Inhibition of cholinesterase activity by extracts, fractions and compounds from Calceolaria talcana and C. integrifolia (Calceolariaceae: Scrophulariaceae)
Por:
Cespedes C.L., Muñoz E., Salazar J.R., Yamaguchi L., Werner E., Alarcon J., Kubo I.
Publicada:
1 ene 2013
Resumen:
Extracts, fractions and compounds from Calceolaria talcana and C. integrifolia exhibited strong inhibitory effects of the activity of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes using the in vitro Ellman's method. The most active samples were from the ethyl acetate extract, which caused a mixed-type inhibition against AChE (69.8% and 79.5% at 100 and 200. µg/ml, respectively) and against BChE (98.5% and 99.8% at 100 and 200. µg/ml, respectively) and its major components verbascoside 8 (50.9% and 70.0% at 200. µg/ml, against AChE and BChE, respectively), martynoside 9, and fraction F- 7 (which corresponds to a mixture of 8, 9, and other phenylethanoids and phenolics that remain unidentified) (80.2% and 85.3% at 100 and 200. µg/ml, against AChE, respectively and 99.1% and 99.7% at 100 and 200. µg/ml, against BChE, respectively) inhibited the acetylcholinesterase enzyme competitively. The most polar fraction F- 5 from n-hexane extract (a mixture of naphthoquinones: 2-hydroxy-3-(1,1-dimethylallyl-1,4-naphthoquinone) 6, a-dunnione 7 and other polar compounds that remain unidentified) showed a mixed-type inhibition (71.5% and 72.1% against AChE and BChE at 200. µg/ml, respectively). Finally, the methanol-soluble residue presented a complex, mixed-type inhibition (39.9% and 67.9% against AChE and BChE at 200. µg/ml, respectively). The mixture F- 3 with diterpenes was obtained from the n-hexane extract: (1,10-cyclopropyl-9-epi-ent-isopimarol) 1, 19-a-hydroxy-abietatriene 2, and F- 4 a mixture of triterpenes a-lupeol 3, ß-sitosterol 4, ursolic acid 5 together with a complex mixture of terpenes that did not show activity. In summary, extracts and natural compounds from C. talcana and C. integrifolia were isolated, identified and characterized as cholinesterase inhibitors. © 2013 Elsevier Ltd.
Filiaciones:
Cespedes C.L.:
Biochemistry and Phytochemical-Ecology Laboratory, Department of Basic Sciences, Faculty of Sciences, University of Bío-Bío, Andres Bello Av. s/n, Chillán, Chile
Muñoz E.:
Biochemistry and Phytochemical-Ecology Laboratory, Department of Basic Sciences, Faculty of Sciences, University of Bío-Bío, Andres Bello Av. s/n, Chillán, Chile
Salazar J.R.:
Facultad de Ciencias Químicas, Universidad la Salle, Mexico, DF, Mexico
Yamaguchi L.:
Instituto de Química, Universidad de São Paulo, São Paulo, Brazil
Werner E.:
Biochemistry and Phytochemical-Ecology Laboratory, Department of Basic Sciences, Faculty of Sciences, University of Bío-Bío, Andres Bello Av. s/n, Chillán, Chile
Alarcon J.:
Synthesis and Biotransformation Laboratory, Department of Basic Sciences, Faculty of Sciences, University of Bío-Bío, Andres Bello Av. s/n, Chillán, Chile
Kubo I.:
ESPM Department, University of California at Berkeley, CA, United States
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