Further Studies on Structure-Cardiac Activity Relationships of Diterpenoid Alkaloids
| Autor: | Feng-Peng Wang, Qiao-Hong Chen, Jia-Yu Ding, Dong-Lin Chen, Hong-Ying Deng, Xi-Xian Jian, Ruo-Bing Chao, Zhong-Tang Zhang |
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| Rok vydání: | 2016 |
| Předmět: |
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 |
| Zdroj: | Natural product communications. 10(12) |
| ISSN: | 1934-578X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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