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Pregled bibliografske jedinice broj: 1074193

Inhibitory effect of acacetin, apigenin, chrysin and pinocembrin on human cytochrome P450 3A4


Kondža, Martin; Rimac, Hrvoje; Maleš, Željan; Turčić, Petra; Ćavar, Ivan; Bojić, Mirza
Inhibitory effect of acacetin, apigenin, chrysin and pinocembrin on human cytochrome P450 3A4 // Croatica chemica acta, 93 (2020), 1; 33-39 doi:10.5562/cca3652 (međunarodna recenzija, članak, znanstveni)


CROSBI ID: 1074193 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Inhibitory effect of acacetin, apigenin, chrysin and pinocembrin on human cytochrome P450 3A4

Autori
Kondža, Martin ; Rimac, Hrvoje ; Maleš, Željan ; Turčić, Petra ; Ćavar, Ivan ; Bojić, Mirza

Izvornik
Croatica chemica acta (0011-1643) 93 (2020), 1; 33-39

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

Ključne riječi
flavonoids ; inhibition ; cytochromes P450

Sažetak
Cytochrome P450 3A4 is the most significant enzyme in metabolism of medications. Flavonoids are common secondary plant metabolites found in fruits and vegetables. Some flavonoids can interact with other drugs by inhibiting cytochrome P450 enzymes. Thus, the objective of this study was to determine inhibition kinetics of cytochrome P450 3A4 by flavonoids: acacetin, apigenin, chrysin and pinocembrin. For this purpose, testosterone was used as marker substrate, and generation of the 6β-hydroxy metabolite was monitored by high performance liquid chromatography coupled with diode array detector. IC 50 values, inhibition constants, and rates of inhibition were determined. IC 50 values ranged between 0.6 and 11.4 µM. The strongest inhibitor was chrysin (IC 50 0.6 µM, inhibition constant 0.6 µM, inhibition rate constant 0.065 min -1 , inhibition efficacy 0.108 min -1 µM -1 ). Compared to other flavonoids analyzed, chrysin’s inhibitory effect can be attributed to the hydrophobic nonsubstituted B ring, as well as rigidity of the structure. When foods rich in chrysin are consumed, e.g. honey and propolis, chrysin can cause food-drug interactions. Further in vitro studies are needed to determine the reactive intermediate responsible for inactivation of cytochrome P450 3A4 enzyme, as well as in vivo studies to determine possible clinical significance of this inhibition

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Farmacija



POVEZANOST RADA


Projekti:
UIP-2014-09-5704 - Metabolizam i interakcije biološki aktivnih spojeva i QSAR (MAINBASE4QSAR) (BOJIć, MIRZA, HRZZ - 2014-09) ( POIROT)

Ustanove:
Farmaceutsko-biokemijski fakultet, Zagreb

Profili:

Avatar Url Petra Turčić (autor)

Avatar Url Martin Kondža (autor)

Avatar Url Hrvoje Rimac (autor)

Avatar Url Željan Maleš (autor)

Avatar Url Mirza Bojić (autor)

doi

Citiraj ovu publikaciju

Kondža, Martin; Rimac, Hrvoje; Maleš, Željan; Turčić, Petra; Ćavar, Ivan; Bojić, Mirza
Inhibitory effect of acacetin, apigenin, chrysin and pinocembrin on human cytochrome P450 3A4 // Croatica chemica acta, 93 (2020), 1; 33-39 doi:10.5562/cca3652 (međunarodna recenzija, članak, znanstveni)
Kondža, M., Rimac, H., Maleš, Ž., Turčić, P., Ćavar, I. & Bojić, M. (2020) Inhibitory effect of acacetin, apigenin, chrysin and pinocembrin on human cytochrome P450 3A4. Croatica chemica acta, 93 (1), 33-39 doi:10.5562/cca3652.
@article{article, year = {2020}, pages = {33-39}, DOI = {10.5562/cca3652}, keywords = {flavonoids, inhibition, cytochromes P450}, journal = {Croatica chemica acta}, doi = {10.5562/cca3652}, volume = {93}, number = {1}, issn = {0011-1643}, title = {Inhibitory effect of acacetin, apigenin, chrysin and pinocembrin on human cytochrome P450 3A4}, keyword = {flavonoids, inhibition, cytochromes P450} }
@article{article, year = {2020}, pages = {33-39}, DOI = {10.5562/cca3652}, keywords = {flavonoids, inhibition, cytochromes P450}, journal = {Croatica chemica acta}, doi = {10.5562/cca3652}, volume = {93}, number = {1}, issn = {0011-1643}, title = {Inhibitory effect of acacetin, apigenin, chrysin and pinocembrin on human cytochrome P450 3A4}, keyword = {flavonoids, inhibition, cytochromes P450} }

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


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