RESUMO
AIM OF STUDY: Securidaca longepedunculata is used in the treatment of erectile dysfunction in South Africa. The aim of the study was to isolate and identify the active constituents and to determine their activity in the relaxation of corpus cavernosal smooth muscle. MATERIALS AND METHODS: Bioassay guided isolation of the bioactive compounds using a smooth muscle relaxation bioassay and structural elucidation was carried out using different spectroscopic techniques including 2D NMR. RESULTS: Two new xanthones were isolated; one of them showed potent activity to relax the corpus cavernosal smooth muscle by 97 % in comparison to sildenafil (Viagra) at 1.8 x 10(-5) mg/ml. CONCLUSIONS: S. longepedunculata's xanthones stimulate the relaxation of corpus cavenosum smooth muscle, which supports the traditional use of its root bark.
Assuntos
Disfunção Erétil/tratamento farmacológico , Fitoterapia , Securidaca/química , Xantonas/farmacologia , Animais , Espectroscopia de Ressonância Magnética , Masculino , Medicinas Tradicionais Africanas , Relaxamento Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Pênis/efeitos dos fármacos , Casca de Planta/química , Coelhos , África do Sul , Espectrofotometria Ultravioleta , Xantonas/isolamento & purificaçãoRESUMO
Chloroform and ethanol extracts of root bark of Securidaca longepedunculata, Wrightia natalensis and Rhoicissus tridentata were investigated for their in vitro activity on the contraction of corpus cavernosal smooth muscle of white New Zealand rabbits. Some of the extracts of these plants relaxed the corpus cavernosal smooth muscle at low concentrations. The highest activity was obtained from Securidaca longepedunculata chloroform extracts at a concentration of 13.0 mg/ml, which induced 66.6% relaxation. Viagra was used as a positive control in this study. Extracts of Securidaca longepedunculata added to human spermatozoa affected certain sperm parameters negatively at 6.5 mg/ml and higher whilst there was no effect at 1.0 mg/ml.
Assuntos
Disfunção Erétil/terapia , Plantas Medicinais , Espermatozoides/fisiologia , Animais , Humanos , Técnicas In Vitro , Masculino , Relaxamento Muscular , Músculo Liso/fisiopatologia , CoelhosRESUMO
1,7-Dimethoxy-2-hydroxy-xanthone and 1,4-dihydroxy-7-methoxy-xanthone isolated from Securidaca longependunculata were tested for their activity on rabbit corpus cavernosum in vitro. Only the former relaxed the corpus cavernosum by 63% at 1.8 x 10(-5) mg/ml.