ABSTRACT
Poliumoside is representative of phenylethanoid glycosides, which are widely found in many plants. Poliumoside is also regarded as the main active component of Callicarpa kwangtungensis Chun (CK), though its oral bioavailability in rat is extremely low (0.69%) and its in vivo and in vitro metabolism has not yet been systematically investigated. In the present study, an ultra performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS) method was employed to identify the metabolites and investigate the metabolic pathways of poliumoside in rat after oral administration 1.5 g·kg-1 of poliumoside. As a result, a total of 34 metabolites (30 from urine, 17 from plasma, and 4 from bile) and 9 possible metabolic pathways (rearrangment, reduction, hydration, hydrolyzation, dehydration, methylation, hydroxylation, acetylation, and sulfation) were proposed in vivo. The main metabolite, acteoside, was quantified after incubated with rat intestinal bacteria in vitro. In conclusion, the present study systematically explored the metabolites of poliumoside in vivo and in vitro, proposing metabolic pathways that may be significant for further metabolic studies of poliumoside.
Subject(s)
Bacteria/metabolism , Bile/chemistry , Caffeic Acids/chemistry , Callicarpa/chemistry , Drugs, Chinese Herbal/chemistry , Glycosides/chemistry , Intestines/microbiology , Plasma/chemistry , Urine/chemistry , Administration, Oral , Animals , Caffeic Acids/administration & dosage , Caffeic Acids/blood , Caffeic Acids/urine , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal/administration & dosage , Drugs, Chinese Herbal/metabolism , Glycosides/administration & dosage , Glycosides/blood , Glycosides/urine , Male , Mass Spectrometry/methods , Molecular Structure , Rats , Rats, Sprague-DawleyABSTRACT
BACKGROUND: Stemonae radix has been applied in traditional Chinese medicine for centuries. Alkaloids are the main active ingredient in stemonae radix, so their composition and concentration levels are directly linked to clinic effects. OBJECTIVE: The objective was to develop an analytical method with multiple markers for quality survey of commercial stemonae radix. MATERIALS AND METHODS: A method for simultaneous determination of six compounds in commercial stemonae radix was performed using solid-phase extraction and high-performance liquid chromatography coupled with evaporative light scattering detector. The separation was carried out on an Agilent TC-C18 column with 0.1% acetonitrile solution of triethylamine aqueous solution and acetonitrile as the mobile phase under gradient elution within 70 min. The hierarchical clustering analysis (HCA) was successfully used to classify the samples in accordance with their chemical constituents. RESULTS: Linearity (R(2) > 0.9990), intra- and inter-day precision (relative standard deviations <4%), limit of detection (0.011-0.086 µg/mL), limit of quantification (0.033-0.259 µg/mL) of the six alkaloids were determined, and the recoveries were between 96.6% and 103.7%. The method was successfully applied to analysis 36 batches of commercial stemonae radix. All the samples could be classified into five clusters by HCA. CONCLUSION: This article provides an accurate and simple analytical method for quality survey of commercial stemonae radix. Because of the significant chemical variations, careful selection of Stemona sources with obvious antitussive value but devoid of croomine followed by good agricultural practice and good manufacturing practice process is suggested.
