2. Academic Validation
  3. Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates

Synthesis, pharmacological profile and 2D-QSAR studies of curcumin-amino acid conjugates as potential drug candidates

  • Eur J Med Chem. 2020 Jun 15:196:112293. doi: 10.1016/j.ejmech.2020.112293.
Siva S Panda 1,  Adel S Girgis 2,  Sean J Thomas 3,  Jason E Capito 3,  Riham F George 4,  Asmaa Salman 5,  May A El-Manawaty 6,  Ahmed Samir 7
Affiliations

Affiliations

  • 1 Department of Chemistry and Physics, Augusta University, Augusta, GA, 30912, USA. Electronic address: sspanda12@gmail.com.
  • 2 Department of Pesticide Chemistry, National Research Centre, Dokki, Giza, 12622, Egypt.
  • 3 Department of Chemistry and Physics, Augusta University, Augusta, GA, 30912, USA.
  • 4 Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt.
  • 5 Medical and Pharmaceutical Chemistry Department, National Research Centre, Dokki, Giza, 12622, Egypt.
  • 6 Drug Bioassay-Cell Culture Laboratory, Pharmacognosy Department, National Research Centre, Dokki, Giza, 12622, Egypt.
  • 7 Microbiology Department, Faculty of Veterinary Medicine, Cairo University, Cairo, Egypt.
PMID: 32311607 DOI: 10.1016/j.ejmech.2020.112293
Abstract

A series of curcumin bis-conjugates 3a-q, 5a-k and 6a-k were synthesized in good yields utilizing an optimized reaction condition. We explored the effect of different Amino acids and protecting groups on biological activities of curcumin. The conjugates were screened for anti-inflammatory, analgesic and antimicrobial properties. Some of the conjugates showed promising biological observations with a potency comparable with the standard references. The variations in biological properties concerning different Amino acids and protecting groups are interesting observations. Effects of the synthesized conjugates on splenocytes and the production of nitric oxide by lipopolysaccharide-stimulated peritoneal macrophages are correlated with the observed anti-inflammatory properties. We have also established the safety profile of the most active conjugates. Robust 2D-QSAR studies supported and validated biological data.

Keywords

2D-QSAR; Amino acid; Analgesic; Anti-inflammatory; Antimicrobial; Curcumin; Prodrug.

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