Calcium Influx Inhibition is Involved in the Hypotensive and Vasorelaxant Effects Induced by Yangambin

Molecules

Mario dos Anjos Neto¹  Lusiane Maria Bendhack¹  Katy Lísias Gondim Dias²  Karla Veruska Marques Cavalcante²  Nadja de Azevedo Correia²  Isac Almeida de Medeiros³  Maria do Carmo de Alustau³  José Maria Barbosa-Filho³  Islania Giselia Albuquerque Araújo³  Robson Cavalcante Veras³  Darizy Flávia Silva⁴ 

[1] Departamento de Farmacologia, Escola de Medicina de Ribeirão Preto, Universidade de São Paulo, postal code Ribeirão Preto, SP, Brazil;Departamento de Fisiologia e Patologia, Centro de Ciências da Saúde, Universidade Federal da Paraíba, Cidade Universitária, 58051-900 João Pessoa, PB, Brazil;Laboratório de Farmacologia Cardiovascular, Centro de Biotecnologia, Universidade Federal da Paraíba, Cidade Universitária, 58051-900 João Pessoa, PB, Brazil;Laboratório de Neurociências, Instituto de Ciências da Saúde, Universidade Federal da Bahia, Avenida Reitor Miguel Calmon, Vale do Canela, 40110-902 Salvador, BA, Brazil;

关键词: lignan;    yangambin;    mesenteric artery;    vasodilation;    calcium influx;   

DOI  :  10.3390/molecules19056863

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown