Metabolic rates and metabolites of three lignans in schisandra chinensis (turcz.) baill in rat liver microsomes / 第二军医大学学报

ABSTRACT

Objective To investigate the metabolic rates of three lignans (deoxyschizandrin, schizandrol B and schisantherin) of Schisandra chinensis (Turcz.) Baill in rat liver microsomes, and to identify their metabolites. Methods Using the in vitro rat liver microsomal model, the contents of the 3 lignans were determined by HPLC-MS and the matobilic rates were calculated. The analytical conditions were as follows column, Agilent Zorbax SB-C18(3. 0 mm × 100 mm, 3. 5 fm) i mobile phase, acetonitrile/water (60 40 V/V), with isocratic elutioni injection volume, 5 μL; flowing rate, 0. 8 mL/mini temperature of column, 30°C; running time, 30 min; selective ion monitoring (SIM) in positive ion mode was used in mass spectrometry, with the drying gas temperature being 350°C, capillary voltage being 4 000 V, drying gas flowing rate being 9. 0 L/min, and fragmentor voltage being 90 eV. Their metabolites were identified by HPLC-TOF/MS, whose mass parameters were the same as those of HPLC-MS. Results Deoxyschizandrin, schizandrol B and schisantherin were separated with good linearity (r>0. 999 0) between 0. 010 22-2. 044, 0. 044 24-2. 212 and 0. 042 32-2. 116 μg/mL, respectively. The intra-day and inter-day precisions were less than 5 %, the matrix effect was higher than 75 %, and the extraction recovery rate was higehr than 80%. The metabolic half-life values of the 3 lignans were as follows deoxyschizandrin 0. 721 0 min,schizandrol B 43. 58 min, and schisantherin 86. 63 min. HPLC-TOF/MS identified 7 metabolites in deoxyschizandrin, 6 in schizandrol B and 4 in schisantherin. Conclusion The lignans in Schisandra chinensis (Turcz.) Baill are easy to be metabolized in rat liver microsomes, which will affect the bioavailability and pharmaceutical efficacy of lignans in Schisandra chinensis (Turcz.) Baill.