齐墩果酸衍生物的合成与表征

Synthesis and Characterization of Oleanolic Acid Derivatives

齐墩果酸属五环三萜类化合物,在自然界中分布广泛,具有多种药理学活性,而且其毒性较低。目前研究发现,齐墩果酸除了具有消炎、降糖、增强免疫、抗氧化、抑制血小板聚集和利尿作用等多方面的临床药理作用,还具有护肝、抗动脉粥样硬化、抗高血脂及抗肿瘤等生物活性,药用开发前景广阔。因此,本文以齐墩果酸为先导化合物,在C-3位通过特定的连接片段丁二酸与氨基酸及其它的活性片段进行偶联,合成了2种新的中间体和7种新的目标产物,并利用IR和1HNMR波谱技术对其结构进行了表征。

Oleanolic acid belongs to pentacyclic triterpenoid of nature compounds. It widely distributes in nature and shows a variety of pharmacology activities and lower toxicity. The present study found that the oleanolic acid has some clinical pharmacological effects, such as diminish inflammation, hypoglycemic effect, enhance immune function, antioxidation, inhibit platelet aggregation and diuresis function. It also has hepatoprotective effect, anti-atherogenic effect, anti-hyperlipidemia action and antitumor bioactivity, and with good pharmaceutical development prospect. Therefore, Oleanolic acid was used as the lead compound via special fragment butanedioic acid on C-3 coupled with amino acids and some active fragments, and two of intermediates and seven final products were synthesized and characterized by IR and 1H NMR spectroscopy techniques.