Inhibitory kinetics and bioactivities of Nuciferine and Methyl Ganoderate on Mucor miehei lipase and 3T3-L1 preadipocytes
| Autor: | Qin Wang, Qing-Xi Chen, Hui-Long Xu, Tian-Tian Liu, Xiao-Tian Liu |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Protein Conformation
alpha-Helical Aporphines Reishi Nuciferine 02 engineering and technology Inhibitory postsynaptic potential Biochemistry Cell Line 03 medical and health sciences chemistry.chemical_compound Mice Structural Biology 3T3-L1 Cells Catalytic Domain Adipocytes Animals Lotus effect Obesity Lipase Rhizomucor Molecular Biology Triglycerides 030304 developmental biology Cell Proliferation 0303 health sciences Chromatography Adipogenesis biology Cholesterol Active site 3T3-L1 Cell Differentiation General Medicine 021001 nanoscience & nanotechnology Fluorescence Triterpenes Molecular Docking Simulation Kinetics chemistry biology.protein Protein Conformation beta-Strand Anti-Obesity Agents 0210 nano-technology |
| Zdroj: | International journal of biological macromolecules. 163 |
| ISSN: | 1879-0003 |
| Popis: | In this study, inhibitory kinetics of Nuciferine and Methyl Ganoderate extrated from Lotus Leaves and Ganoderma lucidum on Mucor miehei Lipase were studied first. The molecular structure of Nuciferine and Methyl Ganoderate were determined. The inhibitory effects of two extracts on lipase were reversible, with the IC50 values of 0.194 and 0.332 mg/mL, respectively. The inhibition kinetic analysis by Lineweaver-Burk plots showed that they were a mixed-type inhibitor of lipase, with inhibition constants KI of 0.16 and 0.29 mg/mL, and KIS of 0.36 and 0.49 mg/mL, respectively. Results of spectral analysis showed that the UV absorption and the molecule fluorescence spectrum of the lipase hydrolyzate were significantly decreased after the inhibitor was added. The molecular docking further suggested that the interaction site between the active substance and inhibitor was located in an α-helix and a β-sheet of the lipase, and the lipase active site was interfered by the inhibitor near the cap structure. In addition, the proliferation and differentiation of 3 T3-L1 preadipocytes were inhibited by two extracts. Total triglycerides and cholesterol were significantly reduced in the cells. The results confirmed that Nuciferine and Methyl Ganoderate can be used as potential obesity treatment drugs. |
| Databáze: | OpenAIRE |
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