Chiou G C, Yao Q S, Varma R S
Institute of Ocular Pharmacology, Texas A&M University College of Medicine, College Station.
J Ocul Pharmacol. 1992 Fall;8(3):213-23. doi: 10.1089/jop.1992.8.213.
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.
通过向大鼠眼玻璃体内注射10微克内毒素诱导后葡萄膜炎,通过向兔眼前房内注射0.75毫克晶状体蛋白诱导眼前部炎症。研究了四种查尔酮衍生物,即RVC - 556(2'-羟基查尔酮)、RVC - 574(2'-羟基查尔酮腙)、RVC - 574P(2'-羟基查尔酮苯腙)和RVC - 588(4,4'-二羟基查尔酮),以及剂量为10毫克/千克腹腔注射、每日三次的泼尼松龙的抗炎作用。RVC - 574在抑制后葡萄膜炎方面比泼尼松龙更有效,分别抑制了65%和43%。RVC - 556、RVC - 574P和RVC - 588对大鼠的后葡萄膜炎没有影响。另一方面,1%的RVC - 556、RVC - 574P和RVC - 588滴眼液可抑制眼前部炎症,但RVC - 574不能。在抑制眼前部炎症方面,RVC - 556比泼尼松龙更有效;RVC - 574P比泼尼松龙效果差;RVC - 588与泼尼松龙效果相当,分别抑制了77%、47%、69%和64%。