A novel GPR120-selective agonist promotes insulin secretion and improves chronic inflammation
文献类型：期刊论文
| 作者 | Yang, Liu2,3; Lei, Xian-Tao1,4; Huang, Qi2; Wang, Ting2; Sun, Hong-Bin1,4; Wang, He-Yao2,3
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| 刊名 | LIFE SCIENCES
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| 出版日期 | 2021-03-15 |
| 卷号 | 269页码:8 |
| 关键词 | GPR120 agonist Insulin secretion Anti-inflammation Insulin resistance Type 2 diabetes mellitus |
| ISSN号 | 0024-3205 |
| DOI | 10.1016/j.lfs.2021.119029 |
| 通讯作者 | Wang, Ting(wangting@simm.ac.cn) ; Sun, Hong-Bin(hongbinsun@cpu.edu.cn) ; Wang, He-Yao(hywang@simm.ac.cn) |
| 英文摘要 | Aims: The present study aimed to disclose a potent and selective GPR120 agonist LXT34 and its anti-diabetic effects. Main methods: Calcium mobilization assay was used to measure the agonistic potency and selectivity of LXT34 in GPR120 or GPR40-overexpression Chinese hamster ovary (CHO) cells. Glucagon-like peptide-1 (GLP-1) release and glucose-stimulated insulin secretion (GSIS) were evaluated in human colonic epithelial cell line NCI-H716 and mouse insulinoma cell line MIN6 by enzyme-linked immunosorbent assay (ELISA), respectively. The antiinflammatory effect was determined in lipopolysaccharide (LPS)-induced murine macrophage cell line RAW264.7. Oral glucose tolerance test (OGTT) and insulin tolerance test (ITT) were performed to assess the antidiabetic effects of LXT34 in db/db mice, and chronic inflammation in liver and adipose tissues were investigated using histomorphology, immunoblot and gene expression analysis. Key findings: LXT34 was a potent GPR120 agonist with negligible activity toward human and mouse GPR40. LXT34 could potentiate GSIS and suppress LPS-induced inflammation in macrophages. LXT34 not only markedly improved glucose tolerance and insulin resistance, but also distinctly reduced macrophages infiltration, proinflammatory cytokines expression and JNK phosphorylation of both liver and adipose tissues in db/db mice. Significance: LXT34, a novel and potent GPR120-selective agonist, showed beneficial effects on improving glucose homeostasis in obesity-related type 2 diabetes. |
| 资助项目 | National Natural Science Foundation of China[81773791] ; National Natural Science Foundation of China[81473262] ; National Natural Science Foundation of China[81503124] ; National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China[2018ZX09711002-002-007] ; Personalized Medicines-Molecular Signature-based Drug Discovery and Development, Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12040336] |
| WOS研究方向 | Research & Experimental Medicine ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000616196300020 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/295798]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Wang, Ting; Sun, Hong-Bin; Wang, He-Yao |
| 作者单位 | 1.China Pharmaceut Univ, Jiangsu Key Lab Drug Discovery Metab Dis, 24 Tongjia Xiang, Nanjing 210009, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 4.China Pharmaceut Univ, State Key Lab Nat Med, 24 Tongjia Xiang, Nanjing 210009, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Liu,Lei, Xian-Tao,Huang, Qi,et al. A novel GPR120-selective agonist promotes insulin secretion and improves chronic inflammation[J]. LIFE SCIENCES,2021,269:8. |
| APA | Yang, Liu,Lei, Xian-Tao,Huang, Qi,Wang, Ting,Sun, Hong-Bin,&Wang, He-Yao.(2021).A novel GPR120-selective agonist promotes insulin secretion and improves chronic inflammation.LIFE SCIENCES,269,8. |
| MLA | Yang, Liu,et al."A novel GPR120-selective agonist promotes insulin secretion and improves chronic inflammation".LIFE SCIENCES 269(2021):8. |
入库方式： OAI收割
来源：上海药物研究所
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