UHPLC-MS/MS method for pharmacokinetic and bioavailability determination of five bioactive components in raw and various processed products of Polygala tenuifolia in rat plasma. (1st January 2020)

• Record Type: Journal Article
• Authors: Zhao, Xin; Xu, Baoxin; Wu, Peng; Zhao, Pan; Guo, Changchuan; Cui, Yueli; Zhang, Yanxue; Zhang, Xuelan; Li, Huifen
• Is Part Of: Pharmaceutical biology. Volume 58:Number 1(2020)
• Page Start: 969
• Page End: 978
• Publication Date: 2020-01-01
• Subjects: Liquorice boiling -- honey stir-baking -- sibiricose A5 -- sibiricose A6 -- 3, 6′-disinapoyl sucrose -- tenuifoliside A -- 3, 4, 5-trimethoxycinnamic acid; Pharmacognosy -- Periodicals; Materia medica, Vegetable -- Periodicals; 615.321
• DOI: 10.1080/13880209.2020.1818790
• Languages: English
• ISSNs: 1388-0209

Abstract

Abstract: Context: Sibiricose A5 (A5), sibiricose A6 (A6), 3, 6′-disinapoyl sucrose (DSS), tenuifoliside A (TFSA) and 3, 4, 5-trimethoxycinnamic acid (TMCA) are the main active components of Polygala tenuifolia Willd. (Polygalaceae) (PT) that are active against Alzheimer's disease. Objective: To compare the pharmacokinetics and bioavailability of five active components in the roots of raw PT (RPT), liquorice-boiled PT (LPT) and honey-stir-baked PT (HPT). Materials and methods: The median lethal dose (LD50 ) was evaluated through acute toxicity test. The pharmacokinetics of five components after oral administration of extracts of RPT, LPT, HPT (all equivalent to 1.9 g/kg of RPT extract for one dose) and 0.5% CMC-Na solution (control group) were investigated, respectively, in Sprague-Dawley rats (four groups, n = 6) using UHPLC-MS/MS. In addition, the absolute bioavailability of A5, A6, DSS, TFSA and TMCA after oral administration (7.40, 11.60, 16.00, 50.00 and 3.11 mg/kg, respectively) and intravenous injection (1/10 of the corresponding oral dose) in rats ( n = 6) was studied. Results: The LD50 of RPT, LPT and HPT was 7.79, 14.55 and 15.99 g/kg, respectively. AUC 0- t of RPT, LPT and HPT were as follows: A5 (433.18 ± 65.48, 680.40 ± 89.21, 552.02 ± 31.10 ng h/mL), A6 (314.55 ± 62.73, 545.76 ± 123.16, 570.06 ± 178.93 ng h/mL) and DSS (100.30 ± 62.44, 232.00 ± 66.08, 197.58 ± 57.37 ng h/mL). The absolute bioavailability of A5, A6, DSS, TFSA and TMCA was 3.25, 2.95, 2.36, 1.17 and 42.91%, respectively. Discussion and conclusions: The pharmacokinetic and bioavailability parameters of each compound can facilitate future clinical studies.