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Pregled bibliografske jedinice broj: 1088290

Vitamin B3-Based Biologically Active Compounds as Inhibitors of Human Cholinesterases


Zandona, Antonio; Lihtar, Gabriela; Maraković, Nikola; Miš, Katarina; Bušić, Valentina; Gašo- Sokač, Dajana; Pirkmajer, Segej; Katalinić, Maja
Vitamin B3-Based Biologically Active Compounds as Inhibitors of Human Cholinesterases // International journal of molecular sciences, 21 (2020), 21; 8088, 19 doi:10.3390/ijms21218088 (međunarodna recenzija, članak, znanstveni)


CROSBI ID: 1088290 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Vitamin B3-Based Biologically Active Compounds as Inhibitors of Human Cholinesterases

Autori
Zandona, Antonio ; Lihtar, Gabriela ; Maraković, Nikola ; Miš, Katarina ; Bušić, Valentina ; Gašo- Sokač, Dajana ; Pirkmajer, Segej ; Katalinić, Maja

Izvornik
International journal of molecular sciences (1422-0067) 21 (2020), 21; 8088, 19

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
AChE ; BChE ; neurodegenerative ; Alzheimer’s ; nicotinamide ; cytotoxicity

Sažetak
We evaluated the potential of nine vitamin B3 scaffold-based derivatives as acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors, as a starting point for the development of novel drugs for treating disorders with cholinergic neurotransmission- linked pathology. As the results indicate, all compounds reversibly inhibited both enzymes in the micromolar range pointing to the preference of AChE over BChE for binding the tested derivatives. Molecular docking studies revealed the importance of interactions with AChE active site residues Tyr337 and Tyr124, which dictated most of the observed differences. The most potent inhibitor of both enzymes with Ki of 4 µM for AChE and 8 µM for BChE was the nicotinamide derivative 1-(4 0 - phenylphenacyl)-3-carbamoylpyridinium bromide. Such a result places it within the range of several currently studied novel cholinesterase inhibitors. Cytotoxicity profiling did not classify this compound as highly toxic, but the induced effects on cells should not be neglected in any future detailed studies and when considering this scaffold for drug development.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija



POVEZANOST RADA


Projekti:
UIP-2017-05-7260 - MOLEKULARNI MEHANIZMI TOKSIČNOSTI PROTUOTROVA I POTENCIJALNIH LIJEKOVA (CellToxTargets) (Katalinić, Maja, HRZZ - 2017-05) ( POIROT)
IP-2018-01-7683 - Analiza interakcija butirilkolinesteraze s novim inhibitorima i reaktivatorima (AnalyseBChE) (Kovarik, Zrinka, HRZZ - 2018-01) ( POIROT)

Ustanove:
Institut za medicinska istraživanja i medicinu rada, Zagreb,
Prehrambeno-tehnološki fakultet, Osijek

Citiraj ovu publikaciju

Zandona, Antonio; Lihtar, Gabriela; Maraković, Nikola; Miš, Katarina; Bušić, Valentina; Gašo- Sokač, Dajana; Pirkmajer, Segej; Katalinić, Maja
Vitamin B3-Based Biologically Active Compounds as Inhibitors of Human Cholinesterases // International journal of molecular sciences, 21 (2020), 21; 8088, 19 doi:10.3390/ijms21218088 (međunarodna recenzija, članak, znanstveni)
Zandona, A., Lihtar, G., Maraković, N., Miš, K., Bušić, V., Gašo- Sokač, D., Pirkmajer, S. & Katalinić, M. (2020) Vitamin B3-Based Biologically Active Compounds as Inhibitors of Human Cholinesterases. International journal of molecular sciences, 21 (21), 8088, 19 doi:10.3390/ijms21218088.
@article{article, year = {2020}, pages = {19}, DOI = {10.3390/ijms21218088}, chapter = {8088}, keywords = {AChE, BChE, neurodegenerative, Alzheimer’s, nicotinamide, cytotoxicity}, journal = {International journal of molecular sciences}, doi = {10.3390/ijms21218088}, volume = {21}, number = {21}, issn = {1422-0067}, title = {Vitamin B3-Based Biologically Active Compounds as Inhibitors of Human Cholinesterases}, keyword = {AChE, BChE, neurodegenerative, Alzheimer’s, nicotinamide, cytotoxicity}, chapternumber = {8088} }
@article{article, year = {2020}, pages = {19}, DOI = {10.3390/ijms21218088}, chapter = {8088}, keywords = {AChE, BChE, neurodegenerative, Alzheimer’s, nicotinamide, cytotoxicity}, journal = {International journal of molecular sciences}, doi = {10.3390/ijms21218088}, volume = {21}, number = {21}, issn = {1422-0067}, title = {Vitamin B3-Based Biologically Active Compounds as Inhibitors of Human Cholinesterases}, keyword = {AChE, BChE, neurodegenerative, Alzheimer’s, nicotinamide, cytotoxicity}, chapternumber = {8088} }

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


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