Inhibition of 11b-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui
Abstract
:1. Introduction
2. Results and Discussion
2.1. Identification of Compounds
2.2. Inhibition of 11β-HSD1
Compounds | Mouse 11β-HSD1 (IC50) | Mouse 11β-HSD2 (IC50) | Mouse HSD2/HSD1 | Human 11β-HSD1 (IC50) | Human 11β-HSD2 (IC50) | Human HSD2/HSD1 |
---|---|---|---|---|---|---|
Compound 1 | 78.44 nM | >1 mM | >12748 | 34.86 nM | 8.179 μM | 234.6 |
Compound 2 | 1.077 μM | >1 mM | >928 | 1.115 μM | 2.626 μM | 2.35 |
Compound 3 | 80.52 nM | >1 mM | >12419 | 16.08 nM | 0.3952 μM | 24.6 |
Compound 4 | 13.36 nM | >1 mM | >74850 | 2.815 nM | 0.107 μM | 38 |
Compound 5 | 49.46 nM | >1 mM | >20218 | 26.47 nM | 1.687 μM | 63.7 |
Compound 6 | 294.7 nM | >1 mM | >3393 | 15.99 nM | 0.6664 μM | 41.7 |
2.3. In Silico Study of the Activities of Compounds
3. Experimental
3.1. General
3.2. Plant Material
3.3. Extraction and Isolation
3.4. Computational Methods
3.5. Biological Testing of Compounds
4. Conclusions
Supplementary Materials
Acknowledgments
Conflict of Interest
- Sample Availability: Contact the authors.
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Guo, J.; Zhou, L.-Y.; He, H.-P.; Leng, Y.; Yang, Z.; Hao, X.-J. Inhibition of 11b-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui. Molecules 2012, 17, 11826-11838. https://doi.org/10.3390/molecules171011826
Guo J, Zhou L-Y, He H-P, Leng Y, Yang Z, Hao X-J. Inhibition of 11b-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui. Molecules. 2012; 17(10):11826-11838. https://doi.org/10.3390/molecules171011826
Chicago/Turabian StyleGuo, Jie, Li-Yan Zhou, Hong-Ping He, Ying Leng, Zhen Yang, and Xiao-Jiang Hao. 2012. "Inhibition of 11b-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui" Molecules 17, no. 10: 11826-11838. https://doi.org/10.3390/molecules171011826