Dipartimento Farmacobiologico, Università Magna Græcia di Catanzaro Complesso Ninì Barbieri, 88021, Roccelletta di Borgia (CZ), Italy.
J Nat Prod. 2011 Nov 28;74(11):2377-81. doi: 10.1021/np200405s. Epub 2011 Oct 20.
Hydroxytyrosol is a potent antioxidant natural molecule isolated from olive leaves and fruits. The presence of three hydroxy groups in its structure poses a limit for the topical application of this lead compound. A set of hydroxytyrosol conjugates with fatty acids at different molecular weights were synthesized under mild conditions. The topical delivery features of this new set of antioxidant molecules were evaluated as a function of their permeation profiles through the human stratum corneum and viable epidermis membranes. A dependence on their partition coefficients, their molecular weights, and their isometric configurations was then postulated. Encouraging results prompt further investigations on the polyfunctional role that hydroxytyrosol conjugates could have as agents in both anti-inflammatory and antioxidant therapies.
羟基酪醇是一种从橄榄叶和果实中分离出来的强效抗氧化天然分子。其结构中存在三个羟基基团，这对这种先导化合物的局部应用构成了限制。在温和的条件下，合成了一组具有不同分子量的脂肪酸羟基酪醇缀合物。作为其通过人角质层和活表皮膜渗透特性的函数，评估了这组新型抗氧化分子的局部递药特征。然后提出了对其分配系数、分子量和等规构型的依赖性。令人鼓舞的结果促使进一步研究羟基酪醇缀合物作为抗炎和抗氧化治疗剂的多功能作用。
