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目的对化合物3,4,5-三羟基-N-[2-(4-羟基苯基)乙基]苯甲酰胺(3,4,5-trihydroxy-N-[2-(4-hydroxyphenyl)ethyl]-benzamide,THHEB)的抗氧化活性进行研究。方法通过测定对有机自由基1,1-二苯基苦基苯肼(1,1-diphenyl-2-picrylhydrazyl,DPPH)的清除能力、6-羟基-2,5,7,8-四甲基苯并二氢吡喃-2-羧酸(6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid,Trolox)当量抗氧化能力(trolox-equivalent antioxidant capacity assay,TEAC),测定超氧自由基的清除活性实验、脂质过氧化法以及羟基自由基诱导DNA损伤的方法评价THHEB的抗氧化活性。结果5种方法检测结果均显示,THHEB具有很强的清除自由基的活性。其中,THHEB对稳定自由基DPPH和超氧自由基的清除能力超过抗坏血酸的相应活性,其IC50值分别为22.8、2.5μmol.L-1。用TEAC方法测定THHEB总的抗氧化能力大约为0.6,也比L-抗坏血酸相应值高。脂质过氧化法测定的THHEB活性要弱于著名的抗氧化化合物2,6-二叔基对甲苯酚(butylated hydroxytoluene,BHT)。此外,非常小浓度比如4μmo.lL-1的THHEB对羟基自由基导致的pBR322 DNA链断裂具有显著的保护作用。结论THHEB具有很强的清除自由基的活性。
Aim To investigate the effect of compound 3,4,5-trihydroxy-N- [2- (4-hydroxyphenyl) ethyl ] -benzamide, THHEB). Methods The scavenging capacity of 1,1-diphenyl-2-picrylhydrazyl (DPPH), an organic free radical, Trichloxystroboyl-2,5-dihydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid (Trolox), trolox-equivalent antioxidant capacity assay (TEAC) Oxygen free radical scavenging activity assay, lipid peroxidation method and hydroxyl radical induced DNA damage method to evaluate the antioxidant activity of THHEB. Results The results of the five methods showed that THHEB had a strong activity of scavenging free radicals. Among them, THHEB had more scavenging ability on free radical DPPH and superoxide free radical than that of ascorbic acid with IC50 values of 22.8 and 2.5μmol.L-1, respectively. The total antioxidant capacity of THHEB measured by the TEAC method is about 0.6, which is also higher than that of L-ascorbic acid. The THHEB activity measured by lipid peroxidation was weaker than that of the well-known antioxidant butylated hydroxytoluene (BHT). In addition, THHEB at a very small concentration such as 4 μmo.lL-1 has a significant protective effect on hydroxyl radical-induced pBR322 DNA strand breaks. Conclusion THHEB has a strong free radical scavenging activity.