Publication: Neuritogenic activity of bi-functional bis-tryptoline triazole
Issued Date
2017-01-01
Resource Type
ISSN
14643391
09680896
09680896
Other identifier(s)
2-s2.0-85009471336
Rights
Mahidol University
Rights Holder(s)
SCOPUS
Bibliographic Citation
Bioorganic and Medicinal Chemistry. Vol.25, No.3 (2017), 1195-1201
Suggested Citation
Jutamas Jiaranaikulwanitch, Sarin Tadtong, Piyarat Govitrapong, Valery V. Fokin, Opa Vajragupta Neuritogenic activity of bi-functional bis-tryptoline triazole. Bioorganic and Medicinal Chemistry. Vol.25, No.3 (2017), 1195-1201. doi:10.1016/j.bmc.2016.12.027 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/42116
Research Projects
Organizational Units
Authors
Journal Issue
Thesis
Title
Neuritogenic activity of bi-functional bis-tryptoline triazole
Other Contributor(s)
Abstract
© 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.