Synthetic curcumin analogs as inhibitors of β -amyloid peptide aggregation: Potential therapeutic and diagnostic agents for Alzheimer’s disease

Bukhari Syed Nasir Abbas, Ibrahim Jantan

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

There is a crucial need to develop new effective drugs for Alzheimer's disease (AD) as the currently available AD treatments provide only momentary and incomplete symptomatic relief. Amongst natural products, curcumin, a major constituent of turmeric, has been intensively investigated for its neuroprotective effect against β-amyloid (Aβ)-induced toxicity in cultured neuronal cells. The ability of curcumin to attach to Aβ peptide and prevent its accumulation is attributed to its three structural characteristics such as the presence of two aromatic end groups and their co-planarity, the length and rigidity of the linker region and the substitution conformation of these aromatics. However, curcumin failed to reach adequate brain levels after oral absorption in AD clinical trials due to its low water solubility and poor oral bioavailability. A number of new curcumin analogs that mimic the active site of the compound along with analogs that mimic the curcumin anti-amyloid effect combined with anticholinesterase effect have been developed to enhance the bioavailability, pharmacokinetics, water solubility, stability at physiological conditions and delivery of curcumin. In this article, we have summarized all reported synthetic analogs of curcumin showing effects on β-amyloid and discussed their potential as therapeutic and diagnostic agents for AD.

Original languageEnglish
Pages (from-to)1110-1121
Number of pages12
JournalMini-Reviews in Medicinal Chemistry
Volume15
Issue number13
Publication statusPublished - 1 Oct 2015

Fingerprint

Curcumin
Amyloid
Alzheimer Disease
Peptides
Solubility
Therapeutics
Biological Availability
Curcuma
Aptitude
Water
Cholinesterase Inhibitors
Neuroprotective Agents
Biological Products
Cultured Cells
Catalytic Domain
Pharmacokinetics
Clinical Trials
Brain
Pharmaceutical Preparations

Keywords

  • Alzheimer’s disease
  • Anti-amyloid effect
  • Brain
  • Neuroprotective effect
  • Synthetic curcumin analogs
  • β-amyloid

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

Cite this

Synthetic curcumin analogs as inhibitors of β -amyloid peptide aggregation : Potential therapeutic and diagnostic agents for Alzheimer’s disease. / Syed Nasir Abbas, Bukhari; Jantan, Ibrahim.

In: Mini-Reviews in Medicinal Chemistry, Vol. 15, No. 13, 01.10.2015, p. 1110-1121.

Research output: Contribution to journalArticle

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