Potent anti-inflammatory activity of novel microtubule-modulating brominated noscapine analogs.

Noscapine, a plant-derived, non-toxic, over-the-counter antitussive alkaloid has tubulin-binding properties. Based upon the structural resemblance of noscapine to colchicine, a tubulin-binding anti-inflammatory drug, noscapine and its semi-synthetic brominated analogs were examined for in vitro anti...

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Main Authors: Susu Zughaier, Prasanthi Karna, David Stephens, Ritu Aneja
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2010-02-01
Series:PLoS ONE
Online Access:https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0009165&type=printable
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author Susu Zughaier
Prasanthi Karna
David Stephens
Ritu Aneja
author_facet Susu Zughaier
Prasanthi Karna
David Stephens
Ritu Aneja
author_sort Susu Zughaier
collection DOAJ
description Noscapine, a plant-derived, non-toxic, over-the-counter antitussive alkaloid has tubulin-binding properties. Based upon the structural resemblance of noscapine to colchicine, a tubulin-binding anti-inflammatory drug, noscapine and its semi-synthetic brominated analogs were examined for in vitro anti-inflammatory activity. Brominated noscapine analogs were found to inhibit cytokine and chemokine release from macrophage cell lines but did not affect cell viability. Brominated noscapine analogs demonstrated anti-inflammatory properties in both TLR- and non-TLR induced in vitro innate immune pathway inflammation models, mimicking septic and sterile infection respectively. In addition, electron microscopy and immunoblotting data indicated that these analogs induced robust autophagy in human macrophages. This study is the first report to identify brominated noscapines as innate immune pathway anti-inflammatory molecules.
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institution DOAJ
issn 1932-6203
language English
publishDate 2010-02-01
publisher Public Library of Science (PLoS)
record_format Article
series PLoS ONE
spelling doaj-art-aca0d125eae24b1abd1d1916afb3af6d2025-08-20T03:07:40ZengPublic Library of Science (PLoS)PLoS ONE1932-62032010-02-0152e916510.1371/journal.pone.0009165Potent anti-inflammatory activity of novel microtubule-modulating brominated noscapine analogs.Susu ZughaierPrasanthi KarnaDavid StephensRitu AnejaNoscapine, a plant-derived, non-toxic, over-the-counter antitussive alkaloid has tubulin-binding properties. Based upon the structural resemblance of noscapine to colchicine, a tubulin-binding anti-inflammatory drug, noscapine and its semi-synthetic brominated analogs were examined for in vitro anti-inflammatory activity. Brominated noscapine analogs were found to inhibit cytokine and chemokine release from macrophage cell lines but did not affect cell viability. Brominated noscapine analogs demonstrated anti-inflammatory properties in both TLR- and non-TLR induced in vitro innate immune pathway inflammation models, mimicking septic and sterile infection respectively. In addition, electron microscopy and immunoblotting data indicated that these analogs induced robust autophagy in human macrophages. This study is the first report to identify brominated noscapines as innate immune pathway anti-inflammatory molecules.https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0009165&type=printable
spellingShingle Susu Zughaier
Prasanthi Karna
David Stephens
Ritu Aneja
Potent anti-inflammatory activity of novel microtubule-modulating brominated noscapine analogs.
PLoS ONE
title Potent anti-inflammatory activity of novel microtubule-modulating brominated noscapine analogs.
title_full Potent anti-inflammatory activity of novel microtubule-modulating brominated noscapine analogs.
title_fullStr Potent anti-inflammatory activity of novel microtubule-modulating brominated noscapine analogs.
title_full_unstemmed Potent anti-inflammatory activity of novel microtubule-modulating brominated noscapine analogs.
title_short Potent anti-inflammatory activity of novel microtubule-modulating brominated noscapine analogs.
title_sort potent anti inflammatory activity of novel microtubule modulating brominated noscapine analogs
url https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0009165&type=printable
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AT prasanthikarna potentantiinflammatoryactivityofnovelmicrotubulemodulatingbrominatednoscapineanalogs
AT davidstephens potentantiinflammatoryactivityofnovelmicrotubulemodulatingbrominatednoscapineanalogs
AT rituaneja potentantiinflammatoryactivityofnovelmicrotubulemodulatingbrominatednoscapineanalogs