alpha-Glucosidase Inhibitors from Salvia circinata
Por:
Flores-Bocanegra L., González-Andrade M., Bye R., Linares E., Mata R.
Publicada:
1 may 2017
Resumen:
A dried infusion prepared from the aerial parts of Salvia circinata did
not provoke acute toxicity in mice (LD50 > 5 g/kg). This infusion showed
poor hypoglycemic and antihyperglycemic effects (100-570 mg/kg) when
tested in normal and hyperglycemic mice using acute and oral glucose
tolerance tests, respectively. However, this infusion possessed
antihyperglycemic action in vivo during an oral sucrose tolerance test
(31.6-316 mg/kg), suggesting the presence of a-glucosidase inhibitors in
S. circinata. Fractionation of a nonpolar extract of the aerial parts of
the plant yielded a new biflavone (1) and four new neoderodane
diterpenoid glucosides (2-5) along with the known compounds amarisolide
(6), pedalitin (7), apigenin-7-O-beta-D-glucoside (8), and the flavone
2-(3,4-dimethoxypheny1)-5,6-dihydroxy7-methoxy-4H-chromen-4-one (9).
Compounds 1 and 6-9 were active against mammalian alpha-glucosidases; 6
and 7 were also active against a recombinant alpha-glucosidase from
Ruminococcus obeum and reduced significantly the postprandial peak
during an oral sucrose tolerance test in healthy mice, consistent with
their alpha-glucosidase inhibitory activity. Molecular docking and
dynamic studies revealed that compounds 6 and 7 might bind to
alpha-glucosidases at the catalytic center of the enzyme.
Filiaciones:
Flores-Bocanegra L.:
Univ Nacl Autonoma Mexico, Fac Quim, Cuidad De Mexico 04510, DF, Mexico
Facultad de Química, Universidad Nacional Autónoma de México, Cuidad de México, 04510, Mexico
González-Andrade M.:
Univ Nacl Autonoma Mexico, Fac Med, Cuidad De Mexico 04510, DF, Mexico
Facultad de Medicina, Universidad Nacional Autónoma de México, Cuidad de México, 04510, Mexico
Bye R.:
Univ Nacl Autonoma Mexico, Inst Biol, Cuidad De Mexico 04510, DF, Mexico
Instituto de Biología, Universidad Nacional Autónoma de México, Cuidad de México, 04510, Mexico
Linares E.:
Univ Nacl Autonoma Mexico, Inst Biol, Cuidad De Mexico 04510, DF, Mexico
Instituto de Biología, Universidad Nacional Autónoma de México, Cuidad de México, 04510, Mexico
Mata R.:
Univ Nacl Autonoma Mexico, Fac Quim, Cuidad De Mexico 04510, DF, Mexico
Facultad de Química, Universidad Nacional Autónoma de México, Cuidad de México, 04510, Mexico
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