Aerial parts of Solanum agrarium Sendtn. (Solanaceae) present the flavonoid myricetin 3,7,3 trimethyl ether and antispasmodic effect on guinea-pig ileum by blockade of voltage-gated calcium channels
| Autor: | Ana Carolina de Carvalho Correia, Bagnólia Araújo da Silva, Ciberio L, im Macecirc, Gislaine Alves de Oliveira, Maria de Fátima Agra, Tania M. S. Silva, Rosimeire F. Santos, Celso A. Camara, Roberto Jefferson Bezerra do Nascimento, Fabio de S. Monteiro |
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| Rok vydání: | 2013 |
| Předmět: |
Pharmacology
chemistry.chemical_classification Carbachol Voltage-dependent calcium channel Stereochemistry Flavonoid Pharmaceutical Science Ileum Plant Science chemistry.chemical_compound medicine.anatomical_structure Complementary and alternative medicine chemistry Drug Discovery medicine Antispasmodic Myricetin Kaempferol Histamine medicine.drug |
| Zdroj: | Journal of Medicinal Plants Research. 7:2293-2299 |
| ISSN: | 1996-0875 |
| Popis: | Solanum agrarium Sendtn. is popularly known in Northeastern Brazil as "gogoia". Previous work has verified the presence of the flavonoid kaempferol and showed the crude ethanolic extract from aerial parts of S. agrarium (SA‑EtOH) to have non-selective antispasmodic effect on guinea‑pig ileum. The aim was to isolate and identify the special metabolites and to investigate antispasmodic mechanism of SA‑EtOH on guinea-pig ileum. From their aerial parts was isolated the flavonoid myricetin‑3,7,3’‑trimethyl ether. SA‑EtOH shifted to the right cumulative concentration-response curves to carbachol or histamine in a reversible and non-competitive manner. SA‑EtOH relaxed the ileum pre-contracted with 40 mM KCl (EC50=17.4±3.5 µg/ml), 10‑6 M carbachol (EC50=119.4±24.3 µg/ml) or 10‑6 M histamine (EC50=18.7±4.6 µg/ml). This is most likely due to the inhibition of calcium influx through voltage-gated calcium channels (CaV). It was confirmed by SA‑EtOH antagonizing CaCl2-induced contractions in depolarizing medium nominally without Ca2+, with non‑parallel shift of the concentration-response curves to the right and reduction of Emax. The uncovering of SA‑EtOH (EC50=187.2±27.3 µg/ml) inhibiting tonic contractions induced by S‑(‑)‑BayK8644 suggests that Ca2+ channel subtype involved is CaV-L. In conclusion, SA‑EtOH shows antispasmodic effect on guinea-pig ileum due, in part, to blockade of calcium influx through CaV channels. Key words: Solanum agrarium, flavonoid, antispasmodic effect, guinea-pig ileum, CaV-L. |
| Databáze: | OpenAIRE |
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