Study of the anti-inflammatory and analgesic effects of novel rigid benzofuran-3, 4-dihydroxy chalcone by formalin, hot-plate and carrageenan tests in mice.
It is reported that dihydroxy chalcones have analgesic and anti-inflammatory effects. Study of the structure activity relationship (SAR) shows that benzofuran-3-one derivatives may be more effective in this respect. In this study, a new (Z)-2-(3,4-dihydroxybenzylidene)-5-methoxybenzofuran-3(2H)-one (compound 5) was synthesized and its analgesic and anti-inflammatory effects were evaluated by formalin, carrageenan and hot-Plate methods in mice. The results showed that, compound 5 induced significant antinociceptive and anti-inflammatory effect (P<0.01). Maximum analgesia (42.6%) was obtained at dose of 25 mg/kg in the first phase of formalin test. The effect of compound 5 was higher (87.7%) in chronic phase of inflammation induced by formalin (P<0.01). Administration of 25 mg/kg of compound 5 inhibited the inflammation induced by carrageenan, 32.8% and 41.7%, 1 and 3 hour after carrageenan injection, respectively. In addition, this dose of compound 5, induces significant analgesia (20.2%) in hot plate test 45 minutes after injection (P<0.01). Therefore it seems that compound 5 has potential for discovery of a compound with potent anti-inflammatory and analgesic effects and its scaffold could be use for further structural modifications.
Heidari
Mahmoud Reza
MR
Department of Toxicology and Pharmacology, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran. heidarimr@kmu.ac.ir
Foroumadi
Alireza
A
Noroozi
Hojat
H
Samzadeh-Kermani
Ali
A
Azimzadeh
Behzad Sarvar
BS
D018712:Analgesics, Non-Narcotic / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D001572:Benzofurans / Q000494:pharmacology*; D002351:Carrageenan; D002599:Chalcone / Q000031:analogs & derivatives* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000139:chemically induced / Q000473:pathology / Q000517:prevention & control*; D005528:Foot / Q000473:pathology; D005557:Formaldehyde; D006358:Hot Temperature; D008297:Male; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects*
C545429:2-(3,4-dihydroxybenzylidene)-5-methoxybenzofuran-3(2H)-one; D018712:Analgesics, Non-Narcotic; D000893:Anti-Inflammatory Agents; D001572:Benzofurans; D005557:Formaldehyde; D002599:Chalcone; D002351:Carrageenan