Transport and metabolism behavior of brazilein during its entrance into neural cells

Brazilein, a natural small molecule, shows a variety of pharmacological activities, especially on nervous system and immune system. As a potential multifunctional drug, we studied the distribution and the transport behavior and metabolic behavior of brazilein in vivo and in vitro. Brazilein was foun...

Full description

Saved in:
Bibliographic Details
Published in:PloS one 2014-10, Vol.9 (9), p.e108000-e108000
Main Authors: Zhao, Shuang, Wang, Xin-Pei, Jiang, Jing-Fei, Chai, Yu-Shuang, Tian, Yu, Feng, Tian-Shi, Ding, Yi, Huang, Jing, Lei, Fan, Xing, Dong-Ming, Du, Li-Jun
Format: Article
Language:English
Subjects:
Animals
Apoptosis
Behavior
Benzopyrans - administration & dosage
Benzopyrans - chemistry
Benzopyrans - metabolism
Benzopyrans - pharmacology
Biochemistry
Biological Transport - drug effects
Biology and Life Sciences
Brain
Brain - metabolism
Brain research
Catechol
Catechol O-methyltransferase
Catechol O-Methyltransferase - chemistry
Catechol O-Methyltransferase - metabolism
Cell Death - drug effects
Chromatography, High Pressure Liquid
Crystal structure
Cytokines
Drug dosages
Electron Transport Complex IV - antagonists & inhibitors
Electron Transport Complex IV - metabolism
Enzymes
Experiments
Immune system
Indenes - administration & dosage
Indenes - chemistry
Indenes - metabolism
Indenes - pharmacology
Laboratory animals
Life sciences
Male
Medical research
Medicine
Medicine and Health Sciences
Metabolism
Metabolites
Methylated metabolites
Methylation
Methylation - drug effects
Methyltransferase
Mice, Inbred ICR
Molecular docking
Nervous system
Neurons - drug effects
Neurons - metabolism
PC12 Cells
Pharmaceutical sciences
Pharmacology
Physical Sciences
Plasma
Proteins
R&D
Rats
Reproducibility of Results
Research & development
Research and Analysis Methods
Tandem Mass Spectrometry
Temperature
Transport
Ultraviolet Rays
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Brazilein, a natural small molecule, shows a variety of pharmacological activities, especially on nervous system and immune system. As a potential multifunctional drug, we studied the distribution and the transport behavior and metabolic behavior of brazilein in vivo and in vitro. Brazilein was found to be able to distribute in the mouse brain and transport into neural cells. A metabolite was found in the brain and in the cells. Positive and negative mode-MS/MS and Q-TOF were used to identify the metabolite. MS/MS fragmentation mechanisms showed the methylation occurred at the 10-hydroxyl of brazilein (10-O-methylbrazilein). Further, catechol-O- methyltransferase (COMT) was confirmed as a crucial enzyme correlated with the methylated metabolite generation by molecular docking and pharmacological experiment.
ISSN:1932-6203
1932-6203
DOI:10.1371/journal.pone.0108000