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| 1 | Small molecules for fat combustion: targeting obesity显示文摘Obesity is increasing in an alarming rate worldwide, which causes higher risks of some diseases, such as type 2 diabetes, cardiovascular diseases, and cancer. Current therapeutic approaches,either pancreatic lipase inhibitors or appetite suppressors, are generally of limited effectiveness. Brown adipose tissue(BAT) and beige cells dissipate fatty acids as heat to maintain body temperature, termed non-shivering thermogenesis; the activity and mass of BAT and beige cells are negatively correlated with overweight and obesity. The existence of BAT and beige cells in human adults provides an effective weight reduction therapy, a process likely to be amenable to pharmacological intervention. Herein, we combed through the physiology of thermogenesis and the role of BAT and beige cells in combating with obesity. We summarized the thermogenic regulators identified in the past decades, targeting G proteincoupled receptors, transient receptor potential channels, nuclear receptors and miscellaneous pathways.Advances in clinical trials were also presented. The main purpose of this review is to provide a comprehensive and up-to-date knowledge from the biological importance of thermogenesis in energy homeostasis to the representative thermogenic regulators for treating obesity. Thermogenic regulatorsmight have a large potential for further investigations to be developed as lead compounds in fighting obesity. | Jingxin Liu Yitao Wang Ligen Lin | 2019 | Acta Pharmaceutica Sinica B2019,9,2: | 18 |
| 2 | Effects of curcumin on glucose metabolism in the brains of rats subjected to chronic unpredictable stress:A18 F-FDG micro-PET study显示文摘 | Zheng Lin Ligen Shi Jing Lu | 2013 | Complementary and Alternative Medicine2013,13,: | 1 |
| 3 | 显示文摘 | Teng Lin Chuanhua Lu Ligen Zhu | 2011 | American Association of Pharmaceutical Scientists2011,12,1: | 1 |
| 4 | Adipocyte expression of PU.1 transcription factor causes insulin resistance through upregulation of inflammatory cytokine gene expression and ROS production显示文摘 | Ligen Lin Weijun Pang Keyun Chen Fei Wang Jon Gengler Yuxiang Sun Qiang Tong | 2012 | AJP: Endocrinology and Metabolism2012,,12: | 1 |
| 5 | Artificial intelligence-aided discovery of prolyl hydroxylase 2 inhibitors to stabilize hypoxia inducible factor-1α and promote angiogenesis显示文摘From ZINC database with a total of 1.8 million small molecules, four compounds are identified as prolyl hydroxylase 2 inhibitors through a virtual screening workflow that sequentially incorporates machine learning, molecular docking, and molecular dynamics. Among them, compound 103,(E)-5-(5-((2-(1Htetrazol-5-yl)hydrazineylidene)methyl)furan-2-yl)isoindoline-1,3-dione, promotes the migration and capillary tube formation capacity of human umbilical vein endothelial cells through enhancing the stability of hypoxia inducible factor-1α and increasing the level of vascular endothelial growth factor. | Jianzhong Zhu Cheng Chen Jie Dong Shasha Cheng Guodong Li Chunming Wang Defang Ouyang Chung-Hang Leung Ligen Lin | 2023 | Chinese Chemical Letters2023,34,2: | 0 |
| 6 | Biscaesalmins A and B from Caesalpinia minax,highly oxidized dimeric cassane diterpenoids as interleukin-1β inhibitors显示文摘To search naturally occurring interleukin-1β(IL-1β) inhibitors,biscaesalmins A(1) and B(2),two highly oxidized dimeric cassane diterpenoids with a newly formed alicyclic skeleton,have been isolated from the traditional Chinese medicine Kushilian(Caesalpinia minax).Their full structures were determined by comprehensive spectroscopic analysis and quantum chemical TD-DFT(time-dependent density functional theory) calculation.Biosynthetically,1 and 2 were formed via an intermolecular [4+2]Diels-Alder cycloaddition of two monomers,affording an additional six-membered carbon ring linkage.Compounds 1 and 2 inhibited nitric oxide production on lipopolysaccharide-stimulated THP-1 macrophages,with IC_(50) values being at 1.20±0.23 and 2.30±0.15 μmol/L,respectively.Furthermore,compound 1 inhibited NLRP3(NOD-,LRR-and pyrin domain-containing protein 3) inflammasomemediated IL-1β production and blocked the migration of macrophages towards adipocyte conditioned medium.Biscaesalmins A and B might be candidates for treating inflammation-related metabolic diseases. | Yunshao Xu Tian Zhang Lu Feng Zheling Feng Qingwen Zhang Yang Ye Lishe Gan Ligen Lin | 2021 | Chinese Chemical Letters2021,32,4: | 0 |