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Pharmacokinetics of mangiferin and its metabolite-norathyriol, Part 2: Influence of UGT, CYP450, P-gp, and enterobacteria and the potential interaction in Rhizoma Anemarrhenae decoction with timosaponin B2 as the major contributor : MGF in Metabolic Disorders Treatment

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      Comparative pharmacokinetics of baicalin after oral administration of pure baicalin, Radix scutellariae extract and Huang-Lian-Jie-Du-Tang to rats.

      Huang-Lian-Jie-Du-Tang (HLJDT) is an important "heat-clearing" multiherb remedy of traditional Chinese medicine, and Radix scutellariae (Scutellaria baicalensis Georgi, Labiatae) is a key ingredient herb in it. Baicalin and wogonoside are two main effective ingredients enriched in Radix scutellariae. In the present study, pharmacokinetic differences of baicalin following oral administration of pure baicalin, Radix scutellariae extract, baicalin co-administrated with extract of the other three herbs of HLJDT and HLJDT were investigated in male S.D. rats with approximately the same dose of 200 mg/kg baicalin. The pharmacokinetic comparison of wogonoside was conducted only in Radix scutellariae extract and HLJDT. Plasma concentrations of baicalin and wogonoside were determined using HPLC method. Unpaired Student's t-test was used for statistical comparison. The results indicated that baicalin and wogonoside demonstrated bimodal phenomenon in the plasma profile. Some ingredients in the other three herbs of HLJDT, not in Radix scutellariae itself, had pharmacokinetic interaction with baicalin and wogonoside and hence decreased their systematic exposure level (p<0.01). The absorption site of baicalin was preliminary evaluated in rat using in situ absorption in stomach and different intestinal segments and results revealed the existence of double-site absorption of baicalin. The first absorption site was in upper intestinal, probably via directly absorption of baicalin; while the second absorption site was in colon in the form of aglygon.
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        Antidiabetic activity of the rhizoma of Anemarrhena asphodeloides and active components, mangiferin and its glucoside.

        The antidiabetic activity of the rhizoma of Anemarrhena asphodeloides was investigated in KK-Ay mice, an animal model of genetic type 2 diabetes. The water extract of the rhizoma (AA) (90 mg/kg) reduced blood glucose levels from 570 +/- 29 to 401 +/- 59 mg/dl 7 h after oral administration (p<0.05) and also tended to reduce serum insulin levels in KK-Ay mice. AA-treated KK-Ay mice had significantly reduced blood glucose levels in an insulin tolerance test. Based on these results, the antidiabetic mechanism of AA may be due to decreased insulin resistance. In addition, the active components of AA were confirmed to be mangiferin and its glucoside.
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          Oxidative demethylenation and subsequent glucuronidation are the major metabolic pathways of berberine in rats.

          Present study was designed to explore roles of metabolic clearance in the disposition of berberine (BBR) in rats, with a focus on oxidative metabolism and subsequent glucuronidation. Plasma from rats after intravenous administration of BBR was collected to identify and quantify BBR and its major metabolites. The major circulating metabolites of BBR were oxidative metabolites M1 (via demethylation) and M2 (via demethylenation) and their corresponding glucuronides, with M2-glucuronide approximately 24-fold higher than M1-glucuronide. Incubations with rat liver microsomes were conducted to examine formation kinetics of two oxidative metabolites-M1 and M2, and depletion kinetics of M1 and M2, leading to the formation of glucuronide conjugates. Efforts were also made to examine roles of key CYPs and UGTs isoforms responsible for BBR metabolism using known chemical inhibitors and/or substrates. In vitro, the formation of M1 and M2 were comparable and multiple CYP enzymes were involved. In contrast, the glucuronidation of M2 was much faster than that of M1. Inhibition studies using well-characterized UGT substrates suggested both M1 and M2 could be glucuronidated by UGT1A1 and UGT2B1 while M2 glucuronidation was favored by UGT1A1. In summary, oxidative demethylenation and the subsequent glucuronidation were the major metabolic pathways of BBR in rats. (c) 2009 Wiley-Liss, Inc. and the American Pharmacists Association
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            Author and article information

            Affiliations
            [1 ]Modernization of Traditional Chinese Medicine, Shanghai Institute of Materia Medica; University of Chinese Academy of Sciences, Shanghai People's Republic of China
            [2 ]College of Life and Environmental Sciences, Shanghai Normal University; Shanghai People's Republic of China
            [3 ]Department of Pharmacy, Harbin University of Commerce; Harbin People's Republic of China
            Journal
            BioFactors
            BioFactors
            Wiley
            09516433
            September 10 2016
            September 10 2016
            May 06 2016
            : 42
            : 5
            : 545-555
            10.1002/biof.1290
            © 2016

            http://doi.wiley.com/10.1002/tdm_license_1.1

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            Self URI (article page): http://doi.wiley.com/10.1002/biof.1290

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