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
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 p...
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2020-01-01
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| Series: | Pharmaceutical Biology |
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| Online Access: | http://dx.doi.org/10.1080/13880209.2020.1818790 |
| _version_ | 1818670247742275584 |
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| author | Xin Zhao Baoxin Xu Peng Wu Pan Zhao Changchuan Guo Yueli Cui Yanxue Zhang Xuelan Zhang Huifen Li |
| author_facet | Xin Zhao Baoxin Xu Peng Wu Pan Zhao Changchuan Guo Yueli Cui Yanxue Zhang Xuelan Zhang Huifen Li |
| author_sort | Xin Zhao |
| collection | DOAJ |
| description | 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. AUC0-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. |
| first_indexed | 2024-12-17T07:05:05Z |
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| institution | Directory Open Access Journal |
| issn | 1388-0209 1744-5116 |
| language | English |
| last_indexed | 2024-12-17T07:05:05Z |
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| spelling | doaj.art-e4dd361327274d5b83ef439b3da217e92022-12-21T21:59:13ZengTaylor & Francis GroupPharmaceutical Biology1388-02091744-51162020-01-0158196997810.1080/13880209.2020.18187901818790UHPLC-MS/MS method for pharmacokinetic and bioavailability determination of five bioactive components in raw and various processed products of Polygala tenuifolia in rat plasmaXin Zhao0Baoxin Xu1Peng Wu2Pan Zhao3Changchuan Guo4Yueli Cui5Yanxue Zhang6Xuelan Zhang7Huifen Li8School of Chinese Pharmacy, Shandong University of Traditional Chinese MedicineSchool of Chinese Pharmacy, Shandong University of Traditional Chinese MedicineSchool of Chinese Pharmacy, Shandong University of Traditional Chinese MedicineSchool of Chinese Pharmacy, Shandong University of Traditional Chinese MedicineShandong Institute for Food and Drug ControlSchool of Chinese Pharmacy, Shandong University of Traditional Chinese MedicineSchool of Chinese Pharmacy, Shandong University of Traditional Chinese MedicineSchool of Chinese Pharmacy, Shandong University of Traditional Chinese MedicineSchool of Chinese Pharmacy, Shandong University of Traditional Chinese MedicineContext 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. AUC0-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.http://dx.doi.org/10.1080/13880209.2020.1818790liquorice boilinghoney stir-bakingsibiricose a5sibiricose a63,6′-disinapoyl sucrosetenuifoliside a3,4,5-trimethoxycinnamic acid |
| spellingShingle | Xin Zhao Baoxin Xu Peng Wu Pan Zhao Changchuan Guo Yueli Cui Yanxue Zhang Xuelan Zhang Huifen Li 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 Pharmaceutical Biology liquorice boiling honey stir-baking sibiricose a5 sibiricose a6 3,6′-disinapoyl sucrose tenuifoliside a 3,4,5-trimethoxycinnamic acid |
| title | 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 |
| title_full | 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 |
| title_fullStr | 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 |
| title_full_unstemmed | 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 |
| title_short | 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 |
| title_sort | 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 |
| topic | liquorice boiling honey stir-baking sibiricose a5 sibiricose a6 3,6′-disinapoyl sucrose tenuifoliside a 3,4,5-trimethoxycinnamic acid |
| url | http://dx.doi.org/10.1080/13880209.2020.1818790 |
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