2. Academic Validation
  3. Simultaneous determination of columbianetin-β-d-glucopyranoside and columbianetin in a biological sample by high-performance liquid chromatography with fluorescence detection and identification of other columbianetin-β-d-glucopyranoside metabolites by ultra high-performance liquid chromatography coupled with quadrupole-time of flight mass spectrometry

Simultaneous determination of columbianetin-β-d-glucopyranoside and columbianetin in a biological sample by high-performance liquid chromatography with fluorescence detection and identification of other columbianetin-β-d-glucopyranoside metabolites by ultra high-performance liquid chromatography coupled with quadrupole-time of flight mass spectrometry

  • J Pharm Biomed Anal. 2018 May 10:153:221-231. doi: 10.1016/j.jpba.2018.02.055.
Lu Zhang 1,  Yuanyuan Ge 1,  Jin Li 2,  Jia Hao 3,  Hui Wang 3,  Jun He 3,  Xiu-Mei Gao 4,  Yan-Xu Chang 5
Affiliations

Affiliations

  • 1 Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China.
  • 2 Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China; Key Laboratory of Formula of Traditional Chinese Medicine (Tianjin University of Traditional Chinese Medicine), Ministry of Education, Tianjin, 300193, China.
  • 3 Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China; Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China.
  • 4 Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China; Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China; Key Laboratory of Formula of Traditional Chinese Medicine (Tianjin University of Traditional Chinese Medicine), Ministry of Education, Tianjin, 300193, China.
  • 5 Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China; Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China; Key Laboratory of Formula of Traditional Chinese Medicine (Tianjin University of Traditional Chinese Medicine), Ministry of Education, Tianjin, 300193, China. Electronic address: [email protected].
PMID: 29506005 DOI: 10.1016/j.jpba.2018.02.055
Abstract

Columbianetin-β-d-glucopyranoside (CBG) and its metabolite columbianetin (CBN) are the bioactive constituents of Angelicae pubescentis radix (APR). They exhibit the anti-platelet aggregation, anti-inflammatory and analgesic properties. The absorption, distribution, metabolism and excretion (ADME) of CBG has not been reported to date. Both high-performance liquid chromatography with fluorescence detection and ultra high-performance liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry methods were developed and validated for the study of ADME of CBG. It was found that CBG could be catabolized into its active metabolite CBN in vivo. The absolute bioavailability of columbianetin-β-d-glucopyranoside was 5.63 ± 4.42%. The other co-existing constituents from the APR ethanol extract could enhance the absorption of CBG. CBG and CBN were rapidly and broadly distributed in the stomach, ovary, kidney, liver, spleen, lung, muscles, heart and brain. Higher levels of accumulation of CBG and CBN were detected in the ovary and kidney tissues. Eight metabolites of CBG were tentatively identified in blood, urine, bile and faeces of rats after oral administration of pure CBG. It was also found that CBG and CBN were mainly excreted through the faecal route. It can be concluded that the validated methods were successfully applied for absorption, distribution, metabolism and excretion study of CBG.

Keywords

ADME; Angelicae pubescentis radix; Columbianetin; Columbianetin-β-d-glucopyranoside; HPLC-FLD; UPLC-Q-TOF.

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