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Synthesis and biological evaluation of ambradiolic acid as an inhibitor of glycogen phosphorylase. | LitMetric

Synthesis and biological evaluation of ambradiolic acid as an inhibitor of glycogen phosphorylase.

Fitoterapia

State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China; Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China. Electronic address:

Published: January 2015

Ambradiolic acid (3) with oleanane skeleton is a natural pentacyclictriterpene. The first synthesis of 3 starting from 23-hydroxybetulinic acid (2) has been accomplished in 12-steps with a total yield of 18.1% in our study. Compound 3 was further biologically evaluated and found to exhibit significant inhibitory activity against rabbit muscle glycogen phosphorylase (GP) with an IC50 value of 12.4 μM, suggesting it could be a potential lead compound for the development of hypoglycemic drugs.

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http://dx.doi.org/10.1016/j.fitote.2014.11.014DOI Listing

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