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 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.
Medienart: |
E-Artikel |
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Erscheinungsjahr: |
2014 |
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Erschienen: |
2014 |
Enthalten in: |
Zur Gesamtaufnahme - volume:9 |
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Enthalten in: |
PloS one - 9(2014), 9 vom: 28., Seite e108000 |
Sprache: |
Englisch |
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Beteiligte Personen: |
Zhao, Shuang [VerfasserIn] |
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Links: |
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Themen: |
600-76-0 |
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Anmerkungen: |
Date Completed 10.06.2015 Date Revised 21.10.2021 published: Electronic-eCollection Citation Status MEDLINE |
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doi: |
10.1371/journal.pone.0108000 |
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funding: |
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Förderinstitution / Projekttitel: |
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PPN (Katalog-ID): |
NLM242409792 |
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520 | |a 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 | ||
650 | 4 | |a Journal Article | |
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700 | 1 | |a Wang, Xin-Pei |e verfasserin |4 aut | |
700 | 1 | |a Jiang, Jing-Fei |e verfasserin |4 aut | |
700 | 1 | |a Chai, Yu-Shuang |e verfasserin |4 aut | |
700 | 1 | |a Tian, Yu |e verfasserin |4 aut | |
700 | 1 | |a Feng, Tian-Shi |e verfasserin |4 aut | |
700 | 1 | |a Ding, Yi |e verfasserin |4 aut | |
700 | 1 | |a Huang, Jing |e verfasserin |4 aut | |
700 | 1 | |a Lei, Fan |e verfasserin |4 aut | |
700 | 1 | |a Xing, Dong-Ming |e verfasserin |4 aut | |
700 | 1 | |a Du, Li-Jun |e verfasserin |4 aut | |
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