Portal de Periódicos da CAPES

Inhibition of Na+, K+-ATPase by 1,2,3,4,6-Penta-O-galloyl-β-D-glucose, a major constituent of both moutan cortex and paeoniae radix

1997; Elsevier BV; Volume: 53; Issue: 4 Linguagem: Inglês

10.1016/s0006-2952(96)00828-3

1873-2968

Kanaka Satoh, Fumiko Nagai, Keiko Ushiyama, Ichiro Yasuda, Takako Seto, Itsu Kano,

Metabolomics and Mass Spectrometry Studies

The inhibition of Na∗,K+-ATPase activity by various constituents of Moutan Cortex and Paeoniae Radix was studied. 1,2,3,4,6-Penta-O-galloyl-β-D-glucose (PGG), a major component of both crude drugs, strongly inhibited Na+,K+-ATPase activity (lC50 = 2.5 x 10-6 M), whereas galloylpaeoniflorin, benzoic acid, and catechin were weakly inhibitory, and albiflorin, oxypaeoniflorin, paeoniflorin, paeonol, and phenol were ineffective. The inhibition of Na+,K+-ATPase activity by PGG was decreased in the presence of BSA or phospholipids. The inhibition mode of PGG was noncompetitive with respect to ATP. The K0.5 value for Na+ was increased by the addition of PGG from 9.1 to 12.3 mM, whereas that for K+ was not altered. PGG also inhibited K+-dependent p-nitrophenyl phosphatase activity with an IC50 value of 5.3 x 10-6 M, and the extent of the inhibition increased at higher concentrations of K+. The K0.5 value for K+ was decreased by the addition of PGG from 3.3 to 2.0 mM. These results suggested that the inhibition of Na+,K+-ATPase activity is caused by interaction of PGG with the enzyme in the E2 state. The inhibitory effect of Moutan Cortex or Paeoniae Radix is considered to be mainly attributable to PGG.