Cruz R, Quintana-Hau J D, González J R, Tornero-Montaño R, Baiza-Durán L M, Vega L
Sección Externa de Toxicología, CINVESTAV, Av. IPN 2508, San Pedro Zacatenco, Mexico DF, 07360, Mexico.
Br J Ophthalmol. 2008 Jan;92(1):120-5. doi: 10.1136/bjo.2007.125179. Epub 2007 Oct 25.
To determine the efficacy of meloxicam ophthalmic formulation on COX-2 activity and expression, inflammation-related cytokines expression and inflammation in an ocular inflammation model.
Ocular inflammation was induced in New Zealand rabbits by topical application of croton oil (3%) for 3 h. An ophthalmic solution of 0.03% meloxicam, 0.1% sodium diclofenac or vehicle (Sophisen) was administered every 4 h. Conjunctiva, cornea, aqueous humour and vitreous humour were collected.
In irritated eyes, 72 h of meloxicam treatment downregulated COX-2 expression and activity (mRNA by RT-PCR and PGE2 levels by ELISA, respectively) in a time-dependent manner and reduced inflammation. Meanwhile, diclofenac failed to reduce COX-2 mRNA or PGE2 to basal levels after 7 days of treatment. Meloxicam treatment downregulated IL-6 and IFN-gamma expression in the conjunctiva and IL-1beta and TNF-alpha expression in the cornea. Diclofenac failed to modify these cytokines in both tissues. Meloxicam treatment increased the expression of IL-6 in conjunctiva, and IL-10 in cornea, while diclofenac had no effect on these cytokines.
Meloxicam treatment was more efficient than diclofenac in downregulating the expression and activity of COX-2, reducing inflammation, and modifying the inflammatory-related cytokines.
在眼部炎症模型中确定美洛昔康眼用制剂对COX-2活性与表达、炎症相关细胞因子表达及炎症的疗效。
通过局部应用3%巴豆油3小时诱导新西兰兔发生眼部炎症。每4小时给予0.03%美洛昔康、0.1%双氯芬酸钠眼药水或赋形剂(Sophisen)。收集结膜、角膜、房水和玻璃体。
在受刺激的眼睛中,美洛昔康治疗72小时以时间依赖性方式下调COX-2表达和活性(分别通过RT-PCR检测mRNA和ELISA检测PGE2水平)并减轻炎症。同时,双氯芬酸钠治疗7天后未能将COX-2 mRNA或PGE2降至基础水平。美洛昔康治疗下调结膜中IL-6和IFN-γ的表达以及角膜中IL-1β和TNF-α的表达。双氯芬酸钠未能改变这两种组织中的这些细胞因子。美洛昔康治疗增加结膜中IL-6的表达以及角膜中IL-10的表达,而双氯芬酸钠对这些细胞因子无影响。
在下调COX-2的表达和活性、减轻炎症以及改变炎症相关细胞因子方面,美洛昔康治疗比双氯芬酸钠更有效。