Department of Drug Sciences, University of Catania, Catania, Italy.
ARPACAL, Catanzaro, Italy.
J Pharm Pharmacol. 2017 Nov;69(11):1502-1512. doi: 10.1111/jphp.12807. Epub 2017 Sep 6.
The purpose of this study was the evaluation of the antioxidant activity of natural and semisynthetic polyphenol derivatives from Olea europea L., by assessing malondialdehyde (MDA), an important marker of oxidative stress.
Polyphenol as hydroxytyrosol, oleuropein, oleuropein aglycone as mix of four tautomeric forms and their respective acetyl-derivatives were obtained from olive leaves using semisynthetic protocols. These compounds were administered intraperitoneally to Wistar rats treated with paraquat, an herbicide which is able to cause oxidative stress after central administration. Malondialdehyde was derivatized with 2,4-dinitrophenylhydrazine to produce hydrazone that was purified by solid-phase extraction. Using high-performance liquid chromatography coupled with a diode array, free and total MDA was measured on homogenate rat brain as marker of lipid peroxidation. The analytical method was fully validated and showed linearity in the tested concentration range, with detection limit of 5 ng/ml. Recovery ranged from 94.1 to 105.8%.
Both natural and semisynthetic polyphenol derivatives from a natural source as olive leaves were able to reduce MDA detection. The more lipophilic acetyl-derivatives showed an antioxidant activity greater than parent compounds. This potency seems to put in evidence a strict correlation between lipophilicity and bioavailability.
本研究旨在评估从欧洲油橄榄(Olea europea L.)中提取的天然和半合成多酚衍生物的抗氧化活性,通过评估丙二醛(MDA)来衡量氧化应激的程度。
采用半合成方法从橄榄叶中提取羟基酪醇、橄榄苦苷、橄榄苦苷苷元(四种互变异构形式的混合物)及其各自的乙酰衍生物。将这些化合物腹腔内给药给用百草枯处理的 Wistar 大鼠,百草枯是一种中枢给药后能够引起氧化应激的除草剂。用 2,4-二硝基苯肼将丙二醛衍生化生成腙,然后通过固相萃取对其进行纯化。采用高效液相色谱-二极管阵列检测法,以匀浆大鼠脑为脂质过氧化标志物,检测游离和总 MDA。该分析方法经过全面验证,在测试浓度范围内呈线性,检测限为 5ng/ml。回收率在 94.1%至 105.8%之间。
天然和半合成多酚衍生物都具有抗氧化活性,能够降低 MDA 的检测水平。亲脂性更强的乙酰衍生物比母体化合物表现出更强的抗氧化活性。这种效力似乎表明亲脂性与生物利用度之间存在严格的相关性。