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A novel natural product inspired scaffold with robust neurotrophic, neurogenic and neuroprotective action

In search for drugs to treat neuropsychiatric disorders wherein neurotrophic and neurogenic properties are affected, two neurotrophically active small molecules specially crafted following natural product leads based on 2-oxa-spiro[5.5]-undecane scaffold, have been thoroughly evaluated for their neu...

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Autores principales: Chakravarty, Sumana, Maitra, Swati, Reddy, R Gajendra, Das, Tapatee, Jhelum, Priya, Kootar, Scherazad, Rajan, Wenson D., Samanta, Anumita, Samineni, Ramesh, Pabbaraja, Srihari, Kernie, Steven G., Mehta, Goverdhan, Kumar, Arvind
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4585672/
https://www.ncbi.nlm.nih.gov/pubmed/26388493
http://dx.doi.org/10.1038/srep14134
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author Chakravarty, Sumana
Maitra, Swati
Reddy, R Gajendra
Das, Tapatee
Jhelum, Priya
Kootar, Scherazad
Rajan, Wenson D.
Samanta, Anumita
Samineni, Ramesh
Pabbaraja, Srihari
Kernie, Steven G.
Mehta, Goverdhan
Kumar, Arvind
author_facet Chakravarty, Sumana
Maitra, Swati
Reddy, R Gajendra
Das, Tapatee
Jhelum, Priya
Kootar, Scherazad
Rajan, Wenson D.
Samanta, Anumita
Samineni, Ramesh
Pabbaraja, Srihari
Kernie, Steven G.
Mehta, Goverdhan
Kumar, Arvind
author_sort Chakravarty, Sumana
collection PubMed
description In search for drugs to treat neuropsychiatric disorders wherein neurotrophic and neurogenic properties are affected, two neurotrophically active small molecules specially crafted following natural product leads based on 2-oxa-spiro[5.5]-undecane scaffold, have been thoroughly evaluated for their neurotrophic, neurogenic and neuroprotective potential in ex vivo primary culture and in vivo zebrafish and mouse models. The outcome of in vivo investigations suggest that one of these molecules is more neurotrophic than neurogenic while the other one is more neurogenic than neurotrophic and the former exhibits remarkable neuroprotection in a mouse acute ischemic stroke model. The molecular mechanisms of action of these compounds appear to be through the TrkB-MEK-ERK-CREB-BDNF pathway as pre-treatment with neurotrophin receptor TrkB inhibitor ANA-12 and MEK inhibitor PD98059 attenuates the neurotrophic action of compounds.
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spelling pubmed-45856722015-09-29 A novel natural product inspired scaffold with robust neurotrophic, neurogenic and neuroprotective action Chakravarty, Sumana Maitra, Swati Reddy, R Gajendra Das, Tapatee Jhelum, Priya Kootar, Scherazad Rajan, Wenson D. Samanta, Anumita Samineni, Ramesh Pabbaraja, Srihari Kernie, Steven G. Mehta, Goverdhan Kumar, Arvind Sci Rep Article In search for drugs to treat neuropsychiatric disorders wherein neurotrophic and neurogenic properties are affected, two neurotrophically active small molecules specially crafted following natural product leads based on 2-oxa-spiro[5.5]-undecane scaffold, have been thoroughly evaluated for their neurotrophic, neurogenic and neuroprotective potential in ex vivo primary culture and in vivo zebrafish and mouse models. The outcome of in vivo investigations suggest that one of these molecules is more neurotrophic than neurogenic while the other one is more neurogenic than neurotrophic and the former exhibits remarkable neuroprotection in a mouse acute ischemic stroke model. The molecular mechanisms of action of these compounds appear to be through the TrkB-MEK-ERK-CREB-BDNF pathway as pre-treatment with neurotrophin receptor TrkB inhibitor ANA-12 and MEK inhibitor PD98059 attenuates the neurotrophic action of compounds. Nature Publishing Group 2015-09-21 /pmc/articles/PMC4585672/ /pubmed/26388493 http://dx.doi.org/10.1038/srep14134 Text en Copyright © 2015, Macmillan Publishers Limited http://creativecommons.org/licenses/by/4.0/ This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/
spellingShingle Article
Chakravarty, Sumana
Maitra, Swati
Reddy, R Gajendra
Das, Tapatee
Jhelum, Priya
Kootar, Scherazad
Rajan, Wenson D.
Samanta, Anumita
Samineni, Ramesh
Pabbaraja, Srihari
Kernie, Steven G.
Mehta, Goverdhan
Kumar, Arvind
A novel natural product inspired scaffold with robust neurotrophic, neurogenic and neuroprotective action
title A novel natural product inspired scaffold with robust neurotrophic, neurogenic and neuroprotective action
title_full A novel natural product inspired scaffold with robust neurotrophic, neurogenic and neuroprotective action
title_fullStr A novel natural product inspired scaffold with robust neurotrophic, neurogenic and neuroprotective action
title_full_unstemmed A novel natural product inspired scaffold with robust neurotrophic, neurogenic and neuroprotective action
title_short A novel natural product inspired scaffold with robust neurotrophic, neurogenic and neuroprotective action
title_sort novel natural product inspired scaffold with robust neurotrophic, neurogenic and neuroprotective action
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4585672/
https://www.ncbi.nlm.nih.gov/pubmed/26388493
http://dx.doi.org/10.1038/srep14134
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