RESUMEN
Two isocoumarin derivatives, stoloniferol A (1) and B (2), a known 5alpha, 8alpha-epidioxy-23-methyl-(22E, 24R)-ergosta-6, 22-dien-3beta-ol (3), and a known dihydrocitrinone (4) were isolated from the ethyl acetate extract of the sea squirt-derived fungus, Penicillium stoloniferum QY2-10, and a halophilic fungus, Penicillium notatum B-52, respectively. Their structures were elucidated by spectroscopic methods and optical rotation. The stereochemistry of 2 was determined on the basis of different NOE experiments and chemical transformation. Compound 3 showed cytotoxicity against P388 cells, with an IC50 value of 4.07 microM.
Asunto(s)
Antineoplásicos/aislamiento & purificación , Isocumarinas/aislamiento & purificación , Penicillium chrysogenum/química , Urocordados/microbiología , Animales , Antineoplásicos/química , Antineoplásicos/farmacología , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Humanos , Concentración 50 Inhibidora , Isocumarinas/química , Isocumarinas/farmacología , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Penicillium/química , Penicillium/aislamiento & purificación , Penicillium chrysogenum/aislamiento & purificación , Agua de MarRESUMEN
AIM: To establish a method for determinate of the inhibitory activity of angiotensin-converting enzyme inhibitor captopril by high performance capillary electrophoresis. METHODS: The characteristic absorptive wavelength of hippuric acid determined by ultraviolet spectrophotometer is 228 nm. The method employed a melted capillary column, 50 mmol.L-1 phosphoric acid (pH 8.3) buffer solution, inject pressure 4.8 kPa, inject time 3 s, separation voltage 20 kV and detection wavelength 228 nm. RESULTS: The reactant and resultant was separated completed within 7 min. IC50 of captopril was 0.019 mumol.L-1. Captopril is a competitive inhibitor, which was proved by enzyme reaction dynamics. CONCLUSION: The method was shown to be accurate, simple and rapid and can be used for determination of the inhibitory activity of captopril.
Asunto(s)
Inhibidores de la Enzima Convertidora de Angiotensina/farmacología , Captopril/farmacología , Hipuratos/análisis , Peptidil-Dipeptidasa A/metabolismo , Electroforesis Capilar/métodosRESUMEN
Three new quinazoline alkaloids, aurantiomides A (1), B (2), and C (3), along with the known metabolite anacine (4) were isolated from the sponge-derived fungus strain Penicillium aurantiogriseum SP0-19 by bioassay-guided fractionation. Their structures were elucidated by spectroscopic and chemical methods. Their absolute configurations were deduced by comparison of their Cotton effects with anacine (4) and by chemical transformations. Compounds 2 and 3 showed moderate cytotoxicities against HL-60, P388 and BEL-7402, P388 cell lines, respectively.