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. 2023 Jan 16;11(1):232.
doi: 10.3390/biomedicines11010232.

Artemisia annua L. Extracts Irreversibly Inhibit the Activity of CYP2B6 and CYP3A4 Enzymes

Martin Kondža  1 , Marta Mandić  1 , Ivona Ivančić  1 , Sanda Vladimir-Knežević  2 , Ivica Brizić  1   3
Affiliations

Artemisia annua L. Extracts Irreversibly Inhibit the Activity of CYP2B6 and CYP3A4 Enzymes

Martin Kondža et al. Biomedicines. .

Abstract

Artemisia annua L. has long been known for its medicinal properties and isolation of ingredients whose derivatives are used for therapeutic purposes. The CYP2B6 and CYP3A4 enzymes belong to a large family of cytochrome P450 enzymes. These enzymes are involved in the metabolism of drugs and other xeonobiotics. It is known that various compounds can induce or inhibit the activity of these enzymes. The aim of this study was to investigate the nature of the inhibitory effect of Artemisia annua extract on CYP2B6 and CYP3A4 enzymes, as well as the type of inhibition, the presence of reversible or pseudo-irreversible inhibition, and the possible heme destruction. The methanolic extract of Artemisia annua showed an inhibitory effect on CYP2B6 (by almost 90%) and CYP3A4 enzymes (by almost 70%). A significant decrease in heme concentration by 46.8% and 38.2% was observed in different assays. These results clearly indicate that the studied plant extracts significantly inhibited the activity of CYP2B6 and CYP3A4 enzymes. Moreover, they showed irreversible inhibition, which is even more important for possible interactions with drugs and dietary supplements.

Keywords: Artemisia annua L.; CYP2B6; CYP3A4; heme; inhibition; methanolic extracts.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Artemisia annua L. [4].
Figure 2
Figure 2
Residual activity (%) of CYP2B6 and CYP3A4 enzymes after incubation with AAE (10 μg/mL) expressed as mean of triplicate; MDI−metabolism-dependent inhibition; TDI−time-dependent inhibition; DI−direct inhibition.
Figure 3
Figure 3
Spectra showing heme destruction with incubations containing AAE and AAE with SOD and CAT.
Figure 4
Figure 4
Residual activity (%) of CYP2B6 and CYP3A4 enzymes after incubation with AAE and dialysis and AAE with PCF and dialysis expressed as mean of triplicate; No statistically significant difference was observed between the samples with and without PCF (p > 0.05); CON—control.
See this image and copyright information in PMC

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