Casagrande Rúbia, Georgetti Sandra R, Verri Waldiceu A, Dorta Daniel J, dos Santos Antônio C, Fonseca Maria J V
Department of Pharmaceutical Science, Faculty of Pharmaceutical Sciences of Ribeirao Preto - USP, Av. do Café s/n, CEP 14040-903, Ribeirao Preto, SP, Brazil.
J Photochem Photobiol B. 2006 Jul 3;84(1):21-7. doi: 10.1016/j.jphotobiol.2006.01.006. Epub 2006 Feb 21.
UV radiation-induced skin damages may result in pre-cancerous and cancerous skin lesions, and acceleration of skin aging. It involves an imbalance of the endogenous antioxidant system that leads to the increase of free radical levels and inflammation. Therefore, antioxidant supplementation might inhibit such imbalance. In this regard, quercetin is a promising drug, this plant derived lipophilic flavonoid presents the higher antioxidant activity among flavonoids and multiple antioxidant mechanisms. Thus, the present study investigated the possible beneficial effects of topical formulations containing quercetin to inhibit UVB irradiation-induced oxidative damages. Quercetin was administered on the dorsal skin of hairless mice using two formulations, formulation 1 (non-ionic emulsion with high lipid content) and formulation 2 (anionic emulsion with low lipid content). The UVB irradiation (0.31-3.69 J/cm(2)) induced a dose-dependent increase in the myeloperoxidase (MPO) activity (4-2708%) and depletion of reduced glutathione (GSH) (22-68%) in the skin of hairless mice after 6h. These results demonstrated that the UVB doses are not excessive, and additionally, they are lower than the doses used in other similar studies. Proteinases secretion/activity, detected by the qualitative sodium dodecyl sulphate polyacrylamide gel electrophoresis substrate-embedded enzymography (zymography), was also enhanced in the same manner as MPO activity using the UVB dose of 1.23J /cm(2). Formulations 1 and 2 inhibited the MPO activity increase (62% and 59%, respectively), GSH depletion (119% and 53%, respectively) and proteinases secretion/activity. To our knowledge, this is the first study to demonstrate the effectiveness of topical formulations containing quercetin to inhibit the UVB irradiation-induced skin damages. Thus, these data suggest the possible usefulness of topical formulations containing quercetin to prevent UVB radiation skin damages.
紫外线辐射引起的皮肤损伤可能导致癌前和癌性皮肤病变,以及皮肤衰老加速。这涉及内源性抗氧化系统失衡,导致自由基水平升高和炎症。因此,补充抗氧化剂可能会抑制这种失衡。在这方面,槲皮素是一种有前景的药物,这种植物来源的亲脂性黄酮类化合物在黄酮类化合物中具有较高的抗氧化活性和多种抗氧化机制。因此,本研究调查了含槲皮素的局部制剂抑制紫外线B(UVB)辐射诱导的氧化损伤的可能有益作用。使用两种制剂将槲皮素施用于无毛小鼠的背部皮肤,制剂1(高脂质含量的非离子乳液)和制剂2(低脂质含量的阴离子乳液)。UVB辐射(0.31 - 3.69 J/cm²)在6小时后导致无毛小鼠皮肤中髓过氧化物酶(MPO)活性呈剂量依赖性增加(4 - 2708%)和还原型谷胱甘肽(GSH)消耗(22 - 68%)。这些结果表明UVB剂量不过高,此外,它们低于其他类似研究中使用的剂量。使用1.23J/cm²的UVB剂量时,通过定性十二烷基硫酸钠聚丙烯酰胺凝胶电泳底物包埋酶谱法(zymography)检测到的蛋白酶分泌/活性也与MPO活性以相同方式增强。制剂1和制剂2抑制了MPO活性增加(分别为62%和59%)、GSH消耗(分别为119%和53%)以及蛋白酶分泌/活性。据我们所知,这是第一项证明含槲皮素的局部制剂抑制UVB辐射诱导的皮肤损伤有效性的研究。因此,这些数据表明含槲皮素的局部制剂预防UVB辐射皮肤损伤的可能有用性。