NDLI: Indirubin-3′-(2,3 dihydroxypropyl)-oximether (E804) is a Potent Modulator of LPS-Stimulated Macrophage Functions

Content Provider	PubMed Central
Author	Babcock, Abigail S. Anderson, Amy E. Rice, Charles D.
Copyright Year	2012
Abstract	Indirubin is a deep-red bis-indole isomer of indigo blue, both of which are biologically active ingredients in Danggui Longhui Wan, an ancient Chinese herbal tea mixture used to treat neoplasia and chronic inflammation and to enhance detoxification of xenobiotics. Multiple indirubin derivatives have been synthesized and shown to inhibit cyclin-dependent kinases (CDKs) and glycogen-synthase kinase (GSK-3β) with varying degrees of potency. Several indirubins are also aryl hydrocarbon receptor (AhR) agonists, with AhR-associated activities covering a wide range of potencies, depending on molecular structure. This study examined the effects of indirubin-3′-(2,3 dihydroxypropyl)-oximether (E804), a novel indirubin with potent STAT3 inhibitory properties, on basal and LPS-inducible activities in murine RAW264.7 macrophages. Using a focused commercial qRT-PCR array platform (SuperArray®), the effects of E804 on expression of a suite of genes associated with stress & toxicity were determined. Most genes up-regulated by LPS treatment were suppressed by E804; including LPS-induced expression of pro-inflammatory cytokines and receptors, apoptosis control genes, and oxidative stress response genes. Using qRT-PCR as a follow up to the commercial arrays, E804 treatment suppressed LPS-induced COX-2, iNOS, IL-6 and IL-10 gene expression, though the effects on iNOS and COX-2 protein expression were less dramatic. E804 also inhibited LPS-induced secretion of IL-6 and IL-10. Functional endpoints, including iNOS and lysozyme enzymatic activity, phagocytosis of fluorescent latex beads, and intracellular killing of bacteria, were also examined, and in each experimental condition E804 suppressed activities. Collectively, these results indicate that E804 is a potent modulator of pro-inflammatory profiles in LPS-treated macrophages.
Related Links	http://dx.doi.org/10.1016/j.taap.2012.10.011
Ending Page	166
Page Count	10
Starting Page	157
File Format	PDF
ISSN	0041008X
e-ISSN	10960333
Journal	Toxicology and applied pharmacology
Issue Number	1
Volume Number	266
Language	English
Publisher Date	2013-01-01
Access Restriction	Open
Subject Keyword	Toxicology Pharmacology Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Toxicology Pharmacology

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in

Indirubin derivative E804 inhibits angiogenesis

A tea catechin, epigallocatechin-3-gallate, is a unique modulator of the farnesoid X receptor

Indirubin derivative E804 inhibits angiogenesis

LPS-Stimulated RAW 264.7 Macrophage Inducible Nitric Oxide Synthase (iNOS) and Nitric Oxide Production is Decreased by an Omega-3 Fatty Acid Lipid Emulsion

Indirubin-3-monoxime exhibits anti-inflammatory properties by down-regulating NF-κB and JNK signaling pathways in lipopolysaccharide-treated RAW264.7 cells

Asymmetric synthesis of novel N-(1-phenyl-2,3-dihydroxypropyl)arachidonylamides and evaluation of their anti-inflammatory activity

Macrophage-derived neutrophil chemotactic factor is involved in the neutrophil recruitment inhibitory activity present in the supernatants of LPS-stimulated macrophages

GG167 (4-guanidino-2,4-dideoxy-2,3-dehydro-N-acetylneuraminic acid) is a potent inhibitor of influenza virus in ferrets.

Quantum chemical calculation of the (S)-9-(2,3-dihydroxypropyl)adenine molecule.

Indirubin-3′-(2,3 dihydroxypropyl)-oximether (E804) is a Potent Modulator of LPS-Stimulated Macrophage Functions

Similar Documents

Indirubin derivative E804 inhibits angiogenesis

A tea catechin, epigallocatechin-3-gallate, is a unique modulator of the farnesoid X receptor

Indirubin derivative E804 inhibits angiogenesis

LPS-Stimulated RAW 264.7 Macrophage Inducible Nitric Oxide Synthase (iNOS) and Nitric Oxide Production is Decreased by an Omega-3 Fatty Acid Lipid Emulsion

Indirubin-3-monoxime exhibits anti-inflammatory properties by down-regulating NF-κB and JNK signaling pathways in lipopolysaccharide-treated RAW264.7 cells

Asymmetric synthesis of novel N-(1-phenyl-2,3-dihydroxypropyl)arachidonylamides and evaluation of their anti-inflammatory activity

Macrophage-derived neutrophil chemotactic factor is involved in the neutrophil recruitment inhibitory activity present in the supernatants of LPS-stimulated macrophages

GG167 (4-guanidino-2,4-dideoxy-2,3-dehydro-N-acetylneuraminic acid) is a potent inhibitor of influenza virus in ferrets.

Quantum chemical calculation of the (S)-9-(2,3-dihydroxypropyl)adenine molecule.

Indirubin-3′-(2,3 dihydroxypropyl)-oximether (E804) is a Potent Modulator of LPS-Stimulated Macrophage Functions