具有抗氧化、抗炎和降血脂功能的阿魏酸、芥子酸、3,4-二甲氧基肉桂酸和吲哚美辛衍生物,Antioxidants

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具有抗氧化、抗炎和降血脂功能的阿魏酸、芥子酸、3,4-二甲氧基肉桂酸和吲哚美辛衍生物
Antioxidants ( IF 6.0 ) Pub Date : 2023-07-17 , DOI: 10.3390/antiox12071436
Panagiotis Theodosis-Nobelos ₁ , Georgios Papagiouvannis ₁ , Eleni A Rekka ₂

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合成了一系列与含有肉桂酸的部分（如阿魏酸、芥子酸和 3,4-二甲氧基肉桂酸）缀合的硫代吗啉和肉桂醇衍生物，并测试了它们的抗氧化、抗炎和降血脂特性。为了进行比较，还制备了2,6-二叔丁基-4-(羟甲基)苯酚的吲哚美辛酯。大多数化合物表现出相当大的抗氧化能力和自由基清除活性，达到与众所周知的抗氧化剂维生素E类似的水平。其中一些对减少角叉菜胶引起的大鼠爪水肿具有增强的抗炎作用（150 μmol/kg 时范围为 17-72%），其活性与用作 NSAID（非甾体抗炎药）的活性相当。参考。它们对大豆脂氧合酶抑制具有中等活性。所有测试的化合物在 Triton 诱导的大鼠高脂血症中均表现出血脂指数显着降低，而最活跃的甘油三酯和总胆固醇在 150 μmol/kg (ip) 时分别降低了 72.5% 和 76%，略好于 150 μmol/kg (ip)。辛伐他汀是一种著名的降胆固醇药物，但其降低甘油三酯的作用可以忽略不计。由于我们设计的化合物似乎表现出多种药理活性，因此它们可用于涉及炎症、氧化应激、血脂失调和退行性疾病的场合。

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Ferulic, Sinapic, 3,4-Dimethoxycinnamic Acid and Indomethacin Derivatives with Antioxidant, Anti-Inflammatory and Hypolipidemic Functionality

A series of thiomorpholine and cinnamyl alcohol derivatives, conjugated with cinnamic acid-containing moieties, such as ferulic acid, sinapic acid and 3,4-dimethoxycinnamic acid, were synthesized and tested for their antioxidant, anti-inflammatory and hypolipidemic properties. An indomethacin ester with 2,6-di-tert-butyl-4-(hydroxymethyl)phenol was also prepared for reasons of comparison. The majority of the compounds demonstrated considerable antioxidant capacity and radical scavenging activity, reaching up to levels similar to the well-known antioxidant trolox. Some of them had an increased anti-inflammatory effect on the reduction of carrageenan-induced rat paw edema (range 17–72% at 150 μmol/kg), having comparable activity to the NSAIDs (non-steroidal anti-inflammatory drugs) used as reference. They had moderate activity in soybean lipoxygenase inhibition. All the tested compounds exhibited a significant decrease in lipidemic indices in Triton-induced hyperlipidemia in rats, whilst the most active triglycerides and total cholesterol decreased by 72.5% and 76%, respectively, at 150 μmol/kg (i.p.), slightly better than that of simvastatin, a well-known hypocholesterolemic drug, but with negligible triglyceride-lowering effect. Since our designed compounds seem to exhibit multiple pharmacological activities, they may be of use in occasions involving inflammation, oxidative stress, lipidemic deregulation and degenerative conditions.

更新日期：2023-07-18

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