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ACACETIN, APIGENIN, CHRYSIN AND PINOCEMBRIN CAUSE IRREVERSIBLE CYP3A4 INHIBITION BY HEME DESTRUCTION (CROSBI ID 707889)

Prilog sa skupa u zborniku | sažetak izlaganja sa skupa

Bojić, Mirza ; Kondža, Martin ; Maleš, Željan ACACETIN, APIGENIN, CHRYSIN AND PINOCEMBRIN CAUSE IRREVERSIBLE CYP3A4 INHIBITION BY HEME DESTRUCTION // 27HSKIKI Book of Abstracts. 2021

Podaci o odgovornosti

Bojić, Mirza ; Kondža, Martin ; Maleš, Željan

engleski

ACACETIN, APIGENIN, CHRYSIN AND PINOCEMBRIN CAUSE IRREVERSIBLE CYP3A4 INHIBITION BY HEME DESTRUCTION

Flavonoids are ubiquitous plant compounds consumed in everyday diet through fruits and vegetables. Cytochrome P450 enzymes are hemoproteins, involved in the metabolism of drugs and lipophilic xenobiotics. Most registered active pharmaceutical ingredients are substrates of CYP3A4 enzyme. It has previously been reported that acacetin, apigenin, chrysin and pinocembrin irreversibly inhibit CYP3A4 enzyme. The objective of this study was to determine if inhibition is achieved through heme destruction. For this purpose, hemochromopyridine test was used. Hemochromopyridine test is based on the formation of heme iron complex with pyridine. Complex is yellow colored and can be measured spectrophotometrically. Heme concentration was measured after incubation of flavonoids with CYP3A4 baculosomes containing NADP reductase and cytochrome b5. Reaction was initiated with the addition of coenzyme NADPH. Heme concentration was determined after 30 minutes of incubation and was expressed as percentage to the control that did not contain an inhibitor. The residual heme concentration after incubation with acacetin, apigenin, chrysin, and pinocembrin was 49%, 45%, 5%, 25%, respectively. Heme destruction can also be caused by the reactive oxygen species that are generated in the nonproductive cytochrome P450 cycle. To eliminate this possibility flavonoids incubations were repeated with the addition of superoxide dismutase and catalase. No significant change was observed in residual heme concentration when compared to incubation without superoxide dismutase and catalase. It can be concluded that inhibition of cytochrome P450 by the analyzed flavonoids is mediated by heme destruction. Further analysis is needed to determine possible heme adducts and reactive flavonoid intermediaries responsible for the destruction.

flavonoids, inhibition, CYP3A4

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Podaci o prilogu

P-013

2021.

objavljeno

Podaci o matičnoj publikaciji

27HSKIKI Book of Abstracts

Podaci o skupu

27. hrvatski skup kemičara i kemijskih inženjera (27HSKIKI)

poster

05.10.2021-08.10.2021

Veli Lošinj, Hrvatska

Povezanost rada

Farmacija