Promise of Retinoic Acid-Triazolyl Derivatives in Promoting Differentiation of Neuroblastoma Cells

Retinoic acid induces differentiation in various types of cells including skeletal myoblasts and neuroblasts and maintains differentiation of epithelial cells. The present study demonstrates synthesis and screening of a library of retinoic acid-triazolyl derivatives for their differentiation potenti...

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Published in:ACS chemical neuroscience 2016-01, Vol.7 (1), p.82-89
Main Authors: Lone, Ali Mohd, Dar, Nawab John, Hamid, Abid, Shah, Wajaht Amin, Ahmad, Muzamil, Bhat, Bilal A
Format: Article
Language:English
Subjects:
Animals
Azides - chemistry
Azides - pharmacology
Cell Differentiation - drug effects
Cell Line, Tumor
Gene Expression Regulation, Neoplastic - drug effects
Mass Spectrometry
Mice
Neuroblastoma - metabolism
Neuroblastoma - pathology
Phosphopyruvate Hydratase - metabolism
Tretinoin - chemistry
Tretinoin - pharmacology
Triazoles - chemistry
Triazoles - pharmacology
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Summary:Retinoic acid induces differentiation in various types of cells including skeletal myoblasts and neuroblasts and maintains differentiation of epithelial cells. The present study demonstrates synthesis and screening of a library of retinoic acid-triazolyl derivatives for their differentiation potential on neuroblastoma cells. Click chemistry approach using copper­(I)-catalyzed azide–alkyne cycloaddition was adopted for the preparation of these derivatives. The neurite outgrowth promoting potential of retinoic acid-triazolyl derivatives was studied on neuroblastoma cells. Morphological examination revealed that compounds 8a, 8e, 8f, and 8k, among the various derivatives screened, exhibited promising neurite-outgrowth inducing activity at a concentration of 10 μM compared to undifferentiated and retinoic acid treated cells. Further on, to confirm this differentiation potential of these compounds, neuroblastoma cells were probed for expression of neuronal markers such as NF-H and NeuN. The results revealed a marked increase in the NF-H and NeuN protein expression when treated with 8a, 8e, 8f, and 8k compared to undifferentiated and retinoic acid treated cells. Thus, these compounds could act as potential leads in inducing neuronal differentiation for future studies.
ISSN:1948-7193
1948-7193
DOI:10.1021/acschemneuro.5b00267