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.
Department of Toxicology and Pharmacology, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran. heidarimr@kmu.ac.ir
Mahmoud Reza
MR
Heidari
Alireza
A
Foroumadi
Hojat
H
Noroozi
Ali
A
Samzadeh-Kermani
Behzad Sarvar
BS
Azimzadeh
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