Neuritogenic activity of bi-functional bis-tryptoline triazole

© 2016 Elsevier Ltd Alzheimer's disease (AD) is a common neurodegenerative disorder, one of the hallmarks of which is the deposition of aggregated β-amyloid peptides (Aβ40,42) as plaques in the brain. Oligomers of these peptides have been reported to be toxic and to inhibit neurite outgrowth, a...

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Main Authors: Jutamas Jiaranaikulwanitch, Sarin Tadtong, Piyarat Govitrapong, Valery V. Fokin, Opa Vajragupta
Format: Journal
Published: 2018
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http://cmuir.cmu.ac.th/jspui/handle/6653943832/56842
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Institution: Chiang Mai University
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spelling th-cmuir.6653943832-568422018-09-05T03:52:09Z Neuritogenic activity of bi-functional bis-tryptoline triazole Jutamas Jiaranaikulwanitch Sarin Tadtong Piyarat Govitrapong Valery V. Fokin Opa Vajragupta Biochemistry, Genetics and Molecular Biology Chemistry Pharmacology, Toxicology and Pharmaceutics © 2016 Elsevier Ltd Alzheimer's disease (AD) is a common neurodegenerative disorder, one of the hallmarks of which is the deposition of aggregated β-amyloid peptides (Aβ40,42) as plaques in the brain. Oligomers of these peptides have been reported to be toxic and to inhibit neurite outgrowth, as evidenced by neurite dystrophy and significant loss of synaptic connectivity of neurons in the AD brain resulting in cognitive decline. These peptides also react with biological metal in the brain to generate free radicals, thereby aggravating neuronal cell injury and death. Herein, multifunctional triazole-based compounds acting on multiple targets, namely β-secretase (BACE1), β-amyloid peptides (Aβ) as well as those possessing metal chelation and antioxidant properties, were developed and evaluated for neuritogenic activity in P19-derived neurons. At the non-cytotoxic concentration (1 nM), all multifunctional compounds significantly enhanced neurite outgrowth. New bis-tryptoline triazole (BTT) increased the neurite length and neurite number, by 93.25% and 136.09% over the control, respectively. This finding demonstrates the ability of multifunctional compounds targeting Aβ to enhance neurite outgrowth in addition to their neuroprotective action. 2018-09-05T03:31:00Z 2018-09-05T03:31:00Z 2017-01-01 Journal 14643391 09680896 2-s2.0-85009471336 10.1016/j.bmc.2016.12.027 https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85009471336&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/56842
institution Chiang Mai University
building Chiang Mai University Library
country Thailand
collection CMU Intellectual Repository
topic Biochemistry, Genetics and Molecular Biology
Chemistry
Pharmacology, Toxicology and Pharmaceutics
spellingShingle Biochemistry, Genetics and Molecular Biology
Chemistry
Pharmacology, Toxicology and Pharmaceutics
Jutamas Jiaranaikulwanitch
Sarin Tadtong
Piyarat Govitrapong
Valery V. Fokin
Opa Vajragupta
Neuritogenic activity of bi-functional bis-tryptoline triazole
description © 2016 Elsevier Ltd Alzheimer's disease (AD) is a common neurodegenerative disorder, one of the hallmarks of which is the deposition of aggregated β-amyloid peptides (Aβ40,42) as plaques in the brain. Oligomers of these peptides have been reported to be toxic and to inhibit neurite outgrowth, as evidenced by neurite dystrophy and significant loss of synaptic connectivity of neurons in the AD brain resulting in cognitive decline. These peptides also react with biological metal in the brain to generate free radicals, thereby aggravating neuronal cell injury and death. Herein, multifunctional triazole-based compounds acting on multiple targets, namely β-secretase (BACE1), β-amyloid peptides (Aβ) as well as those possessing metal chelation and antioxidant properties, were developed and evaluated for neuritogenic activity in P19-derived neurons. At the non-cytotoxic concentration (1 nM), all multifunctional compounds significantly enhanced neurite outgrowth. New bis-tryptoline triazole (BTT) increased the neurite length and neurite number, by 93.25% and 136.09% over the control, respectively. This finding demonstrates the ability of multifunctional compounds targeting Aβ to enhance neurite outgrowth in addition to their neuroprotective action.
format Journal
author Jutamas Jiaranaikulwanitch
Sarin Tadtong
Piyarat Govitrapong
Valery V. Fokin
Opa Vajragupta
author_facet Jutamas Jiaranaikulwanitch
Sarin Tadtong
Piyarat Govitrapong
Valery V. Fokin
Opa Vajragupta
author_sort Jutamas Jiaranaikulwanitch
title Neuritogenic activity of bi-functional bis-tryptoline triazole
title_short Neuritogenic activity of bi-functional bis-tryptoline triazole
title_full Neuritogenic activity of bi-functional bis-tryptoline triazole
title_fullStr Neuritogenic activity of bi-functional bis-tryptoline triazole
title_full_unstemmed Neuritogenic activity of bi-functional bis-tryptoline triazole
title_sort neuritogenic activity of bi-functional bis-tryptoline triazole
publishDate 2018
url https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85009471336&origin=inward
http://cmuir.cmu.ac.th/jspui/handle/6653943832/56842
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