RESUMEN
1. The aurantio-obtusin's glucuronide was detected when aurantio-obtusin was incubated with human liver microsomes (HLMs). Recombinant UGT isoforms screening experiment showed that UGT1A8 was the major isoform contributed to the glucuronidation. 2. The metabolic profiles for aurantio-obtusin in liver microsomes from different species were similar, however, the intrinsic clearance values (Vmax/Km) among the species were: Monkey > Human > Rat > Rabbit > Dog > Pig > Mouse > Guinea pig.
Asunto(s)
Antraquinonas/metabolismo , Glucurónidos/metabolismo , Glucuronosiltransferasa/metabolismo , Animales , Pruebas de Enzimas , Glucurónidos/química , Humanos , Cinética , Espectrometría de Masas , Microsomas Hepáticos/metabolismo , Proteínas Recombinantes/metabolismo , Especificidad de la EspecieRESUMEN
OBJECTIVE: To establish an effective and convenient method for HPLC fingerprints of Xuezhiling tablets and new Xuezhiling tablets, and to observe the changes of fingerprint with crude and processed Cassiae Semen in Xuezhiling tablets. METHODS: The HPLC with Agilent TC-C18 (4.6 mm x 250 mm, 5 microm) column was used for the gradient elution of acetonitrile-0.1% phosphoric acid solution, at the flow rate of 1.0 mL/min. Detection wavelength was set at 284 nm and the column temperature was 30 degrees C. RESULTS: Ten batches of Xuezhiling tablets and new Xuezhiling tablets were tested and gained HPLC fingerprint containing 20 common peaks, respectively. CONCLUSION: This method is stable and reliable. The number of common peaks of fingerprint had little change after the crude and processed Cassiae Semen in Xuezhiling tablets interchangeably, but the contents of some components had significant changes.