Journal
FRONTIERS IN PHARMACOLOGY
Volume 8, Issue -, Pages -Publisher
FRONTIERS MEDIA SA
DOI: 10.3389/fphar.2017.00376
Keywords
arctigenin; pharmacokinetics; UPLC/MS/MS; bioavailability; microsomes
Categories
Funding
- Shandong Province Science and Technology Major Project [2015ZDJQ05004]
- National Science and Technology Support Program [2012CB724001]
- Generic Manufacture Technology of Chinese Traditional Medicine
- Lunan Pharmaceutical Group Co., Ltd.
Ask authors/readers for more resources
Although arctigenin (AG) has diverse bioactivities, such as anti-oxidant, antiinflammatory, anti-cancer, immunoregulatory and neuroprotective activities, its pharmacokinetics have not been systematically evaluated. The purpose of this work was to identify the pharmacokinetic properties of AG via various experiments in vivo and in vitro. In this research, rats and beagle dogs were used to investigate the PK (pharmacokinetics, PK) profiles of AG with different drug-delivery manners, including intravenous (i.v), hypodermic injection (i.h),and sublingual (s.l) administration. The data shows that AG exhibited a strong absorption capacity in both rats and beagle dogs (absorption rate < 1 h), a high absorption degree (absolute bioavailability > 100%), and a strong elimination ability (t(1/2) < 2 h). The tissue distributions of AG at different time points after i. h showed that the distribution of AG in rat tissues is rapid (2.5 h to reach the peak) and wide (detectable in almost all tissues and organs). The AG concentration in the intestine was the highest, followed by that in the heart, liver, pancreas, and kidney. In vitro, AG were incubated with human, monkey, beagle dog and rat liver microsomes. The concentrations of AG were detected by UPLC-MS/MS at different time points (from 0 min to 90 min). The percentages of AG remaining in four species' liver microsomes were human (62 +/- 6.36%) > beagle dog (25.9 +/- 3.24%) > rat (15.7 +/- 9%) > monkey (3.69 +/- 0.12%). This systematic investigation of pharmacokinetic profiles of arctigenin (AG) in vivo and in vitro is worthy of further exploration.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available