Neuroprotective Effects of the Securinine-Analogs: Identification of Allomargaritarine as a Lead Compound
Oxidative stress and mitochondrial disturbances are the common and important causative factors of aging, and play an important role in the late onset of sporadic neurodegenerative diseases, including Alzheimer disease (AD). Furthermore, emerging evidence from in vitro and in vivo disease models suggests that oxidative stress and increased vulnerability to induction of mitochondrial permeability transition leads to the pathogenesis of the neurological disorders. Towards the goals of developing effective neuroprotectors, this article describes the synthesis and neuroprotective studies of various derivatives of the naturally occurring alkaloid securinine, based on which a lead compound, allomargaritarine (a diastereomer of margaritarine), was identified as an effective therapeutic for neuroprotection. Allomargaritarine exhibits high antioxidant activity, and has significant mitoprotective effect on cellular models of neurodegeneration.
M. E. Neganova et al., "Neuroprotective Effects of the Securinine-Analogs: Identification of Allomargaritarine as a Lead Compound," CNS and Neurological Disorders - Drug Targets, vol. 15, no. 1, pp. 102-107, CNS and Neurological Disorders - Drug Targets, Feb 2016.
The definitive version is available at https://doi.org/10.2174/1871527314666150821111812
Keywords and Phrases
Alkaloid Derivative; Allomargaritarine; Plant Medicinal Product; Securinine; Securinine Derivative; Unclassified Drug; Aging; Alzheimer Disease; Animal Cell; Animal Tissue; Antioxidant Activity; Cell Survival; Controlled Study; Disorders of Mitochondrial Functions; Drug Synthesis; Lipid Peroxidation; Male; Mitochondrial Membrane Potential; Mitochondrial Permeability; MTT Assay; Nerve Degeneration; Neuroprotection; Newborn; Nonhuman; Oxidative Stress; Rat; Ultraviolet Spectroscopy
International Standard Serial Number (ISSN)
Article - Journal
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01 Feb 2016