【摘 要】
：
Herein,the purpose of this study is to evaluate the effects of kaempferol on bioavailability and pharmacokinetics of nifedipine and its metabolite dehydronifedipine in rats.The experimental design is based on with or without kaempferol in the oral and int
【机 构】
：
Hazardous Substances Analysis Division, Gwangju Regional Office of Food and Drug Safety, Gwangju 610
论文部分内容阅读
Herein,the purpose of this study is to evaluate the effects of kaempferol on bioavailability and pharmacokinetics of nifedipine and its metabolite dehydronifedipine in rats.The experimental design is based on with or without kaempferol in the oral and intravenous administration of nifedipine in rats.Moreover,the pharmacokinetic parameters including nifedipine and dehydronifedipine were evaluated in rats.The in vitro studies of kaempferol were investigated on P-glycoprotein (P-gp) and cytochrome P450 (CYP) 3A4 activity.Kaempferol reduced a 50％ inhibitory concentration (IC50) of 8.6 μmol·L-1 on CYP3A4 enzyme activity.Moreover,kaempferol clearly improved the cell internalization of rhodamine-123 in MCF-7/ADR cells overexpressing P-gp.Depending on increased concentrations of kaempferol,the areas under the plasma concentration-time curve (A UCo-∞) and the peak concentration (Cmax)of nifedipine were increased after oral and intravenous administration.Moreover,the absolute bioavailability (AB) and relative bioavailability (RB) of nifedipine in the presence of kaempferol was significantly higher than those of the control group after oral and intravenous administration.Improvement of bioavailability of nifedipine by kaempferol may be mainly because of the inhibition of the P-gp-mediated effiux transporter in the small intestine and CYP3A4-mediated metabolism in the small intestine or liver,or both.
其他文献
Shuang-huang-lian Injection (SHLI) is the first successfully developed drug from traditional Chinese medicine (TCM) powder for injection, since its use for the treatment of acute respiratory tract infection, pneumonia, influenza, etc. At the same time, it
Angiogenesis is a crucial process in the development of inflammatory diseases, including cancer, psoriasis and rheumatoid arthritis. Recently, several alkaloids from Picrasma quassioides had been screened for angiogenic activity in the zebrafish model, an
Cancerous inhibitor of protein phosphatase 2A (CIP2A) is a human oncoprotein that is overexpressed in multiple kinds of cancers including non-small cell lung cancer (NSCLC).CIP2A plays an\'oncogenic nexus\' to participate in the tumorigenesis and chem
Diabetic nephropathy (DN) is one of the common microvascular complications of diabetes mellitus.Renal fibrosis is closely related to the deterioration of renal function.The present study aimed to investigate protective effect of Taxus chinensis on high-fa
In the present study,a gastric retention floating system for Bruceajavanica oil,composed of alginate and carrageenan,was prepared using ionotropic gelation.Parameters for floatability,drug load,encapsulation efficiency,bead morphology,in vitro release,and
In the present study,two new acetylene conjugate compounds,dibutyl (2Z,6Z)-octa-2,6-dien-4-yne dioate (1),and dibutyl (2E,6E)-octa-2,6-dien-4-yne dioate (2),were isolated from the dry stem leaves of Viscum album,along with nine known compounds (3-11).Thei
Pharmacological activities and adverse side effects of ginkgolic acids (GAs),major components in extracts from the leaves and seed coats of Ginkgo biloba L,have been intensively studied.However,there are few reports on their hepatotoxicity.In the present
According to folk usage ofAconitum carmichaelii Debx.,the present study was designed to determine the feasibility of the stems and leaves of Aconitum carmichaelii Debx.as a new medicinal resource.Fourteen alkaloids in mother roots,fibrous roots,stems,and
Seven new isoquinoline alkaloids,9-(2\'-formyl-5\',6\'-dimethoxyphenoxy)-1,2,3,10-tetramethoxy dehydroaporphine (1),9-(2\'-formyl-5\',6\'-dimethoxyphenoxy)-1,2,3,10-tetramethoxy oxoaporphine (2),3-methoxy-2\'-formyl oxohemandalin (3),(-)-9-(
In the present study,three new aconitine-type diterpenoid alkaloids brochyponines A-C (1-3) were isolated from the roots of Aconitum brevicalcaratum.Their structures were established on the basis of extensive spectroscopic analyses (IR,HR-ESI-MS,and lD an