Berberine derivatives as inhibitors of acetylcholinesterase: A systematic review

Chem Biol Drug Des. 2023 Dec;102(6):1592-1603. doi: 10.1111/cbdd.14337. Epub 2023 Sep 4.

Abstract

Alzheimer's disease (AD) is a chronic age-related neurodegenerative brain disorder characterized by the impairment of memory accompanied by worsening of thinking ability of an individual. The exact pathophysiology of AD is not fully understood. However low level of the neurotransmitter named acetylcholine (ACh), aggregation of Aβ peptide into toxic Aβ plaque, hyperphosphorylation of tau, bio-metal imbalance, and oxidative stress are the main hallmarks of this disease. Due to the complex pathophysiology of AD, no specific treatment is available in the market, and treatment is only limited to the symptomatic relief. So, there is an urgent need for the development of new drug candidate, which can have disease-modifying effect and improve learning and memory in AD patient. Therefore, berberine-based multifunction compounds with potential cholinesterase inhibitory properties were reviewed in this article. Structure-activity relationship (SAR) and biological activity provide highlights on the new derivatives used for the management of AD.

Keywords: Alzheimer's disease; acetylcholine; acetylcholinesterase; berberine.

Publication types

  • Systematic Review
  • Review

MeSH terms

  • Acetylcholinesterase / metabolism
  • Alzheimer Disease* / drug therapy
  • Amyloid beta-Peptides / metabolism
  • Berberine* / pharmacology
  • Berberine* / therapeutic use
  • Cholinesterase Inhibitors / pharmacology
  • Cholinesterase Inhibitors / therapeutic use
  • Humans
  • Oxidative Stress

Substances

  • Amyloid beta-Peptides
  • Acetylcholinesterase
  • Berberine
  • Cholinesterase Inhibitors