Abstract
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.
| Original language | English |
|---|---|
| Pages (from-to) | 50-55 |
| Number of pages | 6 |
| Journal | Fitoterapia |
| Volume | 100 |
| DOIs | |
| State | Published - Jan 2015 |
Bibliographical note
Publisher Copyright:© 2014 Elsevier B.V. All rights reserved.
Funding
The project was funded by the National Natural Science Foundation of China (No. 81273377 ), Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources (Guangxi Normal University), Ministry of Education of China (No. CMEMR2013-B05 ) and the Project Program of State Key Laboratory of Natural Medicines, China Pharmaceutical University (No. SKLNMZZCX201404 ).
| Funders | Funder number |
|---|---|
| National Natural Science Foundation of China (NSFC) | 81273377 |
| Ministry of Education of the People's Republic of China | CMEMR2013-B05 |
| Guangxi Normal University | |
| State Key Laboratory of Natural Medicines, China Pharmaceutical University | SKLNMZZCX201404 |
| State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources |
Keywords
- 23-Hydroxybetulinic acid
- Ambradiolic acid
- First synthesis
- Glycogen phosphorylase (GP)
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery
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