Estudios científicos
Synthesis and biological evaluation of quercetin and resveratrol peptidyl derivatives as potential anticancer and antioxidant agents
Abstract:
Quercetin and resveratrol are polyphenolic compounds, members of the flavonoid and the stilbene family, respectively, both medicinally important as dietary anticancer and antioxidant agents. They are present in a variety of foods-including fruits, vegetables, tea, wine, as well as other dietary supplements-and are responsible for various health benefits. Different quercetin and resveratrol esters of Leu/Met-enkephalin and tetrapeptide Leu-Ser-Lys-Leu (LSKL) were synthesized as model systems for monitoring the influence of the peptides on biological activity of resveratrol and quercetin. General formula of the main peptidyl-quercetin derivatives is 2-[3-(aa)n-4-hydroxyphenyl]-3,5,7-tri-hydroxy-4H-1-benzopyran-4-on, and the general formula of the main peptidyl-resveratrol derivatives is (E)-5-[4-(aa)n)styryl]benzene-1,3-diol. The antioxidant and anticancer activities of prepared compounds were investigated. Significant anticancer activity was obtained for the LSKL-based both quercetin and resveratrol derivatives. All prepared compounds exhibit antioxidant activity, in particular quercetin derivative containing Met-enkephalin.
Comentarios divulgativos:
La quercetina y el resveratrol son compuestos minoritarios del vino que se han relacionad con propiedades anticancerígenas y antioxidantes. En este estudio los autores fabrican variantes de estos compuestos para conocer qué efecto tienen las diferentes modificaciones.
Observan que los compuestos diseñados mantienen la actividad antioxidante y que la capacidad anticancerígena varía según las modificaciones. También indican que a través de estas modificaciones se mejora su solubilidad y su biodisponibilidad, es decir la cantidad y velocidad con la que son absorbidos.
