Curcumin Stereoisomer, Cis-Trans Curcumin, as a Novel Ligand to A1 and A3 Adenosine Receptors
نویسندگان
چکیده
Adenosine receptors (ARs) are being explored to generate non-opioid pain therapeutics. Vanilloid compounds, curcumin, capsaicin, and vanillin possess antinociceptive properties through their interactions with the transient receptor potential channel family. However, binding adenosine has not been well studied. The hypothesis in this study was that a vanilloid compound, cis-trans curcumin (CTCUR), binds each of two Gi-linked AR subtypes (A1AR A3AR). CTCUR synthesized from (CUR) using cavitand-mediated photoisomerization technique. cell lines transfected specific or A3AR) were treated CUR analyzed competitive assays, confocal microscopy, docking. assays molecular docking indicated had Ki values 306 nM (A1AR) 400 (A3AR). These suggest is selective for ARs over Gs-linked (A2AAR A2BAR), based on our previous published research. In addition, showed toggle switch domain ARs. Curcumin did exhibit at any these receptors. summary, other modifications can be developed as novel therapeutic ligands involved cancer.
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ژورنال
عنوان ژورنال: Pharmaceuticals
سال: 2023
ISSN: ['1424-8247']
DOI: https://doi.org/10.3390/ph16070917