Inhibition of ocular inflammation by chalcone derivatives and prednisolone.
Posterior uveitis was induced by injection of 10 micrograms endotoxin intravitreally into rat eyes and anterior ocular inflammation was induced by injection of 0.75 mg of lens protein intracamerally into rabbit eyes. Four chalcone derivatives, RVC-556 (2'-hydroxychalcone), RVC-574 (2'-hydroxychalcone hydrazone), RVC-574P (2'-hydroxychalcone phenyl hydrazone) and RVC-588 (4,4'-dihydroxy chalcone) were studied along with prednisolone at a dose of 10 mg/kg i.p. t.i.d. for their anti-inflammatory actions. RVC-574 was more active than prednisolone in inhibiting posterior uveitis by 65% and 43%, respectively. RVC-556, RVC-574P, and RVC-588 did not affect the posterior uveitis in rats. On the other hand, anterior ocular inflammation was inhibited by 1% eyedrops of RVC-556, RVC-574P and RVC-588 but not by RVC-574. RVC-556 was more active than; RVC-574P was less active than; and RVC-588 was about equiactive as prednisolone in inhibiting anterior ocular inflammation by 77%, 47%, 69%, and 64%, respectively.
Chiou
G C
GC
Institute of Ocular Pharmacology, Texas A&M University College of Medicine, College Station.
Yao
Q S
QS
Varma
R S
RS
D000818:Animals; D002599:Chalcone / Q000031:analogs & derivatives* / Q000627:therapeutic use; D003459:Crystallins; D004731:Endotoxins; D005260:Female; D007274:Injections, Intraperitoneal; D008297:Male; D009883:Ophthalmic Solutions; D011239:Prednisolone / Q000627:therapeutic use*; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D014606:Uveitis, Anterior / Q000139:chemically induced / Q000188:drug therapy*; D015866:Uveitis, Posterior / Q000139:chemically induced / Q000188:drug therapy*
D003459:Crystallins; D004731:Endotoxins; D009883:Ophthalmic Solutions; D002599:Chalcone; D011239:Prednisolone