The indirubin derivative 6-bromoindirubin-3'-glycerol-oxime ether (6BIGOE) potently modulates inflammatory cytokine and prostaglandin release from human monocytes through GSK-3 interference.
Adolescent
Adult
Aged
Animals
Chickens
Cytokines
/ antagonists & inhibitors
Dose-Response Relationship, Drug
Female
Glycogen Synthase Kinase 3
/ antagonists & inhibitors
Humans
Indoles
/ pharmacology
Inflammation Mediators
/ antagonists & inhibitors
Male
Middle Aged
Monocytes
/ drug effects
Oximes
/ pharmacology
Prostaglandin Antagonists
/ pharmacology
Prostaglandins
/ metabolism
Young Adult
Cytokine
Glycogen synthase kinase-3
Indirubin
Inflammation
Lipid mediator
Journal
Biochemical pharmacology
ISSN: 1873-2968
Titre abrégé: Biochem Pharmacol
Pays: England
ID NLM: 0101032
Informations de publication
Date de publication:
10 2020
10 2020
Historique:
received:
15
06
2020
revised:
20
07
2020
accepted:
20
07
2020
pubmed:
28
7
2020
medline:
1
1
2021
entrez:
26
7
2020
Statut:
ppublish
Résumé
Indirubin is a natural bis-indole alkaloid contained as active ingredient in the traditional Chinese remedy Danggui Longhui Wan. Indirubin and its 3'-oxime derivatives exhibit anti-cancer and anti-inflammatory properties and they inhibit glycogen synthase kinase (GSK)-3 in cell-free assays where 6-bromoindirubin-3'-oxime (6BIO) is among the most potent analogs. Here, we reveal 6-bromoindirubin-3'-glycerol-oxime ether (6BIGOE) as highly potent derivative able to inhibit pro-inflammatory cytokine, chemokine and prostaglandin (PG) release in human primary monocytes while increasing anti-inflammatory interleukin (IL)-10 levels. 6BIGOE suppressed lipopolysaccharide (LPS)-induced IL-1β and PGE
Identifiants
pubmed: 32710971
pii: S0006-2952(20)30406-8
doi: 10.1016/j.bcp.2020.114170
pii:
doi:
Substances chimiques
6-bromoindirubin-3'-oxime
0
Cytokines
0
Indoles
0
Inflammation Mediators
0
Oximes
0
Prostaglandin Antagonists
0
Prostaglandins
0
Glycogen Synthase Kinase 3
EC 2.7.11.26
indirubin
V86L8P74GI
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
114170Informations de copyright
Copyright © 2020 Elsevier Inc. All rights reserved.