Metabolite Profiles of Epimedin B in Rats by Ultraperformance Liquid Chromatography/Quadrupole-Time-of-Flight Mass Spectrometry

Cui, Li; Sun, E; Zhang, Zhenhai; Qian, Qian; Tan, Xuecai; Xu, Fei; Jia, Xiao‐Bin

doi:10.1021/jf304625x

Cited by 24 publications

(9 citation statements)

References 16 publications

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“…Third, these flavonoids can be hydrolyzed by hydrolase in the intestinal mucosa and flora. Lactase phlorizin hydrolase (LPH) and b-glucosidase were confirmed as the main hydrolases in intestinal mucosa and flora, which could hydrolyze the epimedium flavonoids to secondary glycosides or aglycon (Zhao et al, 2010;Qian et al, 2012;Cui et al, 2013). The above results were obtained with healthy animals; however, the absorption and hydrolysis behavior in osteoporotic animals remains unknown.…”

Section: Introductionmentioning

confidence: 95%

Intestinal Absorption and Metabolism of Epimedium Flavonoids in Osteoporosis Rats

et al. 2015

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Herba Epimdii is a traditional Chinese medicine used to treat osteoporosis. Its main pharmacological ingredients are flavonoids. In previous studies conducted in healthy animals, we showed that epimedium flavonoids could be hydrolyzed into secondary glycosides or aglycon by intestinal flora or enzymes, thereby enhancing their absorption and antiosteoporosis activity. To study the medicine in the pathologic state, epimedium flavonoids were incubated with intestinal mucosa and feces in vitro and intestinal perfusion in situ to explore the differences in absorption and metabolism between sham and osteoporosis rats. For osteoporosis rats, the hydrolysis rates of icariin, epimedin A, epimedin B, and epimedin C incubated with intestinal flora for 1 hour were reduced by 0.19, 0.26, 0.19, and 0.14, respectively, compared with that in sham rats. Hydrolysis rates were reduced by 0.21, 0.24, 0.08, and 0.31 for icariin, epimedin A, epimedin B, and epimedin C incubated with duodenal enzymes for 1 hour and by 0.13, 0.09, 0.07, and 0.47 for icariin, epimedin A, epimedin B, and epimedin C incubated with jejunum enzymes, respectively, compared with the sham group. In addition, the apparent permeability coefficient and elimination percentage of the four epimedium flavonoids in the duodenum, jejunum, ileum, and colon decreased by 29%-44%, 32%-50%, 40%-56%, and 27%-53% compared with that in sham rats, respectively. The main metabolites of the four epimedium flavonoids were the same for the two groups after intestinal perfusion, or flora and enzyme incubation. In conclusion, the amount and activity of intestinal flora and enzymes changed in ovariectomized rats, which affected the intestinal absorption and hydrolysis of epimedium flavonoids whose structures contain 7-glucose.

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Section: Introductionmentioning

confidence: 95%

Intestinal Absorption and Metabolism of Epimedium Flavonoids in Osteoporosis Rats

et al. 2015

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“…UPLC‐QTOF/MS, a powerful hyphenated technique, was used for profiling studies of the metabolites of the active ingredients with high resolution, high sensitivity . Chromatography was performed using an ACQUITY UPLC system (Waters Corp., Milford, MA, USA) equipped with a conditioned autosampler at 4 °C.…”

Section: Methodsmentioning

confidence: 91%

“…UPLC-QTOF/MS, a powerful hyphenated technique, [15,16] was used for profiling studies of the metabolites of the active ingredients with high resolution, high sensitivity. [17][18][19][20][21] Chromatography was performed using an ACQUITY UPLC system (Waters Corp., Milford, MA, USA) equipped with a conditioned autosampler at 4°C. The separation was carried out on an Acquity UPLC BEH C 18 column (ID, 1.7 μm; 2.1 × 50 mm; Waters, Milford, MA, USA).…”

Section: Instrumentation and Conditions Of Uplc-qtof-msmentioning

confidence: 99%

Metabolic profiling of isomeric aglycones central‐icaritin (c‐IT) and icaritin (IT) in osteoporotic rats by UPLC‐QTOF‐MS

Jiang

Feng

Sun

et al. 2014

Drug Testing and Analysis

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The isomers, although of similarly chemical structures, have different pharmacological activities due to their metabolic processes in vivo. Central-icaritin (c-IT) and icaritin (IT) are isomers and major bioactive aglycones of the Herba Epimedii. In this study, we found that the anti-osteoporotic effect of c-IT was stronger than IT on bone structural changes in osteoporotic rats evaluated by Micro-μCT with the parameters of bone mineral density (BMD), bone mineral content (BMC), tissue mineral content (TMC), and tissue mineral density (TMD). c-IT treatment significantly increased the bone microarchitecture, compared with IT (p < 0.05). In order to explain their differences in anti-osteoporosis, the metabolic profiling and pathways of c-IT and IT in the plasma, bile, urine, and faeces of ovariectomized (OVX) rats were investigated by ultra-performance liquid chromatography quadrupole time of flight mass spectrometry (UPLC-QTOF-MS) after oral administration of c-IT or IT (80 mg/kg). Finally, 59 metabolites of c-IT and 43 metabolites of IT were identified by elucidating their corresponding quasimolecular ions and fragment ions. IT could be quickly absorbed into blood and reached a maximum plasma concentration, and then be rapidly conversed to its glucuronidation metabolites, most of which were excreted out by urine. Interestingly, the absorbed and conjugated speeds of c-IT were slower than IT. The metabolic processes of c-IT existed enterohepatic circulation, which decreased the metabolism and excretion rate of c-IT, and prolonged the anti-osteoporosis effect. Our findings provided evidence on the difference on metabolic profiles of c-IT and IT in osteoporotic rats, which might shed new lights on improving anti-osteoporotic effects of IT and c-IT.

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“…Rats were divided into two groups: epimedin C and control; each group contained three rats. Epimedin C preparation containing 20% polyethylene glycol-400 was orally administered to male rats at a single dose of 80 mg/kg body weight (Cui et al, 2013). In the control group, deionized water was administered orally to rats at a dose of 10 mL/kg body weight.…”

Section: Animals and Drug Administrationmentioning

confidence: 99%

Metabolite profiles of epimedin C in rat plasma and bile by ultra‐performance liquid chromatography coupled with quadrupole‐TOF‐MS

Cui

Sun

Zhang

et al. 2014

Biomedical Chromatography

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Epimedin C is one of the major bioactive constituents of Herba Epimedii. In this study, the metabolite profiles of epimedin C in rat plasma and bile were qualitatively investigated, and the possible metabolic pathways of epimedin C were subsequently proposed. After oral administration of epimedin C at a single dose of 80 mg/kg, rat biological samples were collected and pretreated by protein precipitation. Then these pretreated samples were injected into an Acquity UPLC BEH C18 column and detected by ultra-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry. In all, 12 metabolites were identified in the biosamples. Of these, eight, two from plasma and six from bile, are, to our knowledge, reported here for the first time. The results indicated that epimedin C was metabolized via desugarization, dehydrogenation, hydrogenation, dehydroxylation, hydroxylation, demethylation and glucuronidation pathways in vivo. Thus, this study revealed the possible metabolite profiles of epimedin C in rat plasma and bile.

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Metabolite Profiles of Epimedin B in Rats by Ultraperformance Liquid Chromatography/Quadrupole-Time-of-Flight Mass Spectrometry

Cited by 24 publications

References 16 publications

Intestinal Absorption and Metabolism of Epimedium Flavonoids in Osteoporosis Rats

Intestinal Absorption and Metabolism of Epimedium Flavonoids in Osteoporosis Rats

Metabolic profiling of isomeric aglycones central‐icaritin (c‐IT) and icaritin (IT) in osteoporotic rats by UPLC‐QTOF‐MS

Metabolite profiles of epimedin C in rat plasma and bile by ultra‐performance liquid chromatography coupled with quadrupole‐TOF‐MS

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