Molecular Regulation of Betulinic Acid on α3β4 Nicotinic Acetylcholine Receptors
Abstract
:1. Introduction
2. Results
2.1. Concentration-Dependent Inhibitory Effect of BA on α3β4 nAChRs
2.2. Current-Voltage Relationship of IACh and Non-Competitive Inhibition by Betulinic Acid
2.3. Docking Model of Betulinic Acid and Nicotinic Acetylcholine Receptor α3β4
2.4. Inhibitory Effect of Betulinic Acid on a Double-Mutant Nicotinic Acetylcholine Receptor α3β4
3. Discussion
4. Materials and Methods
4.1. Materials
4.2. Oocyte Preparation
4.3. In Vitro Transcription of mRNA and Injection into Oocytes
4.4. Mutagenesis
4.5. D Structure Modeling and Molecular-Docking Studies
4.6. Data Recording with Two-Electrode Voltage Clamp
4.7. Data Analysis
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
Sample Availability
References
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Subunit Mutants | Imax | IC50 | nH |
---|---|---|---|
Wild α3 + Wild β4 | 101.5 ± 5.9 | 12.8 ± 2.0 | 0.9 ± 0.1 |
α3 (L257A) + Wild β4 | 48.9 ± 2.7 | 18.6 ± 1.7 | 1.6 ± 0.1 |
Wild α3 + β4 (I263A) | 33.1 ± 3.3 | 13.4 ± 1.9 | 2.7 ± 1.0 |
α3 (L257A) + β4 (I263A) | 7.4 | 26.2 | 2 |
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Lee, S.; Jung, W.; Eom, S.; Yeom, H.D.; Park, H.-D.; Lee, J.H. Molecular Regulation of Betulinic Acid on α3β4 Nicotinic Acetylcholine Receptors. Molecules 2021, 26, 2659. https://doi.org/10.3390/molecules26092659
Lee S, Jung W, Eom S, Yeom HD, Park H-D, Lee JH. Molecular Regulation of Betulinic Acid on α3β4 Nicotinic Acetylcholine Receptors. Molecules. 2021; 26(9):2659. https://doi.org/10.3390/molecules26092659
Chicago/Turabian StyleLee, Shinhui, Woog Jung, Sanung Eom, Hye Duck Yeom, Heui-Dong Park, and Junho H. Lee. 2021. "Molecular Regulation of Betulinic Acid on α3β4 Nicotinic Acetylcholine Receptors" Molecules 26, no. 9: 2659. https://doi.org/10.3390/molecules26092659