Structural basis of the anti-inflammatory activity of quercetin: inhibition of the 5-hydroxytryptamine type 2 receptor.
The anti-inflammatory activity of quercetin was evaluated through serotonin-induced rat-paw edema. The experiments showed that quercetin had an important effect on acute inflammatory processes. Docking of serotonin and quercetin into the homology model of the 5-Hydroxytryptamine Type 2 Receptor allowed to analyze the structural basis of the anti-inflammatory activity. Results showed that serotonin and quercetin bind in the same region of the active site with a similar binding energy but quercetin has a much bigger inhibition constant. Therefore, it seems possible that quercetin may act as a natural inhibitor of the receptor blocking the acute inflammation generated by serotonin.
Rotelli
Alejandra Ester
AE
Laboratorio de Farmacologia, Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis, Chacabuco y Pedernera, San Luis, 5700, Argentina. arotelli@unsl.edu.ar
Aguilar
Carlos Fernando
CF
Pelzer
Lilian Eugenia
LE
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D001665:Binding Sites; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy / Q000378:metabolism; D008958:Models, Molecular; D011487:Protein Conformation; D011794:Quercetin / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D017208:Rats, Wistar; D044348:Receptors, Serotonin, 5-HT2 / Q000737:chemistry / Q000378:metabolism; D012701:Serotonin / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D058830:Serotonin 5-HT2 Receptor Antagonists
D000894:Anti-Inflammatory Agents, Non-Steroidal; D044348:Receptors, Serotonin, 5-HT2; D058830:Serotonin 5-HT2 Receptor Antagonists; D012701:Serotonin; D011794:Quercetin