Vasorelaxant effect of new neo-clerodane diterpenoids isolated from Croton schiedeanus

The vasorelaxant effect of two new neo-clerodane diterpenoids, (12 R)-12-hydroxycascarillone and 5β-hydroxy- cis-dehydrocrotonin, in addition to the known cis-dehydrocrotonin and trans-dehydrocrotonin, all them previously isolated by us from Croton schiedeanus Schlecht, was studied in isolated aorta...

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Bibliographic Details
Published in:Journal of ethnopharmacology 2004-09, Vol.94 (1), p.185-189
Main Authors: Guerrero, M.F, Puebla, P, Carrón, R, Martı́n, M.L, San Román, L
Format: Article
Language:English
Subjects:
(12 R)-12-Hydroxycascarillone
5β-Hydroxy- cis-dehydrocrotonin
Animals
Aorta, Thoracic
bioactive properties
Biological and medical sciences
cis-Dehydrocrotonin
Croton
Croton schiedeanus
Diterpenes, Clerodane - isolation & purification
Diterpenes, Clerodane - pharmacology
diterpenoids
General pharmacology
In Vitro Techniques
Male
Medical sciences
neo-Clerodane diterpenoids
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
phytochemicals
Rats
Rats, Wistar
trans-Dehydrocrotonin
Vasodilator Agents - isolation & purification
Vasodilator Agents - pharmacology
vasorelaxant activity
Vasorelaxant effect
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Summary:The vasorelaxant effect of two new neo-clerodane diterpenoids, (12 R)-12-hydroxycascarillone and 5β-hydroxy- cis-dehydrocrotonin, in addition to the known cis-dehydrocrotonin and trans-dehydrocrotonin, all them previously isolated by us from Croton schiedeanus Schlecht, was studied in isolated aorta rings contracted by high K + (80 mM) or phenylephrine (1 μM). According to their IC 50 values to KCl induced contraction, the potency order was (12 R)-12-hydroxycascarillone > cis-dehydrocrotonin > 5β-hydroxy- cis-dehydrocrotonin > trans-dehydrocrotonin (0.3, 1.5, 96 and >100 mM, respectively). The possible cooperativity between diterpenoid compounds and the predominant flavonoid (ayanin) was studied. The vasorelaxant activity of cis-dehydrocrotonin and ayanin was increased when both compounds were incorporated simultaneously to the aortic rings precontracted with phenylephrine. These results suggest that Croton schiedeanus induces its effects via the synergistic actions of several vasodilator substances, among which neo-clerodane diterpenoids play an important role.
ISSN:0378-8741
1872-7573
DOI:10.1016/j.jep.2004.05.018