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Structure-cardiac activity relationship of C19-diterpenoid alkaloids
Xi-Xian Jian1, Pei Tang, Xiu-Xiu Liu
1Department of Chemistry of Medicinal Natural Products, West China College of Pharmacy, Sichuan University, Chengdu, Sichuan, PR China 610041.
Natural Product Communications
|July 24, 2012
Summary
Eleven C19-diterpenoid alkaloids showed significant cardiac activity in bullfrog heart assays. Specific structural features, like hydroxyl groups and amine types, are crucial for this activity in aconitine-type alkaloids.
Area of Science:
- Pharmacology
- Natural Products Chemistry
Background:
- C19-diterpenoid alkaloids from Aconitum and Delphinium species are known for diverse biological activities.
- Cardiac activity of these alkaloids is of significant interest for potential therapeutic applications.
Purpose of the Study:
- To evaluate the cardiac activity of thirty-three C19-diterpenoid alkaloids.
- To identify key structural features responsible for the observed cardiac effects.
Main Methods:
- Cardiac activity was assessed using an isolated bullfrog heart assay.
- Structure-activity relationships were analyzed for active compounds.
Main Results:
- Eleven out of thirty-three tested alkaloids exhibited cardiac activity, with amplitude increases ranging from 16-118%.
- Mesaconine, hypaconine, and beiwutinine demonstrated potent cardiac effects.
- Specific structural elements, including hydroxyl groups at C-15 and C-8, and functional groups at C-1 and ring A, were identified as critical for activity.
Conclusions:
- The study identified novel C19-diterpenoid alkaloids with significant cardiac activity.
- Key structure-activity relationships were elucidated, providing insights into the pharmacophore of these compounds.
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