Preliminary studies of berberine and its semi-synthetic derivatives as a promising class of multi-target anti-parkinson agents

Nat Prod Res. 2018 Jun;32(12):1395-1401. doi: 10.1080/14786419.2017.1350669. Epub 2017 Jul 10.

Abstract

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.

Keywords: Berberine; PDE; Parkinson’s; multi-target.

MeSH terms

  • Antiparkinson Agents / chemistry*
  • Antiparkinson Agents / pharmacology*
  • Berberine / chemistry*
  • Berberine / pharmacology
  • Computer Simulation
  • Drug Evaluation, Preclinical / methods
  • Humans
  • Magnetic Resonance Spectroscopy
  • Molecular Docking Simulation
  • Molecular Targeted Therapy
  • Monoamine Oxidase / chemistry
  • Monoamine Oxidase / metabolism
  • Monoamine Oxidase Inhibitors / pharmacology*
  • Parkinson Disease / drug therapy

Substances

  • Antiparkinson Agents
  • Monoamine Oxidase Inhibitors
  • Berberine
  • Monoamine Oxidase