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天然及类天然多酚化合物：抗氧化活性及治疗应用潜力

Natural and natural-like polyphenol compounds: antioxidant activity and potential for therapeutic application.

作者信息

Brboric Jasmina, Klisic Aleksandra, Kotur-Stevuljevic Jelena, Delogu Giovanna, Gjorgieva Ackova Darinka, Kostic Kristina, Antonietta Dettori Maria, Fabbri Davide, Carta Paola, Saso Luciano

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Serbia, Serbia.

Primary Health Care Center, University of Montenegro, Faculty of Medicine, Podgorica, Montenegro, Montenegro.

出版信息

Arch Med Sci. 2021 Apr 18;19(3):651-671. doi: 10.5114/aoms/135379. eCollection 2023.

DOI:10.5114/aoms/135379
PMID:37313202
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10259401/
Abstract

INTRODUCTION

Phenols are a large family of natural and synthetic compounds with known antioxidant activity. The aim of this study was to perform screening of natural and natural-like phenol monomers and their C2-symmetric dimers (hydroxylated biphenyls) in order to identify those representatives whose pharmacophores have the strongest antioxidant and the lowest prooxidant activity.

MATERIAL AND METHODS

Antioxidative properties of 36 compounds (monomers and their C2-symmetric dimers) were evaluated . Different (red/ox) assays were used to measure their total oxidative potential (TOP), their total antioxidative capacity (TAC), the pro-oxidative-antioxidant balance (PAB) and total SH-group content (SHG) in a biologically relevant environment. The Pro-oxidative Score, Antioxidative Score and the Oxy Score were also calculated. Trolox, a water soluble analogue of α-tocopherol, was used as a positive control.

RESULTS

In an assay consisting of pooled human serum, 6 of the 36 compounds showed significant antioxidant activity (compounds 6, 7, 12, 13, 26, and 27), whereas 4 showed extremely weak antioxidant activity (compounds 2, 29, 30, and 31). Within the 36 compounds comprising zingerone, dehydrozingerone, aurone, chalcone, and magnolol derivatives, in both monomeric and dimeric forms, the 2 compounds that indicated the highest antioxidant activity were dehydrozingerone derivatives (compounds 6 and 12). Trolox's activity was found between the strong and weak antioxidant compounds analysed in our study.

CONCLUSIONS

In this study selected dehydrozingerones were identified as good candidates for in-depth testing of their biological behaviour and for possible precursors for synthesis of novel polyphenolic molecules with potential therapeutic applications.

摘要

引言

酚类是一大类具有已知抗氧化活性的天然和合成化合物。本研究的目的是对天然和类天然酚单体及其C2对称二聚体（羟基联苯）进行筛选，以确定那些药效基团具有最强抗氧化活性和最低促氧化活性的代表物。

材料与方法

评估了36种化合物（单体及其C2对称二聚体）的抗氧化性能。使用不同的（氧化/还原）测定法来测量它们在生物相关环境中的总氧化电位（TOP）、总抗氧化能力（TAC）、促氧化-抗氧化平衡（PAB）和总SH基团含量（SHG）。还计算了促氧化评分、抗氧化评分和氧评分。α-生育酚的水溶性类似物Trolox用作阳性对照。

结果

在一项由混合人血清组成的测定中，36种化合物中的6种表现出显著的抗氧化活性（化合物6、7、12、13、26和27），而4种表现出极弱的抗氧化活性（化合物2、29、30和31）。在包含姜辣素、脱氢姜辣素、橙酮、查尔酮和厚朴酚衍生物的36种化合物中，无论是单体形式还是二聚体形式，抗氧化活性最高的2种化合物是脱氢姜辣素衍生物（化合物6和12）。发现Trolox的活性介于我们研究中分析的强抗氧化和弱抗氧化化合物之间。

结论

在本研究中，选定的脱氢姜辣素被确定为深入测试其生物学行为的良好候选物，以及可能用于合成具有潜在治疗应用的新型多酚分子的前体。

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