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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Evaluation of antioxidant and antimicrobial activities of Bergenin and its derivatives obtained by chemoenzymatic synthesis.
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Evaluation of antioxidant and antimicrobial activities of Bergenin and its derivatives obtained by chemoenzymatic synthesis.

机译:化学合成法获得的卑尔根及其衍生物的抗氧化和抗菌活性的评估。

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摘要

Bergenin pentacetate (2), a peracetate derivative of biologically active lead compound Bergenin (1) isolated from Bergenia stracheyi was subjected to lipase catalyzed regioselective alcoholysis to obtain 3,4,10,11-tetracetate of Bergenin (3). The free hydroxyl group of 3 was derivatised using higher carboxylic acids to obtain acyl derivatives (4-7). These compounds synthesized via chemoenzymatic route were characterized using 1H NMR, 13C NMR and mass spectral data and evaluated for DPPH radical scavenging, antimicrobial and xanthine oxidase inhibitory activities. The studies revealed that biological activity of Bergenin can be optimized by selective modification of its structure.
机译:分离自佛手柑中的生物活性铅化合物佛手柑(1)的过乙酸酯衍生物佛手柑五乙酸酯(2)进行脂酶催化的区域选择性醇解反应,得到3,4,10,11-四氢萘醌(3)。使用高级羧酸将3的游离羟基衍生化,以获得酰基衍生物(4-7)。使用1H NMR,13C NMR和质谱数据对通过化学酶促途径合成的这些化合物进行表征,并评估其对DPPH自由基的清除,抗菌和黄嘌呤氧化酶的抑制活性。研究表明,可以通过选择性修饰其结构来优化卑尔根素的生物活性。

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