Absorption characteristics of the total alkaloids from Mahonia bealei in an in situ single-pass intestinal perfusion assay
| Autor: | Xin He, Yu-He Sun, Li Ping, Cui-Lan Dong, Zhonglin Yang, Zi-Jing Song, Chun-Feng Zhang, Ming-Xing Lu, Xiaolin Yang |
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| Rok vydání: | 2014 |
| Předmět: |
Male
Jatrorrhizine Stereochemistry Mahonia bealei Mahonia Absorption (skin) Permeability Intestinal absorption Borneol Rats Sprague-Dawley chemistry.chemical_compound Alkaloids Berberine Drug Stability Drug Discovery Animals Intestinal Mucosa Chromatography biology Chemistry General Medicine biology.organism_classification Menthone Rats Intestines Kinetics Intestinal Absorption Complementary and alternative medicine Menthol Drugs Chinese Herbal |
| Zdroj: | Chinese Journal of Natural Medicines. 12:554-560 |
| ISSN: | 1875-5364 |
| DOI: | 10.1016/s1875-5364(14)60085-6 |
| Popis: | Aim To investigate the absorption characteristics of the total alkaloids from Mahoniae Caulis (TAMC) through the administration of monterpene absorption enhancers or protein inhibitors. Method The absorption behavior was investigated in an in situ single-pass intestinal perfusion (SPIP) assay in rats. Results The intestinal absorption of TAMC was much more than that of a single compound or a mixture of compounds (jatrorrhizine, palmatine, and berberine). Promotion of absorption by the bicyclic monoterpenoids (borneol or camphor) was higher than by the monocyclic monoterpenes (menthol or menthone), and promotion by compounds with a hydroxyl group (borneol or menthol) was higher than those with a carbonyl group (camphor or menthone). The apparent permeability coefficient ( Papp ) of TAMC was increased to 1.8-fold by verapamil, while it was reduced to one half by thiamine. The absorption rate constant ( Ka ) and Papp of TAMC were unchanged by probenecid and pantoprazole. Conclusion The intestinal absorption characteristics of TAMC might be passive transport, and the intestinum tenue was the best absorptive site. In addition, TAMC might be likely a substrate of P-glycoprotein (P-gp) and organic cation transporters (OCT), rather than multidrug resistance protein (MRP) and breast cancer resistance protein (BCRP). Compared with a single compound and a mixture of compounds, TAMC was able to be absorbed in the blood circulation effectively. |
| Databáze: | OpenAIRE |
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