Preliminary studies of berberine and its semi-synthetic derivatives as a promising class of multi-target anti-parkinson agents
| Autor: | Sergio Bova, Giuseppe Zagotto, Giovanni Ribaudo, Marcella Canton, Enrico Zanforlin |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Drug Magnetic Resonance Spectroscopy Monoamine Oxidase Inhibitors Berberine Monoamine oxidase In silico media_common.quotation_subject Drug Evaluation Preclinical Plant Science Pharmacology PDE Biochemistry Analytical Chemistry Antiparkinson Agents 03 medical and health sciences chemistry.chemical_compound Multi-target Parkinson’s Computer Simulation Humans Molecular Docking Simulation Molecular Targeted Therapy Monoamine Oxidase Parkinson Disease media_common Chemistry Organic Chemistry Phosphodiesterase Adenosine receptor Preclinical In vitro 030104 developmental biology Drug Evaluation multi-target Parkinsonâs Parkinsonâ s |
| DOI: | 10.6084/m9.figshare.5189089 |
| Popis: | Parkinson’s disease (PD) is a neurodegenerative disorder bearing motor and nonmotor symptoms. The treatment today is symptomatical rather than preventive or curative and this leaves the field open for the search of both novel molecular targets and drug candidates. Interference with α-synuclein fibrillation, monoamine oxidase (MAO) inhibition, modulation of adenosine receptors and the inhibition of specific phosphodiesterase (PDE) isoforms are some of the currently pursued strategies. We synthesised and studied some semi-synthetic berberine derivatives using a set of in silico tools. We evaluated their drug-likeness and tested the compounds against a set of target proteins involved in the onset or progression of PD, with a particular attention to MAO-B. Preliminary in vitro assay on MAO-B confirmed our in silico predictions. |
| Databáze: | OpenAIRE |
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