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Semisynthesis and Biological Evaluation of Oleanolic Acid 3-O-β-d-Glucuronopyranoside Derivatives for Protecting H9c2 Cardiomyoblasts against H2O2-Induced Injury

机译:齐墩果酸3-O-β-d-葡糖醛酸吡喃糖苷衍生物的半合成和生物学评价对H9c2成肌细胞免受H2O2诱导的伤害的保护作用

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摘要

A series of novel oleanolic acid 3-O-β-d-glucuronopyranoside derivatives have been designed and synthesized. Biological evaluation has indicated that some of the synthesized compounds exhibit moderate to good activity against H2O2-induced injury in rat myocardial cells (H9c2). Particularly, derivative 28-N-isobutyl ursolic amide 3-O-β-d-galactopyranoside (>8a) exhibited a greater protective effect than the positive control oleanolic acid 3-O-β-d-glucuronopyranoside, indicating that it possesses a great potential for further development as a cardiovascular disease modulator by structural modification.
机译:设计并合成了一系列新型齐墩果酸3-O-β-d-葡糖醛酸吡喃糖苷衍生物。生物学评估表明,某些合成的化合物对H2O2诱导的大鼠心肌细胞(H9c2)损伤具有中等至良好的活性。特别是,衍生物28-N-异丁基熊果糖酰胺3-O-β-d-吡喃半乳糖苷(> 8a )表现出比阳性对照齐墩果酸3-O-β-d-葡糖醛酸吡喃糖苷更大的保护作用,这表明它具有通过结构修饰作为心血管疾病调节剂进一步发展的巨大潜力。

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