Calcium Influx Inhibition is Involved in the Hypotensive and Vasorelaxant Effects Induced by Yangambin
| Autor: | José Maria Barbosa-Filho, Islania Giselia Albuquerque Araújo, Karla Veruska Marques Cavalcante, Nadja de Azevedo Correia, Isac Almeida de Medeiros, Mário dos Anjos Neto, Katy Lísias Gondim Dias, Maria C. Alustau, Robson Cavalcante Veras, Darizy Flávia Silva, Lusiane Maria Bendhack |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2014 |
| Předmět: |
Chronotropic
Inotrope Tachycardia Male Vasodilator Agents Pharmaceutical Science Vasodilation Blood Pressure VASODILATAÇÃO Muscle Smooth Vascular Analytical Chemistry Potassium Chloride Phenylephrine Drug Discovery vasodilation Chemistry medicine.anatomical_structure Chemistry (miscellaneous) Molecular Medicine lignan yangambin mesenteric artery calcium influx medicine.symptom Hypotension Artery medicine.drug medicine.medical_specialty Endothelium In Vitro Techniques Article Lignans lcsh:QD241-441 lcsh:Organic chemistry Nifedipine Mesenteric Artery Superior Internal medicine medicine Animals Heart Atria Physical and Theoretical Chemistry Rats Wistar Furans Dose-Response Relationship Drug Organic Chemistry Endocrinology Calcium Endothelium Vascular |
| Zdroj: | Molecules; Volume 19; Issue 5; Pages: 6863-6876 Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual) Universidade de São Paulo (USP) instacron:USP Molecules Molecules, Vol 19, Iss 5, Pp 6863-6876 (2014) |
| ISSN: | 1420-3049 |
| DOI: | 10.3390/molecules19056863 |
| Popis: | The pharmacological effects on the cardiovascular system of yangambin, a lignan isolated from Ocotea duckei Vattimo (Lauraceae), were studied in rats using combined functional and biochemical approaches. In non-anaesthetized rats, yangambin (1, 5, 10, 20, 30 mg/kg, i.v.) induced hypotension (−3.5 ± 0.2; −7.1 ± 0.8; −8.9 ± 1.3; −14 ± 2.3, −25.5% ± 2.6%, respectively) accompanied by tachycardia (5.9 ± 0.5; 5.9 ± 1.6; 8.8 ± 1.4; 11.6, 18.8% ± 3.4%, respectively). In isolated rat atria, yangambin (0.1 µM–1 mM) had very slight negative inotropic (Emax = 35.6% ± 6.4%) and chronotropic effects (Emax = 10.2% ± 2.9%). In endothelium-intact rat mesenteric artery, yangambin (0.1 µM–1 mM) induced concentration-dependent relaxation (pD2 = 4.5 ± 0.06) of contractions induced by phenylephrine and this effect was not affected by removal of the endothelium. Interestingly, like nifedipine, the relaxant effect induced by yangambin was more potent on the contractile response induced by KCl 80 mM (pD2 = 4.8 ± 0.05) when compared to that induced by phenylephrine. Furthermore, yangambin inhibited CaCl2-induced contractions in a concentration-dependent manner. This lignan also induced relaxation (pD2 = 4.0 ± 0.04) of isolated arteries pre-contracted with S(−)-Bay K 8644. In fura-2/AM-loaded myocytes of rat mesenteric arteries, yangambin inhibited the Ca2+ signal evoked by KCl 60 mM. In conclusion, these results suggest that the hypotensive effect of yangambin is probably due to a peripheral vasodilatation that involves, at least, the inhibition the Ca2+ influx through voltage-gated Ca2+ channels. |
| Databáze: | OpenAIRE |
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