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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...
Autores principales: | , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Nature Publishing Group
2015
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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. |
format | Online Article Text |
id | pubmed-4585672 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2015 |
publisher | Nature Publishing Group |
record_format | MEDLINE/PubMed |
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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