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Absorption characteristics of the total alkaloids from Mahonia bealei in an in situ single-pass intestinal perfusion assay

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Chinese Journal of Natural Medicines 2014年第7期12卷 554-560页

作者： SUN Yu-He HE Xin YANG Xiao-Lin DONG Cui-Lan ZHANG Chun-Feng SONG Zi-Jing LU Ming-Xing YANG Zhong-Lin LI Ping State Key Laboratory of Natural Medicines China Pharmaceutical University School of pharmacy Nanjing University of Chinese Medicine Guangdong Provincial Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research Jinan University The People's Hospital of Zhangqiu City

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.

关键词： mahoniae Caulis Total alkaloids In situ single-pass intestinal perfusion Absorption enhancers Protein inhibitors

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