyperglycemic activity as rosiglitazone. HPN therefore have potential for development as treatments for Type 2 diabetes. |
| WOS关键词 | TYROSINE-PHOSPHATASE 1B ; PTP1B INHIBITORS ; BIOLOGICAL EVALUATION ; INSULIN SENSITIVITY ; ACID-DERIVATIVES ; DRUGS ; SESQUITERPENES ; DESIGN |
| 资助项目 | National Natural Science Foundation of China[41276167] ; National Natural Science Foundation of China[41206066] ; Natural Science Foundation of Jiangsu Province[BK2012223] ; Nantong Municipal Natural Science Foundation[AS2011013] ; Qingdao Municipal Natural Science Foundation[10-3-4-8-2-JCH] ; Shangdong Excellent Young Scientists Award Fund[BS2009YY011] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000315396800005 |
| 出版者 | MDPI AG |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277743]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Shi, Dayong |
| 作者单位 | 1.Chinese Acad Sci, Nantong Branch, Inst Oceanol, Nantong 226006, Peoples R China; 2.China Pharmaceut Univ, Jiangsu Ctr Drug Screening, Nanjing 210009, Jiangsu, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 4.Chinese Acad Sci, Inst Oceanol, Qingdao 266071, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Shi, Dayong,Guo, Shuju,Jiang, Bo,et al. HPN, a Synthetic Analogue of Bromophenol from Red Alga Rhodomela confervoides: Synthesis and Anti-Diabetic Effects in C57BL/KsJ-db/db Mice[J]. MARINE DRUGS,2013,11(2):350-362. |
| APA | Shi, Dayong.,Guo, Shuju.,Jiang, Bo.,Guo, Chao.,Wang, Tao.,...&Li, Jingya.(2013).HPN, a Synthetic Analogue of Bromophenol from Red Alga Rhodomela confervoides: Synthesis and Anti-Diabetic Effects in C57BL/KsJ-db/db Mice.MARINE DRUGS,11(2),350-362. |
| MLA | Shi, Dayong,et al."HPN, a Synthetic Analogue of Bromophenol from Red Alga Rhodomela confervoides: Synthesis and Anti-Diabetic Effects in C57BL/KsJ-db/db Mice".MARINE DRUGS 11.2(2013):350-362. |
入库方式： OAI收割
来源：上海药物研究所
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