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Lim, Mi Hee
MetalloNeuroChemistry Lab (MNCL)
Research Interests
  • Neurodegenerative disease, small molecule design, network between metal, proteins, and ROS

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Methyl yellow: A potential drug scaffold for parkinson's disease

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Title
Methyl yellow: A potential drug scaffold for parkinson's disease
Author
Geldenhuys, Werner J.Kochi, AkikoLin, LiSutariya, VijaykumarDluzen, Dean E.Van der Schyf, Cornelis J.Lim, Mi Hee
Issue Date
2014-07
Publisher
WILEY-V C H VERLAG GMBH
Citation
CHEMBIOCHEM, v.15, no.11, pp.1591 - 1598
Abstract
Parkinson's disease (PD) is an age-related neurodegenerative disease affecting movement. To date, there are no currently available therapeutic agents which can prevent or slow disease progression. Here, we evaluated an azobenzene derivative, methyl yellow (MY), as a potential drug scaffold for PD; its inhibitory activity toward monoamine oxidase B (MAO-B) as well as drug-like properties were investigated. The inhibitory effect of MY on MAO activity was determined by a MAO enzyme inhibition assay. In addition, the in vitro properties of MY as a drug candidate (e.g., blood-brain barrier (BBB) permeability, serum albumin binding, drug efflux through P-glycoprotein (P-gp), drug metabolism by P450, and mitochondrial toxicity) were examined. In vivo effectiveness of MY was also evaluated in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) Parkinsonian mouse model. MY selectively inhibited MAO-B in a dose-dependent and reversible manner. MY was BBB-permeable, bound relatively weakly to serum albumin, was an unlikely substrate for both systems of P-gp and P450, and did not cause mitochondrial toxicity. Results from the MPTP Parkinsonian mouse model indicated that, upon treatment with MY, neurotoxicity induced by MPTP was mitigated. Investigations of MY demonstrate its inhibitory activity toward MAO-B, compliant properties for drug consideration, and its neuroprotective capability in the MPTP Parkinsonian mouse model. These data provide insights into potential use, optimization, and new design of azobenzene derivatives for PD treatment.
URI
https://scholarworks.unist.ac.kr/handle/201301/5305
URL
http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84904679466
DOI
10.1002/cbic.201300770
ISSN
1439-4227
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