The Bioactive Phenolic Agents Diaryl Ether CVB2-61 and Diarylheptanoid CVB4-57 as Connexin Hemichannel Blockers
Abstract
:1. Introduction
2. Results
2.1. Synthesis of the Bioactive Phenolic Agents CVB2-61 and CVB4-57
2.2. Connexin Expression in N2A and HeLa Cells
2.3. Functionality of Expressed Cx Hemichannels
2.4. Inhibition of Cx Hemichannels
3. Discussion
4. Materials and Methods
4.1. Chemical Synthesis of the Bioactive Agent CVB4-57
4.1.1. General
4.1.2. 1-(4-((Tert-butyldimethylsilyl)oxy)phenethyl)piperazine
4.1.3. 1-(3-Bromo-4-methoxybenzyl)-4-(4-((tert-butyldimethylsilyl)oxy)phenethyl)piperazine
4.1.4. 4-(2-(4-(3-Bromo-4-methoxybenzyl)piperazin-1-yl)ethyl)phenol: CVB4-57
4.2. Materials
4.3. Molecular Cloning and Transfection
4.4. Immunofluorescence Staining
4.5. Dye-Uptake Assay
4.6. Transepithelial Electrical Restistance (TEER) Measurement
4.7. Gold-Nanoparticle-Mediated Laser Perforation/Dye Transfer (GNOME-LP/ DT)
4.8. Statistical Analyses
5. Conclusions
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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Primer | 5’-3’ Sequence |
---|---|
GW_BP-cloning hCx26 attB1 F | GGGGACAAGTTTGTACAAAAAAGCAGGCTTAATGGATTGGGGCACGCT |
GW_BP-cl. hCx26 stop attB2 R | GGGACCACTTTGTACAAGAAAGCTGGGTTCTAAACTGGCTTTTTTGACTTCCCAGAAC |
GW_BP-cloning hCx46 attB1 F | GGGGACAAGTTTGTACAAAAAAGCAGGCTCCATGGGCGACTGGAGCTTTCTGG |
GW_BP-cl. hCx46 stop attB2 R | GGGGACCACTTTGTACAAGAAAGCTGGGTTCTAGATGGCCAAGTCCTCCGGT |
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Dierks, A.; Vanucci-Bacqué, C.; Schäfer, A.-M.; Lehrich, T.; Ruhe, F.; Schadzek, P.; Bedos-Belval, F.; Ngezahayo, A. The Bioactive Phenolic Agents Diaryl Ether CVB2-61 and Diarylheptanoid CVB4-57 as Connexin Hemichannel Blockers. Pharmaceuticals 2022, 15, 1173. https://doi.org/10.3390/ph15101173
Dierks A, Vanucci-Bacqué C, Schäfer A-M, Lehrich T, Ruhe F, Schadzek P, Bedos-Belval F, Ngezahayo A. The Bioactive Phenolic Agents Diaryl Ether CVB2-61 and Diarylheptanoid CVB4-57 as Connexin Hemichannel Blockers. Pharmaceuticals. 2022; 15(10):1173. https://doi.org/10.3390/ph15101173
Chicago/Turabian StyleDierks, Anne, Corinne Vanucci-Bacqué, Anne-Marie Schäfer, Tina Lehrich, Frederike Ruhe, Patrik Schadzek, Florence Bedos-Belval, and Anaclet Ngezahayo. 2022. "The Bioactive Phenolic Agents Diaryl Ether CVB2-61 and Diarylheptanoid CVB4-57 as Connexin Hemichannel Blockers" Pharmaceuticals 15, no. 10: 1173. https://doi.org/10.3390/ph15101173