PEG superoxide dismutase derivatives: anti-inflammatory activity in carrageenan pelurisy in rats.
Two derivatives of superoxide dismutase (SOD) with monomethoxypolyethyleneglycol, having different molecular weights (46,000 and 121,000 D) and different plasma half-lives are tested in carrageenan pleurisy in rats after single i.v. injection. The compounds were prepared following an original method where the polymer is activated by trichlorophenylchloroformate to give a phenylcarbonate which is reactive towards the protein amino groups. The anti-inflammatory activity of derivatives results correlated to their kinetics, lasting longer for the derivative with the longest half-life (SOD-PEG 18). SOD activity, in plasma of rats treated with SOD-PEG 18, is still present 24 hour after carrageenan, in agreement with the prolonged anti-inflammatory activity. Moreover SOD-PEG 18 diffuses well in pleural exudate, as it is evidentiated from the increase with time of exudate/plasma concentration ratio.
Conforti
A
A
Istituto di Farmacologia, University of Verona, Italy.
Franco
L
L
Milanino
R
R
Velo
G P
GP
Bocc+53u
E
E
Largajolli
E
E
Schiavon
O
O
Veronese
F M
FM
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001772:Blood Cell Count; D002351:Carrageenan; D005122:Exudates and Transudates / Q000201:enzymology; D005260:Female; D010998:Pleurisy / Q000188:drug therapy* / Q000209:etiology; D011092:Polyethylene Glycols / Q000494:pharmacology*; D051381:Rats; D013482:Superoxide Dismutase / Q000097:blood / Q000378:metabolism / Q000494:pharmacology*; D013997:Time Factors
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011092:Polyethylene Glycols; D002351:Carrageenan; D013482:Superoxide Dismutase