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Further Studies on Structure-Cardiac Activity Relationships of Diterpenoid Alkaloids
- Source :
- Natural product communications. 10(12)
- Publication Year :
- 2016
-
Abstract
- The cardiac effect of thirty-eight diterpenoid alkaloids was evaluated on the isolated bullfrog heart model. Among them, twelve compounds exhibited appreciable cardiac activity, with compounds 3 and 35 being more active than the reference drug lanatoside. The structure-cardiac activity relationships of the diterpenoid alkaloids were summarized based on our present and previous studies [2]: i) 1α-OMe or 1α-OH, 8-OH, 14-OH, and NH (or NMe) are key structural features important for the cardiac effect of the aconitine-type C19-diterpenoid alkaloids without any esters. C18-diterpenoid alkaloids, lycoctonine-type C19-diterpenoid alkaloids, and the veatchine- and denudatine-type C20-diterpenoid alkaloids did not show any cardiac activity; ii) the presence of 3α-OH is beneficial to the cardiac activity; iii) the effect on the cardiac action of 6α-OMe, 13-OH, 15α-OH, and 16-demethoxy or a double bond between C-15 and C-16 depends on the substituent pattern on the nitrogen atom.
- Subjects :
- Pharmacology
chemistry.chemical_classification
Rana catesbeiana
Double bond
Molecular Structure
Chemistry
Stereochemistry
Substituent
Cardiac activity
Cardiovascular Agents
Heart
Plant Science
General Medicine
Reference drug
Terpenoid
chemistry.chemical_compound
Structure-Activity Relationship
Alkaloids
Complementary and alternative medicine
Bullfrog
Drug Discovery
Cardiovascular agent
Structure–activity relationship
Animals
Diterpenes
Subjects
Details
- ISSN :
- 1934578X
- Volume :
- 10
- Issue :
- 12
- Database :
- OpenAIRE
- Journal :
- Natural product communications
- Accession number :
- edsair.doi.dedup.....f50a97da42fa68bcebcaec5d23f3e6ff