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1.
Drug Dev Res ; 79(7): 332-338, 2018 11.
Artículo en Inglés | MEDLINE | ID: mdl-30244493

RESUMEN

Soulattrolide is a natural coumarin synthesized by the leaves of species of Calophyllum (Calophyllaceae) rain forest trees, including the American C. brasiliense, and the Asian C. teysmanii. Soulattrolide is a potent inhibitor of the reverse transcriptase from HIV-1 (RT-HIV-1), and active against Mycobacterium tuberculosis. However, the effects of this coumarins on other systems, remains to be evaluated. C. brasiliense is used in traditional medicine for the treatment of pain and inflammation. Therefore, we decided to explore the antinociceptive, anti-inflammatory activity of soulattrolide in mice, as well as, some of its possible effects on the CNS. Soulattrolide showed antinociceptive effects in the writhing test (ED50 = 33.8 mg/kg), as well as, in the formalin test with an ED50 = 7.9, and 22.1 mg/kg for Phases 1 and 2, respectively. The highest dose of soulattrolide (50 mg/kg) induced 40% of antinociception in the hot plate test. Regarding to anti-inflammatory activity, in the 12-O-Tetradecanoylphorbol-13-acetate (TPA) test, soulattrolide showed an IC50 = 1.81 µmol/ear, whereas in the myeloperoxidase assay, it showed an inhibition of 87% (1 µmol/ear). Soulattrolide showed sedative effects on the pentobarbital-induced sleeping time test, and the rotarod test, but lacked antidepressant activity on the tail suspension test. In conclusion, we report for the first time, the antinociceptive effects of soulattrolide in mice, like those of naproxen; soulattrolide also showed mild anti-inflammatory activity, as well as mild sedative and anxiolytic properties, therefore, it has also activity on the CNS.


Asunto(s)
Analgésicos/farmacología , Ansiolíticos/farmacología , Antiinflamatorios/farmacología , Fármacos del Sistema Nervioso Central/farmacología , Cumarinas/farmacología , Dimensión del Dolor/efectos de los fármacos , Analgésicos/química , Animales , Ansiolíticos/química , Antiinflamatorios/química , Fármacos del Sistema Nervioso Central/química , Cumarinas/química , Relación Dosis-Respuesta a Droga , Hipnóticos y Sedantes/química , Hipnóticos y Sedantes/farmacología , Masculino , Ratones , Ratones Endogámicos BALB C , Dimensión del Dolor/métodos
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