Design, synthesis and evaluation of genistein-polyamine conjugates as multi-functional anti-Alzheimer agents

A series of genistein-polyamine conjugates (4a–4h) were designed, synthesized and evaluated as multi-functional anti-Alzheimer agents. The results showed that these compounds had significant cholinesterases (ChEs) inhibitory activity. Compound 4b exhibited the strongest inhibition to acetylcholinesterase (AChE) with an IC50 value of 2.75 μmol/L, which was better than that of rivastigmine (5.60 μmol/L). Lineweaver–Burk plot and molecular modeling study showed that compound 4b targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, compound 4b showed potent metal-chelating ability. In addition, it was found that 4a–4h did not affect HepG-2 cell viability at the concentration of 10 μmol/L.

• Publication year

  2015

• Venue

  Acta Pharmaceutica Sinica B

• Publication date

  2015-01-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/j.apsb.2014.12.008PMID 26579427PMCID 4629212
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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