Vasodilator activity of Michelia figo Spreng. (Magnoliaceae) by in vitro functional study.
The methanolic extract of leaves of Michelia figo Spreng. (Magnoliaceae), as well as several purified fractions, showed a concentration-dependent vasorelaxing effect on aortic rings endothelium-deprived and pre-contracted by norepinephrine (NE). For further pharmacological investigation on the mechanism of action, the fraction S4 was selected, since it showed the best vasodilator properties. The pharmacological effect was not produced through the stimulation of cyclooxygenase, adenyl cyclase, or guanylyl cyclase, since selective inhibitors did not prevent the fraction S4-induced effects. Moreover, the vasorelaxing effect of the fraction was resistant to the block of nifedipine-sensitive Ca(2+) channels. The fraction S4 (10(-4) g/ml) produced a shift towards the right of the concentration-contractile response curve to NE, in normal conditions, and the shift was more evident in Ca(2+)-free Tyrode solution, suggesting an action on intracellular Ca(2+)-channels. The vasodilator action of fraction S4 on NE pre-contracted rings was not prevented by cyclopiazonic acid (blocker of Ca(2+)/ATPase), which excludes a role for mechanisms involving the storage of Ca(2+) in the sarcoplasmic reticulum. The reduction of the contraction elicited by caffeine, an opener of ryanodine-sensitive receptors, suggests that the fraction S4 of Michelia figo leaves could produce the vasorelaxing response by the blockade of ryanodine-sensitive Ca(2+) channels of the sarcoplasmic reticulum.
Chericoni
Silvio
S
Dipartimento di Chimica Bioorganica e Biofarmacia, Università di Pisa, via Bonanno, 33, 56126 Pisa, Italy.
Testai
Lara
L
Campeol
Elisabetta
E
Calderone
Vincenzo
V
Morelli
Ivano
I
Martinotti
Enrica
E
D000818:Animals; D001011:Aorta / Q000187:drug effects* / Q000502:physiology; D004305:Dose-Response Relationship, Drug; D004730:Endothelium, Vascular / Q000187:drug effects / Q000502:physiology; D029562:Magnoliaceae; D008297:Male; D009638:Norepinephrine; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D018515:Plant Leaves; D051381:Rats; D017208:Rats, Wistar; D014661:Vasoconstriction / Q000187:drug effects*; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use
D010936:Plant Extracts; D014665:Vasodilator Agents; D009638:Norepinephrine