Absorption Properties of Luteolin and Apigenin in Genkwa Flos Using In Situ Single-Pass Intestinal Perfusion System in the Rat
| Autor: | Xin He, Chun-Feng Zhang, Cui-Ping Jiang, Zi-Jing Song |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
Male
Daphne genkwa Colon Flos Ileum Flowers Pharmacology 030226 pharmacology & pharmacy Intestinal absorption Rats Sprague-Dawley 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Intestine Small medicine Animals Apigenin Luteolin biology Probenecid General Medicine biology.organism_classification Small intestine Camphor Perfusion medicine.anatomical_structure Intestinal Absorption Complementary and alternative medicine Biochemistry chemistry 030220 oncology & carcinogenesis Genkwanin Models Animal Daphne |
| Zdroj: | The American Journal of Chinese Medicine. 45:1745-1759 |
| ISSN: | 1793-6853 0192-415X |
| DOI: | 10.1142/s0192415x1750094x |
| Popis: | The flower bud of Daphne genkwa (Genkwa Flos) is a commonly used herbal medicine in Asian countries. Luteolin and apigenin are two recognized active flavonoids in Genkwa Flos. The aim of this study was to investigate the intestinal absorption mechanisms of Genkwa Flos flavonoids using in situ single-pass intestinal perfusion rat model. Using HPLC, we determined its major effective flavonoids luteolin, apigenin, as well as, hydroxygenkwanin and genkwanin in biological samples. The intestinal absorption mechanisms of the total flavonoids in Genkwa Flos (TFG) were investigated using in situ single-pass intestinal perfusion rat model. Comparing the TFG absorption rate in different intestinal segments, data showed that the small intestine absorption was significantly higher than that of the colon ([Formula: see text]). Compared with duodenum and ileum, the jejunum was the best small intestinal site for TFG absorption. The high TFG concentration (61.48[Formula: see text][Formula: see text]g/ml) yielded the highest permeability ([Formula: see text]). Subsequently, three membrane protein inhibitors (verapamil, pantoprazole and probenecid) were used to explore the TFG absorption pathways. Data showed probenecid, a multidrug resistance protein (or MRP) inhibitor, effectively enhanced the TFG absorption ([Formula: see text]). Furthermore, by comparing commonly used natural absorption enhancers on TFG, it was observed that camphor was the most effective. In Situ single-pass intestinal perfusion experiment shows that TFG absorption is much higher in the small intestine than in the colon, and the TFG is absorbed mainly via an active transport pathway with MRP-mediated efflux mechanism. Camphor obviously enhanced the TFG absorption, and this could be an effective TFG formulation preparation method to increase clinical effectiveness after Genkwa Flos administration. Our study elucidated the TFG absorption mechanisms, and provided new information for its formulation preparation. |
| Databáze: | OpenAIRE |
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