Pharmacokinetics, bioavailability, tissue distribution and excretion of tangeretin in rat
Tangeretin, 4′,5,6,7,8-pentamethoxyflavone, is one of the major polymethoxyflavones (PMFs) existing in citrus fruits, particularly in the peels of sweet oranges and mandarins. Tangeretin has been reported to possess several beneficial bioactivities including anti-inflammatory, anti-proliferative and...
Main Authors: | , , , , , , |
---|---|
Format: | Article |
Language: | English |
Published: |
Elsevier
2018-04-01
|
Series: | Journal of Food and Drug Analysis |
Online Access: | http://www.sciencedirect.com/science/article/pii/S1021949817301588 |
id |
doaj-96e0ae97000f4d9dac7b5a2b6e0c347b |
---|---|
record_format |
Article |
spelling |
doaj-96e0ae97000f4d9dac7b5a2b6e0c347b2020-11-24T23:32:24ZengElsevierJournal of Food and Drug Analysis1021-94982018-04-01262849857Pharmacokinetics, bioavailability, tissue distribution and excretion of tangeretin in ratWei-Lun Hung0Wei-Shan Chang1Wen-Chien Lu2Guor-Jien Wei3Yu Wang4Chi-Tang Ho5Lucy Sun Hwang6Citrus Research and Education Center, Department of Food Science and Human Nutrition, University of Florida, Lake Alfred, FL 33850, USAGraduate Institute of Food Science and Technology, National Taiwan University, No. 1, Section 4, Roosevelt Rd., Taipei 10617, TaiwanDepartment of Food and Beverage Management, Chung-Jen Junior College of Nursing, Health Sciences and Management, Chiayi 60077, TaiwanDepartment of Nutrition and Health Sciences, Kainan University, Taoyuan 33857, TaiwanCitrus Research and Education Center, Department of Food Science and Human Nutrition, University of Florida, Lake Alfred, FL 33850, USADepartment of Food Science, Rutgers University, 65 Dudley Rd., New Brunswick, NJ 08901, USAGraduate Institute of Food Science and Technology, National Taiwan University, No. 1, Section 4, Roosevelt Rd., Taipei 10617, Taiwan; Corresponding author. Fax: +886 2 33664113.Tangeretin, 4′,5,6,7,8-pentamethoxyflavone, is one of the major polymethoxyflavones (PMFs) existing in citrus fruits, particularly in the peels of sweet oranges and mandarins. Tangeretin has been reported to possess several beneficial bioactivities including anti-inflammatory, anti-proliferative and neuroprotective effects. To achieve a thorough understanding of the biological actions of tangeretin in vivo, our current study is designed to investigate the pharmacokinetics, bioavailability, distribution and excretion of tangeretin in rats. After oral administration of 50 mg/kg bw tangeretin to rats, the Cmax, Tmax and t1/2 were 0.87 ± 0.33 μg/mL, 340.00 ± 48.99 min and 342.43 ± 71.27 min, respectively. Based on the area under the curves (AUC) of oral and intravenous administration of tangeretin, calculated absolute oral bioavailability was 27.11%. During tissue distribution, maximum concentrations of tangeretin in the vital organs occurred at 4 or 8 h after oral administration. The highest accumulation of tangeretin was found in the kidney, lung and liver, followed by spleen and heart. In the gastrointestinal tract, maximum concentrations of tangeretin in the stomach and small intestine were found at 4 h, while in the cecum, colon and rectum, tangeretin reached the maximum concentrations at 12 h. Tangeretin excreted in the urine and feces was recovered within 48 h after oral administration, concentrations were only 0.0026% and 7.54%, respectively. These results suggest that tangeretin was mainly eliminated as metabolites. In conclusion, our study provides useful information regarding absorption, distribution, as well as excretion of tangeretin, which will provide a good base for studying the mechanism of its biological effects. Keywords: Tangeretin, Oral bioavailability, Pharmacokinetics, Tissue distribution, Excretionhttp://www.sciencedirect.com/science/article/pii/S1021949817301588 |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Wei-Lun Hung Wei-Shan Chang Wen-Chien Lu Guor-Jien Wei Yu Wang Chi-Tang Ho Lucy Sun Hwang |
spellingShingle |
Wei-Lun Hung Wei-Shan Chang Wen-Chien Lu Guor-Jien Wei Yu Wang Chi-Tang Ho Lucy Sun Hwang Pharmacokinetics, bioavailability, tissue distribution and excretion of tangeretin in rat Journal of Food and Drug Analysis |
author_facet |
Wei-Lun Hung Wei-Shan Chang Wen-Chien Lu Guor-Jien Wei Yu Wang Chi-Tang Ho Lucy Sun Hwang |
author_sort |
Wei-Lun Hung |
title |
Pharmacokinetics, bioavailability, tissue distribution and excretion of tangeretin in rat |
title_short |
Pharmacokinetics, bioavailability, tissue distribution and excretion of tangeretin in rat |
title_full |
Pharmacokinetics, bioavailability, tissue distribution and excretion of tangeretin in rat |
title_fullStr |
Pharmacokinetics, bioavailability, tissue distribution and excretion of tangeretin in rat |
title_full_unstemmed |
Pharmacokinetics, bioavailability, tissue distribution and excretion of tangeretin in rat |
title_sort |
pharmacokinetics, bioavailability, tissue distribution and excretion of tangeretin in rat |
publisher |
Elsevier |
series |
Journal of Food and Drug Analysis |
issn |
1021-9498 |
publishDate |
2018-04-01 |
description |
Tangeretin, 4′,5,6,7,8-pentamethoxyflavone, is one of the major polymethoxyflavones (PMFs) existing in citrus fruits, particularly in the peels of sweet oranges and mandarins. Tangeretin has been reported to possess several beneficial bioactivities including anti-inflammatory, anti-proliferative and neuroprotective effects. To achieve a thorough understanding of the biological actions of tangeretin in vivo, our current study is designed to investigate the pharmacokinetics, bioavailability, distribution and excretion of tangeretin in rats. After oral administration of 50 mg/kg bw tangeretin to rats, the Cmax, Tmax and t1/2 were 0.87 ± 0.33 μg/mL, 340.00 ± 48.99 min and 342.43 ± 71.27 min, respectively. Based on the area under the curves (AUC) of oral and intravenous administration of tangeretin, calculated absolute oral bioavailability was 27.11%. During tissue distribution, maximum concentrations of tangeretin in the vital organs occurred at 4 or 8 h after oral administration. The highest accumulation of tangeretin was found in the kidney, lung and liver, followed by spleen and heart. In the gastrointestinal tract, maximum concentrations of tangeretin in the stomach and small intestine were found at 4 h, while in the cecum, colon and rectum, tangeretin reached the maximum concentrations at 12 h. Tangeretin excreted in the urine and feces was recovered within 48 h after oral administration, concentrations were only 0.0026% and 7.54%, respectively. These results suggest that tangeretin was mainly eliminated as metabolites. In conclusion, our study provides useful information regarding absorption, distribution, as well as excretion of tangeretin, which will provide a good base for studying the mechanism of its biological effects. Keywords: Tangeretin, Oral bioavailability, Pharmacokinetics, Tissue distribution, Excretion |
url |
http://www.sciencedirect.com/science/article/pii/S1021949817301588 |
work_keys_str_mv |
AT weilunhung pharmacokineticsbioavailabilitytissuedistributionandexcretionoftangeretininrat AT weishanchang pharmacokineticsbioavailabilitytissuedistributionandexcretionoftangeretininrat AT wenchienlu pharmacokineticsbioavailabilitytissuedistributionandexcretionoftangeretininrat AT guorjienwei pharmacokineticsbioavailabilitytissuedistributionandexcretionoftangeretininrat AT yuwang pharmacokineticsbioavailabilitytissuedistributionandexcretionoftangeretininrat AT chitangho pharmacokineticsbioavailabilitytissuedistributionandexcretionoftangeretininrat AT lucysunhwang pharmacokineticsbioavailabilitytissuedistributionandexcretionoftangeretininrat |
_version_ |
1725534391963222016 |