芦丁酯的酶催化区域选择性合成及其抗氧化活性研究进展

Research progress on enzymatic regioselective synthesis of rutin and its antioxidant activity

中文关键词:  芦丁  脂溶性  脂肪酶  区域选择性  抗氧化

英文关键词:rutin  lipid solubility  lipase  regioselectivity  antioxidant

中文摘要:

      芦丁即槲皮素-3-O-芸香糖苷, 是存在于苦荞、芸香、槐树等的天然类黄酮类化合物。芦丁具有抗氧化、降糖、预防心血管疾病等生物活性, 但低溶解度限制了其实际应用。通过对芦丁结构进行亲油修饰合成芦丁酯, 可以有效改善脂溶性, 提高生物利用率。本文详细综述了非水相酶催化合成芦丁酯的研究进展, 重点介绍了酶种类、反应介质、酰基供体等因素对芦丁酯酶促合成规律的影响。酶促合成芦丁酯的难点在于芦丁含多个羟基及其与酰基供体的不互溶性, 本文总结了芦丁的修饰位点, 提出了通过介质复配、物理辅助手段改善底物溶解性, 通过筛选酶、酶修饰等可以得到高区域选择性的芦丁酯; 进一步阐述了酰化修饰对芦丁抗氧化活性的影响, 并总结了现有芦丁酯的分离纯化策略; 最后展望了芦丁酯的未来研究方向, 对今后芦丁酯的深入研究与开发利用具有指导意义。

英文摘要:

      Rutin, or quercetin-3-O-rutinoside, is a natural flavonoid present in buckwheat, rue, and Sophora japonica and other plants. Rutin has various biological activities such as antioxidant, hypoglycemic, and cardiovascular disease prevention, but its low solubility limits its practical application. The synthesis of rutin ester by lipophilic modification of rutin structure can effectively improve lipid solubility and increase bioavailability. This study presented a detailed review of the progress of enzyme-catalyzed synthesis of rutin ester in the non-aqueous phase, focusing on the effects of enzyme type, reaction media and acyl donor on the synthesis law of rutin ester. The difficulty of enzymatic synthesis of rutin ester was that rutin contained multiple hydroxyl groups and its insolubility with acyl donors and this study summarized the modification sites of rutin. The substrate solubility could be improved by through media compounding and physical assistance. High regioselectivity of rutin ester could be obtained by screening enzymes, enzyme modification, etc, further described the effect of acyl modification on the antioxidant activity of rutin, and summarized the existing strategies for the isolation and purification of rutin. Finally, proposed the future research directions of rutin esters, which are of guidance for their further research and exploitation in the future.