Anti-inflammatory and gastroprotective properties of some chalcones.
The synthesis of 1,3-diaryl propen-1-ones (chalcones) by the Claisen-Schmidt condensation between acetophenones and benzaldehydes in potassium hydroxide/methanol medium at room temperature yielded: 1-(4-nitrophenyl)-3-(2,4,6-trimethoxyphenyl)propen-1-one (3a), 1-(4-nitrophenyl)-3-(3-bromophenyl)propen-1one (3b), 1-(4-methoxyphenyl)-3-(3-bromophenyl)propen-1-one (3c), 1-(4-methoxyphenyl)-3-(2,4,6-trimethoxyphenyl)propen-1-one (3d), 1-(2,4-dihydroxyphenyl)-3-(phenyl)propen-1-one (3e), 1-(4-nitrophenyl)-3-(4-chlorophenyl)propen-1-one (3f) which were evaluated for anti-inflammatory activity at doses of 20, 40 and 80mg/kg. The compounds were found to be effective inhibitors of carrageenan-induced rat paw edema in Wistar rats and this activity was dose dependent and increased between the third and fourth hour. The gastroprotective activity of the compounds was investigated (using 200 mg/kg acetylsalicylic acid-induced ulceration) in Wistar rats at a single dose of 100 mg/kg for all the compounds synthesized and compound 3d had significant activity (p<0.001) comparable to cimetidine. The compounds were found to have anti-inflammatory and anti-ulcer activities at the doses employed.
Okunrobo
Lucky O
LO
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Benin, Benin City, Nigeria. bricyedo@yahoo.com
Usifoh
Cyril O
CO
Uwaya
John O
JO
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology*; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D047188:Chalcones / Q000138:chemical synthesis / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D005260:Female; D008297:Male; D051381:Rats; D017208:Rats, Wistar
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000897:Anti-Ulcer Agents; D047188:Chalcones