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Pharmacokinetics of anthraquinones in rat plasma after oral administration of a rhubarb extract.
Biomed Chromatogr. 2014 Apr; 28(4):564-72.BC

Abstract

A sensitive and specific LC-MS/MS method was developed for simultaneous determination of aloe-emodin, rhein, emodin, chrysophanol and physcion and their conjugates in rat plasma. The lower limit of quantitation of each anthraquinone was 0.020-0.040 µm. Intra-day and inter-day accuracies were 90.1-114.3% and the precisions were <14.6%. The matrix effects were 104.0-113.2%. The method was successfully applied to a pharmacokinetic study in rats receiving a rhubarb extract orally. The area under the concentration-time curve (AUC0-t) and peak concentration (Cmax) of free aloe-emodin and emodin in rat plasma were much lower than those of rhein. The amounts of chrysophanol and physcion were too low to be continuously detected. After treating the plasma samples with β-glucuronidases, each anthraquinone was detectable throughout the experimental period (36 h) and showed much higher plasma concentrations and AUC0-t . The free/total ratios of aloe-emodin, rhein and emodin were 6.5, 49.0 and 1.7% for Cmax and 3.7, 32.5 and 1.1% for AUC0-t , respectively. The dose-normalized AUC0-t and Cmax of the total of each anthraquinone were in the same descending order: rhein > emodin > chrysophanol > physcion > aloe-emodin. These findings reveal phase II conjugates as the dominant in vivo existing forms of rhubarb antharquinones and warrant a further study to evaluate their contribution to the herbal activity.

Authors+Show Affiliations

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24136708

Citation

Wu, Wenjin, et al. "Pharmacokinetics of Anthraquinones in Rat Plasma After Oral Administration of a Rhubarb Extract." Biomedical Chromatography : BMC, vol. 28, no. 4, 2014, pp. 564-72.
Wu W, Yan R, Yao M, et al. Pharmacokinetics of anthraquinones in rat plasma after oral administration of a rhubarb extract. Biomed Chromatogr. 2014;28(4):564-72.
Wu, W., Yan, R., Yao, M., Zhan, Y., & Wang, Y. (2014). Pharmacokinetics of anthraquinones in rat plasma after oral administration of a rhubarb extract. Biomedical Chromatography : BMC, 28(4), 564-72. https://doi.org/10.1002/bmc.3070
Wu W, et al. Pharmacokinetics of Anthraquinones in Rat Plasma After Oral Administration of a Rhubarb Extract. Biomed Chromatogr. 2014;28(4):564-72. PubMed PMID: 24136708.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pharmacokinetics of anthraquinones in rat plasma after oral administration of a rhubarb extract. AU - Wu,Wenjin, AU - Yan,Ru, AU - Yao,Meicun, AU - Zhan,Ying, AU - Wang,Yitao, Y1 - 2013/10/18/ PY - 2013/07/30/received PY - 2013/09/09/revised PY - 2013/09/20/accepted PY - 2013/10/19/entrez PY - 2013/10/19/pubmed PY - 2014/11/14/medline KW - LC-MS/MS KW - anthraquinones KW - conjugation KW - pharmacokinetics KW - rhubarb SP - 564 EP - 72 JF - Biomedical chromatography : BMC JO - Biomed Chromatogr VL - 28 IS - 4 N2 - A sensitive and specific LC-MS/MS method was developed for simultaneous determination of aloe-emodin, rhein, emodin, chrysophanol and physcion and their conjugates in rat plasma. The lower limit of quantitation of each anthraquinone was 0.020-0.040 µm. Intra-day and inter-day accuracies were 90.1-114.3% and the precisions were <14.6%. The matrix effects were 104.0-113.2%. The method was successfully applied to a pharmacokinetic study in rats receiving a rhubarb extract orally. The area under the concentration-time curve (AUC0-t) and peak concentration (Cmax) of free aloe-emodin and emodin in rat plasma were much lower than those of rhein. The amounts of chrysophanol and physcion were too low to be continuously detected. After treating the plasma samples with β-glucuronidases, each anthraquinone was detectable throughout the experimental period (36 h) and showed much higher plasma concentrations and AUC0-t . The free/total ratios of aloe-emodin, rhein and emodin were 6.5, 49.0 and 1.7% for Cmax and 3.7, 32.5 and 1.1% for AUC0-t , respectively. The dose-normalized AUC0-t and Cmax of the total of each anthraquinone were in the same descending order: rhein > emodin > chrysophanol > physcion > aloe-emodin. These findings reveal phase II conjugates as the dominant in vivo existing forms of rhubarb antharquinones and warrant a further study to evaluate their contribution to the herbal activity. SN - 1099-0801 UR - https://www.unboundmedicine.com/medline/citation/24136708/Pharmacokinetics_of_anthraquinones_in_rat_plasma_after_oral_administration_of_a_rhubarb_extract_ L2 - https://doi.org/10.1002/bmc.3070 DB - PRIME DP - Unbound Medicine ER -