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Effect of cortex mori on pharmacokinetic profiles of main isoflavonoids from pueraria lobata in rat plasma

作者 Xiao, Bingxin; Sun, Zengxian; Sun, Shu yang; Dong, Jie; Li, Yanli; Gao, Shan; Pang, Jie; Chang, Qi

期刊 JOURNAL OF ETHNOPHARMACOLOGY , JAN 10 2014,1:151

DOI 10.1016/j.jep.2013.11.024 PubMed 24286962

摘要 Ethnopharmacological relevance: Radix pueraria (the root of pueraria lobata (Wild.) Ohwi.), which contains a class of isoflavonoids as the main active components, as well as cortex mori (the root bark of Morus alba L), which contains abundant active alkaloids, have been employed for the treatment of diabetes in traditional Chinese medicine for centuries. In previous studies, pharmacodynamic synergistic reactions have been observed in compatible application of pueraria lobata isoflavonoids extracts (PLF) and cortex mod alkaloids extracts (CME) for inhibiting a-glycosidase activity. It has also been demonstrated that PLF can effectively slow down the absorption of active alkaloid from CME, so as to produce a higher effective concentration in small intestine for depressing the elevation of postprandial blood glucose through inhibiting a-glycosidase activity.Aim of the study: In this study, the hypoglycemic effect of PLF, CME or CME-PLF mixture (the mixture of CME and PLF at a ratio of 1:6.3) was further evaluated through in vivo glucose tolerance studies. And the effect of CME on pharmacokinetic profiles of main isoflavonoids from PLF in rat plasma was investigated to further underlie compatibility mechanism of the two herbs.Materials and methods: Four groups of rats received an oral dose of starch solution alone or simultaneously with drugs by gavage feeding. The blood samples were collected to determine glucose concentrations by glucose oxidase method. In addition, another two groups of rats were orally administered with PLF or CME-PLF. The plasma samples were collected and assayed using an LC/MS/MS method for comparatively pharmacokinetic studies of five main isoflavonoids.Results: For starch loading, co-administration of CME-PLF resulted in more potent inhibition effects on glucose responses compared to those by CME or PLF in rat. The isoflavonoids from PLF were rapidly absorbed, presenting similarly low concentrations in plasma. When CME was added, the C-max and AUC of all the five isoflavonoids were increased. A phenomenon of double peaks was found for all analysts. The elimination rates of all the detected isoflavonoids were also slowed down with extension of tin.Conclusions: CME has been found to increase the absorption and delay the elimination of main isoflavonoids from PLF, which might result in higher concentrations of circulating active compounds for anti diabetes.

涉及物种 桑 Morus alba