摘要
目的建立没食子酸冰片酯的合成方法,并研究其体外抗氧化作用。方法以没食子酸、冰片为原料,在氮气保护下采用1,3-二环己基碳二亚胺(DDC)缩合制备没食子酸冰片酯,进一步通过自由基清除实验,考察了没食子酸冰片酯对1,1-二苯基-2-三硝基苯肼自由基(DPPH·)、羟自由基(OH·)和超氧阴离子自由基(O_(2)^(-)·)的体外清除率。结果没食子酸冰片酯的结构通过核磁共振(NMR)图谱、高分辨液质联用(HRHPLC-MS)的综合解释加以确证。体外自由基清除实验显示,没食子酸冰片酯能有效清除DPPH·和O_(2)^(-)·两种自由基,清除率优于没食子酸和维生素C,且没食子酸冰片酯的抗氧化能力与其浓度剂量呈现依赖关系,没食子酸冰片酯对DPPH·和O_(2)^(-)·的半数清除率浓度分别是6.17和68.7μg·mL^(-1)。但与维生素C相比,没食子酸冰片酯清除OH·的能力较弱,半数清除率为150μg·mL^(-1)。结论所建立的没食子酸冰片酯的合成方法简单易行,没食子酸冰片酯表现出良好的抗氧化活性,值得进一步深入研发。
Objective To establish the synthetic method of bornyl gallate and to study its antioxidant activity in vitro.Methods 1,3-Dicyclohexylcarbodiimide(DCC)condensation was conducted to prepare bornyl gallate by using gallic acid and borneol as raw materials under the protection of nitrogen.Then in vitro scavenging rates of bornyl gallate against1,1-diphenyl-2-trichronitrophenylhydrazine radical(DPPH·),hydroxyl radical(OH·)and superoxide anion radical(O_(2)^(-)·)were investigated through free radical scavenging experiment.Results The structure of bornyl gallate was confirmed by nuclear magnetic resonance(NMR)and high-resolution liquid chromatography-mass spectrometry(HRHPLC-MS).In vitro free radical scavenging experiment showed that bornyl gallate could effectively scavenge two kinds of free radicals(DPPH·and O_(2)^(-)·).The scavenging rates of bornyl gallate against DPPH·and O_(2)^(-)·are better than those of gallic acid and vitamin C.Moreover,the antioxidant capacity of bornyl gallate was dependent on its concentration.The half scavenging rates of bornyl gallate to DPPH·,O_(2)^(-)·were 6.17 and 68.7μg·mL^(-1),respectively.However,compared to standard drug vitamin C,bornyl gallate exhibited a weaker antioxidant activity against OH·,and the half scavenging rate was 150μg·mL^(-1).Conclusion The developed method for the synthesis of bornyl gallate is simple and easy to implement.Bornyl gallate exhibits good antioxidant activity and is worthy of further research and development.
作者
余梓楷
柏心瑜
王涛
YU Zikai;BAI Xinyu;WANG Tao(School of Pharmaceutical Sciences,Guangzhou University of Chinese Medicine,Guangzhou 510006 Guangdong,China)
出处
《中药新药与临床药理》
CAS
CSCD
北大核心
2023年第8期1129-1133,共5页
Traditional Chinese Drug Research and Clinical Pharmacology
基金
国家自然科学基金项目(30701100)
广州中医药大学“双一流”与高水平大学学科协同创新团队项目(2021xk87)。
