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目的:探索含23-羟基或24-羟基的天然五环三萜化合物的糖原磷酸化酶抑制活性。方法:以齐墩果酸为起始原料分别合成阿江揽仁酸、贝萼皂苷元、常春藤酮酸及4-异构常春藤酮酸,并对其进行抗糖原磷酸化酶的生物活性评估。结果:以多步反应半合成了阿江揽仁酸、贝萼皂苷元、常春藤酮酸及4-异构常春藤酮酸,其中阿江揽仁酸的合成共11步,总收率约10%,贝萼皂苷元的合成其14步,总收率约12%。生物活性研究结果表明,阿江揽仁酸、贝萼皂苷元、常春藤酮酸及4-异构常春藤酮酸具有中等强度的糖原磷酸化酶抑制活性,其IC50介于53～103μmol·L?1之间。结论:阿江揽仁酸、贝萼皂苷元、常春藤酮酸及4-异构常春藤酮酸是中等强度的糖原磷酸化酶抑制剂,齐墩果烷骨架中23-羟基或24羟基的引入对GP抑制活性有不利影响的趋势。
Objective: To explore glycogen phosphorylase inhibitory activity of natural pentacyclic triterpene compounds containing 23-hydroxy or 24-hydroxy. Methods: Oleanolic acid, calyciflorin, ivy acid and 4-isomeric ivyonic acid were synthesized from oleanolic acid, respectively, and their anti-glycogen phosphorylase activity Activity assessment. RESULTS: A multi-step reaction of Arenic acid, calyciflorin, ivy acid and 4-isomeric ivyonic acid was synthesized. The synthesis of Acrylamide was 11 steps, and the total yield was about 10%, calyx saponin synthesis of its 14 steps, the total yield of about 12%. The results of biological activity showed that adefovir dipivoxil, calycium saponin, ivy acid and 4-isomeric ivyonic acid have moderate glycogen phosphorylase inhibitory activity with IC50 ranging from 53 to 103 μmol · L? 1 between. CONCLUSIONS: Arenic acid, calycone, ivyonic acid and 4-isomeric ivyonic acid are moderate-intensity glycogen phosphorylase inhibitors with 23-hydroxy or 24-hydroxy groups in the oleanane backbone The introduction of GP inhibitory activity adversely affect the trend.