Metabolite profile analysis and pharmacokinetic study of emodin, baicalin and geniposide in rats

• Published in: Xenobiotica Vol. 48; no. 9; pp. 927 - 937
• Main Authors: Yu, Jing, Guo, Xiucai, Zhang, Qingqing, Peng, Ying, Zheng, Jiang
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 02-09-2018
• Subjects: Animals; Calibration; Drugs, Chinese Herbal - pharmacokinetics; Emodin - metabolism; Emodin - pharmacokinetics; Flavonoids - metabolism; Flavonoids - pharmacokinetics; Iridoids - metabolism; Iridoids - pharmacokinetics; Limit of Detection; Male; Mass Spectrometry - methods; Metabolic fate of multiple components; metabolic pathways; metabolite identification; pharmacokinetics; Rats, Sprague-Dawley; Reproducibility of Results; UPLC/Q-TOF-MS; Zhi-Su-Ning; pharmacokinetics; Metabolic fate of multiple components; UPLC/Q-TOF-MS; Zhi-Su-Ning; metabolite identification; metabolic pathways
• ISSN: 0049-8254; 1366-5928
• DOI: 10.1080/00498254.2017.1382748

1. Emodin, baicalin and geniposide are the major bioactive components in Da-Huang, Huang-Qin and Zhi-Zi which are herbal medicines widely used in Asian nations.
2. The metabolism of the three compounds was found to undergo hydroxylation, decarboxylation, dehydration, methylation, hydrolysis, hydrogenation, dihydrogenation, sulfation, glucosidation and/or glucuronidation. A total of 63 metabolites were detected in urine, plasma and bile of rats given a mixture of the three compounds.
3. Pharmacokinetic properties of the three compounds were determined in rats given the extracts of Da-Huang, Huang-Qin and Zhi-Zi. The pharmacokinetic parameters for emodin, baicalin and geniposide were found to be 0.13 ± 0.11, 0.25 ± 0.12 and 0.40 ± 0.09 h (T
max
); 21 ± 9, 1515 ± 254 and 482 ± 50 ng/mL (C
max
); 8.6 ± 5.5, 18.3 ± 2.8 and 22.1 ± 17.2 h (t
1/2
); 29 ± 20, 16886 ± 3734 and 2936 ± 551 ng/mLċh (AUC
(0-t)
); and 37 ± 20, 22624 ± 6295 and 3582 ± 820 ng/mLċh (AUC
(0-∞)
).
4. The metabolism and pharmacokinetic studies facilitate appropriate employment of Da-Huang, Huang-Qin and Zhi-Zi in clinic.