Identification of Interleukin-8-Reducing Lead Compounds Based on SAR Studies on Dihydrochalcone-Related Compounds in Human Gingival Fibroblasts (HGF-1 cells) In Vitro
Abstract
:1. Introduction
2. Results
2.1. Compound Category Effectiveness
2.2. Substitution Pattern Analysis of Aromatic Rings A and B
2.3. Single Substance Matched
Matched Pair Analysis (MPA)
3. Discussion
4. Materials and Methods
4.1. Chemicals
4.2. Compounds
4.3. Cell Culture
4.4. Cell Vitality
4.5. Measurement of IL-8 in Cell Culture Supernatants
4.6. Analysis of IL-8 mRNA Expression in pgLPS-Stimulated HGF-1 Cells Incubated with Selected Dihydrochalcones
4.7. Statistical Analysis
5. Conclusions
Supplementary Materials
Author Contributions
Funding
Acknowledgments
Conflicts of Interest
Appendix A. Preparation and Structure Elucidation of Compounds 6, 10, 11, 15, and 16
Appendix A.1. Compound 6
Appendix A.2. Compound 10
Appendix A.3. Compound 11
Appendix A.4. Compound 15
Appendix A.5. Compound 16
References
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Sample Availability: Samples of the compounds are not available from the authors. Most compounds (1–5, 7–9, 12–14, 17 and 18) are commercially available. However, the authors described the preparation of the commercially non-available compounds (6, 10, 11, 15 and 16) in the appendix to allow other researchers the repreparation of these compounds. |
No | Common Name | Structure | AUC (1–100 µM) Mean ±SD |
---|---|---|---|
A,C-bicyclic system with solitary Bring | | - | |
- | A-ring-linker-B-ring system | | - |
1 | Neohesperidin dihydrochalcone | | 7930 ± 1730 |
2 | Neohesperidin | | 9111 ± 2497 |
3 | Hesperidin | | 6648 ± 1589 |
4 | Hesperetin | | 7740 ± 1782 |
5 | Liquiritigenin | | 8942 ± 2450 |
6 | Hesperetin dihydrochalcone | | 5945 ± 969 |
7 | 2′,4,4′,6′-tetrahydroxy 3-methoxydihydrochalcone | | 3303 ± 816 |
8 | Phloretin | | 7872 ± 629 |
9 | Davidigenin | | 6527 ± 1625 |
10 | 2′,4,4′-trihydroxy 3-methoxydihydrochalcone | | 5052 ± 596 |
11 | 2′,3,4′-trihydroxy 4-methoxydihydrochalcone | | 5626 ± 614 |
12 | 4,4′-dihydroxy 3-methoxydihydrochalcone- | | 6940 ± 950 |
13 | 4-hydroxybenzoic acid N-vanillylamide | | 4363 ± 696 |
14 | 2,4-dihydroxybenzoic acid N-vanillylamide | | 7558 ± 973 |
15 | 3′,5,7,-trihydroxy 4′-methoxyflavan | | 7341 ± 942 |
16 | 3′,7-dihydroxy 4′-methoxyflavan | | 9063 ± 1511 |
17 | 3′methoxy 2,4,4′-trihydroxydeoxybenzoin | | 6378 ± 1389 |
18 | Resveratrol | | 6512 ± 1761 |
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Schueller, K.; Hans, J.; Pfeiffer, S.; Walker, J.; Ley, J.P.; Somoza, V. Identification of Interleukin-8-Reducing Lead Compounds Based on SAR Studies on Dihydrochalcone-Related Compounds in Human Gingival Fibroblasts (HGF-1 cells) In Vitro. Molecules 2020, 25, 1382. https://doi.org/10.3390/molecules25061382
Schueller K, Hans J, Pfeiffer S, Walker J, Ley JP, Somoza V. Identification of Interleukin-8-Reducing Lead Compounds Based on SAR Studies on Dihydrochalcone-Related Compounds in Human Gingival Fibroblasts (HGF-1 cells) In Vitro. Molecules. 2020; 25(6):1382. https://doi.org/10.3390/molecules25061382
Chicago/Turabian StyleSchueller, Katharina, Joachim Hans, Stefanie Pfeiffer, Jessica Walker, Jakob P. Ley, and Veronika Somoza. 2020. "Identification of Interleukin-8-Reducing Lead Compounds Based on SAR Studies on Dihydrochalcone-Related Compounds in Human Gingival Fibroblasts (HGF-1 cells) In Vitro" Molecules 25, no. 6: 1382. https://doi.org/10.3390/molecules25061382