| In vitro: |
| Drug Metab Dispos,2015,43:1590–1600. | | Intestinal Absorption and Metabolism of Epimedium Flavonoids in osteoporosis rats. [Reference: WebLink] | Herba Epimdii is a traditional Chinese medicine used to treat
osteoporosis. Its main pharmacological ingredients are flavonoids.
In previous studies conducted in healthy animals, we showed that
epimedium flavonoids could be hydrolyzed into secondary glycosides or aglycon by intestinal flora or enzymes, thereby enhancing
their absorption and antiosteoporosis activity.
To study the medicine in the pathologic state, epimedium flavonoids were
incubated with intestinal mucosa and feces in vitro and intestinal
perfusion in situ to explore the differences in absorption and
metabolism between sham and osteoporosis rats.
METHODS AND RESULTS:
For osteoporosis
rats, the hydrolysis rates of icariin, epimedin A(Epimedin A1), epimedin B, and
epimedin C incubated with intestinal flora for 1 hour were reduced
by 0.19, 0.26, 0.19, and 0.14, respectively, compared with that in sham
rats. Hydrolysis rates were reduced by 0.21, 0.24, 0.08, and 0.31
for icariin, epimedin A, epimedin B, and epimedin C incubated
with duodenal enzymes for 1 hour and by 0.13, 0.09, 0.07, and 0.47
for icariin, epimedin A, epimedin B, and epimedin C incubated with
jejunum enzymes, respectively, compared with the sham group. In
addition, the apparent permeability coefficient and elimination
percentage of the four epimedium flavonoids in the duodenum,
jejunum, ileum, and colon decreased by 29%–44%, 32%–50%,
40%–56%, and 27%–53% compared with that in sham rats,
respectively. The main metabolites of the four epimedium flavonoids were the same for the two groups after intestinal perfusion,
or flora and enzyme incubation.
CONCLUSIONS:
In conclusion, the amount and
activity of intestinal flora and enzymes changed in ovariectomized
rats, which affected the intestinal absorption and hydrolysis of
epimedium flavonoids whose structures contain 7-glucose. |
|
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