齐墩果酸 3-O-β-d-吡喃葡萄糖醛酸苷衍生物的半合成及对 H₂O₂诱导的 H9c2 心肌细胞损伤的保护作用研究。
Semisynthesis and Biological Evaluation of Oleanolic Acid 3-O-β-d-Glucuronopyranoside Derivatives for Protecting H9c2 Cardiomyoblasts against H₂O₂-Induced Injury.
机构信息
Beijing Key Laboratory of Innovative Drug Discovery of Traditional Chinese Medicine (Natural Medicine) and Translational Medicine, Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Key Laboratory of Efficacy Evaluation of Chinese Medicine against Glycolipid Metabolic Disorders, State Administration of Traditional Chinese Medicine, Zhong Guan Cun Open Laboratory of the Research and Development of Natural Medicine and Health Products, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China.
Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China.
出版信息
Molecules. 2018 Jan 10;23(1):44. doi: 10.3390/molecules23010044.
A series of novel oleanolic acid 3---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--isobutyl ursolic amide 3---d-galactopyranoside () exhibited a greater protective effect than the positive control oleanolic acid 3---d-glucuronopyranoside, indicating that it possesses a great potential for further development as a cardiovascular disease modulator by structural modification.
一系列新型的齐墩果酸 3---d-葡萄糖醛酸苷衍生物被设计和合成。生物评价表明，一些合成的化合物对 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--异丁基熊果酸酰胺 3---d-半乳糖苷 () 表现出比阳性对照齐墩果酸 3---d-葡萄糖醛酸苷更大的保护作用，表明它具有作为心血管疾病调节剂通过结构修饰进一步开发的巨大潜力。
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