Study on pharmacokinetics and tissues distribution of neomangiferin, mangiferin, timosaponin BII, Timosaponin BIII, and timosaponin AIII after oral administration of Anemarrhenae rhizoma extract in rats

Pharmacognosy Magazine ,2019,15,65,557-567.DOI:10.4103/pm.pm_65_19Published:September 2019Type:Original Article Authors:De Ji, Jin-Chun Qiu, Xiao-Nan Su, Yu-Wen Qin, Min Hao, Lin Li, Tu-Lin Lu, Xiao-Kun Li, and Cheng-Xi Jiang Author(s) affiliations:De Ji1, Jin-Chun Qiu2, Xiao-Nan Su3, Yu-Wen Qin4, Min Hao3, Lin Li3, Tu-Lin Lu3, Xiao-Kun Li5, Cheng-Xi Jiang6 1Department of Chinese Medicinal Processing, School of Pharmacy, Nanjing University of Chinese Medicine; Molecular Pharmacology Research Center, School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou, PR China 2Department of Pharmacy, Children's Hospital of Nanjing Medical University, Nanjing, PR China 3Department of Chinese Medicinal Processing, School of Pharmacy, Nanjing University of Chinese Medicine, Wenzhou, PR China 4Department of Chinese Medicinal Resources, Life Sciences Institute, Wenzhou University, Wenzhou, PR China 5Molecular Pharmacology Research Center, School of Pharmaceutical Science, Wenzhou Medical University; Department of Chinese Medicinal Resources, Biomedical Collaborative Innovation Center of Zhejiang, Wenzhou, PR China 6Department of Chinese Medicinal Resources, Life Sciences Institute, Wenzhou University; Department of Chinese Medicinal Resources, Biomedical Collaborative Innovation Center of Zhejiang, Wenzhou, PR China Abstract:Background: Anemarrhenae rhizoma (AR) is widely used for the treatment of febrile diseases, cough, and diabetes in traditional Chinese medicines. AR mainly contains flavonoids and steroidal saponins, such as neomangiferin, mangiferin, timosaponin BII, timosaponin BIII, and timosaponin AIII, which showed various biological activities. Objective: The main objective of the study is to establish an ultra-high-performance liquid chromatography-tandem mass spectrometry (MS/MS) method to determine the concentrations of five bioactive constituents in rats' plasma and various tissues. Materials and Methods: The analytes were separated on a C18reversed-phase column. A triple-quadrupole MS/MS equipped with an electrospray ionization source was used as a detector. The main pharmacokinetic parameters were estimated with Drug and Statistics 2.0 Software Package. Results: Neomangiferin and mangiferin exhibit poor oral absorption and slow clearance from the body. Timosaponin BII and timosaponin BIII could be quickly absorbed into the blood circulation and showed double plasma concentration peaks. Timosaponin AIII exhibited a single peak in the plasma concentration-time plot and pharmacokinetic parameters of timosaponin AIII indicated slower absorption, longer body residence time, and slower elimination than timosaponin BII and timosaponin BIII. The five analytes were widely distributed to most of the tissues. Neomangiferin and mangiferin exhibited the maximum concentration in the lung at 6 h after oral administration, the highest levels of timosaponin BII and timosaponin BIII were also observed in the lung at 1 h after oral administration, and the maximum concentration of timosaponin AIII was observed in the liver. Conclusion: The findings of the present study might be helpful to better understand the pharmacokinetics and distribution of AR bioactive constituents in vivo, which would facilitate the clinical application of AR. Keywords:Anemarrhenae rhizoma, herbal medicine, pharmacokinetics, tissue distribution, Traditional Chinese medicine, ultra-high-performance liquid chromatography-tandem mass spectrometryView:PDF (1.95 MB)