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β‐glucuronidase inhibition and diuretic activity of Fabiana imbricata R. & P. (Solanaceae)
Author(s) -
SchmedaHirschmann G.,
Loyola J. I.,
Reyes S.,
Hubert E.,
Rodriguez M.,
Rodriguez J.,
DutraBehrens M.
Publication year - 1994
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.2650080810
Subject(s) - scopoletin , diuretic , toxicity , pharmacology , acute toxicity , pharmacognosy , oral administration , hydrochlorothiazide , chemistry , solanaceae , urine , in vitro , traditional medicine , biology , biological activity , biochemistry , medicine , endocrinology , alternative medicine , organic chemistry , pathology , gene , blood pressure
The hydroalcoholic extract of Fabiana imbricata inhibited the enzyme β‐glucuronidase (β‐gluc) in vitro. Bioassay‐guided isolation led to scopoletin as the main active constituent of F. imbricata. Scopoletin was a noncompetitive inhibitor of β‐D‐glucuronidase with a K i value of 4 × 10 −5 M. A single oral dose of 250 mg/kg body weight F. imbricata extract produced a significant increase ( p <0.05) in the urine output of rats. The diuretic effect of the extract was weak in comparison with hydrochlorothiazide at 25 mg/kg. In the acute oral toxicity study in rats, ‘Pichi’ was shown to be a low toxicity crude drug at doses up to 5 g crude extract/kg body weight. At concentrations up to 0.50 mg/mL, the crude extract did not increase the number of chromosome aberrations in the in vitro human lymphocyte assay.