Details

Autor(en) / Beteiligte

• Buqui, Gabriela A.
• Sy, Sherwin K.B.
• Merino-Sanjuán, Matilde
• Gouvea, Dayana R.
• Nixdorf, Suzana L.
• Kimura, Elza
• Derendorf, Hartmut
• Lopes, Norberto P.
• Diniz, Andrea

Titel

Characterization of intestinal absorption of C-glycoside flavonoid vicenin-2 from Lychnophora ericoides leafs in rats by nonlinear mixed effects modeling

Ist Teil von

• Revista brasileira de farmacognosia, 2015-05, Vol.25 (3), p.212-218

Ort / Verlag

Cham: Elsevier Editora Ltda

Erscheinungsjahr

2015

Quelle

Free E-Journal (出版社公開部分のみ）

Beschreibungen/Notizen

• Vicenin-2 (apigenin-6,8-di-C-β-d-glucopyranoside) is present in hydroalcoholic extracts of the Brazilian species Lychnophora ericoides Mart., Asteraceae, leaves, and the biological effects of this compound have been demonstrated including anti-inflammatory, antioxidant and anti-tumor effects in rat models. Given the potential of this compound as a pharmacological agent, the aims of this investigation were to evaluate the extent of intestinal absorption of vicenin-2, and to determine the intestinal permeation profile using an in situ single-pass intestinal perfusion technique. A validated HPLC–UV method was applied to measure the amount of unabsorbed vicenin-2 in the gut after an oral administration of 180mgkg−1 in five rats. A nonlinear mixed effects model was used to determine the absorption pharmacokinetic parameters assuming a first order absorption and active secretion processes for this compound, wherein the active secretion was characterized by a zero-order process. The population pharmacokinetic parameters obtained were 0.274min−1 for the first-order absorption rate constant, 16.3%min−1 for the zero-order rate constant; the final percentage of the original dose that was absorbed in vivo was 40.2±2.5%. These parameters indicated that vicenin-2 was rapidly absorbed in the small intestine. In contrast to literature information indicating no absorption of vicenin-2 in Caco-2 cells, our results suggested that vicenin-2 can be absorbed in the small intestine of rats. The finding supports further investigation of vicenin-2 as a viable oral phytopharmaceutical agent for digestive diseases.