Investigation of Some Metabolic Enzyme Inhibition Properties of Novel Chalcone-Cu Complexes


Ebiri R., Turgut M., Aktas Anil D., Demir Y., Saglamtas R., Abdullah Alagoz M., ...Daha Fazla

ChemistrySelect, cilt.9, sa.27, 2024 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 9 Sayı: 27
  • Basım Tarihi: 2024
  • Doi Numarası: 10.1002/slct.202401093
  • Dergi Adı: ChemistrySelect
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier
  • Anahtar Kelimeler: AChE, Antioxidant activity, Chalcone-Cu complexes, hCA I and hCA II, Molecular docking
  • Atatürk Üniversitesi Adresli: Evet

Özet

Fourteen novel Chalcone-Cu complexes were effectively synthesized in this work. The newly synthesized Chalcone-Cu complexes were assessed for their effects on human carbonic anhydrase isoenzymes I and II, acetylcholinesterase enzymes, and antioxidant activity. The intricate compounds exhibited Ki values ranging from 41.65–190.42 nM against hCA I, 15.79–259.07 nM against hCA II, and 14.36–175.73 nM against AChE enzymes. These complexes demonstrated potent inhibitory profiles against the specified metabolic enzymes, surpassing the inhibitory effects of acetazolamide (for hCA I and II) and tacrine (for AChE). The antioxidant properties of the compounds were assessed using DPPH and ABTS radical scavenging assays, revealing that the complexes had moderate to high efficacy in neutralizing free radicals. All complexes underwent molecular docking experiments. Compounds 14, 22, and 23 yielded the highest docking scores. Compound 14 demonstrated a docking score of −6.414 kcal/mol against hCAI, whereas compound 23 attained a docking score of −6.697 kcal/mol against hCA II. Compound 22 exhibited the most favorable docking score of −9.645 kcal/mol against AChE. The acquired results have the potential to help towards the development of new drugs containing Cu complex structures for the treatment of prevalent ailments such as glaucoma and Alzheimer's diseases.