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.
Edible berries such as the fruits of black chokeberry (Aronia melanocarpa (Michx.) Elliott) and bilberry (Vaccinium myrtillus L.) are considered to be rich in phenolic compounds, which are nowadays attracting great interest due to their promising health benefits. The main objective of our study was to investigate, for the first time, their inhibitory properties on Src tyrosine kinase activity, as this enzyme plays an important role in multiple cellular processes and is activated in both cancer and inflammatory cells. In hydroethanolic fruit extracts, 5.0–5.9% of total polyphenols were determined spectrophotometrically, including high amounts of hydroxycinnamic acid derivatives. HPLC analysis revealed that the black chokeberry and bilberry extracts contained 2.05 mg/g and 2.54 mg/g of chlorogenic acid, respectively. Using a time-resolved fluorescence resonance energy transfer (TR-FRET) assay, the extracts studied were found to have comparable inhibitory effects on Src tyrosine kinase, with IC50 values of 366 µg/mL and 369 µg/mL, respectively. The results also indicated that chlorogenic acid contributes significantly to the observed effect. In addition, both fruit extracts exhibited antioxidant activity by scavenging DPPH and NO radicals with SC50 values of 153–352 µg/mL. Our study suggested that black chokeberry and bilberry fruits may be beneficial in cancer and other inflammation-related diseases.
In the present study, the extraction of volatile terpenes from A. annua with supercritical CO2 (sc-CO2) was optimized by a full factorial design procedure and compared with conventional distillation. The influence of pressure (100–220 bar) and temperature (40–60 °C) on sc-CO2 extraction was investigated to obtain extracts rich in the desired components while maintaining a high yield. Extraction yields (m/m) varied from 0.62% (130 bar/40 °C) to 1.92% (100 bar/60 °C). Monoterpenes were the most abundant constituents of the sc-CO2 extracts, among which artemisia ketone (16.93–48.49%), camphor (3.29–18.44%) and 1,8-cineole (4.77–11.89%) dominated. Arteannuin B (3.98–10.03%) and β-selinene (1.05–7.42%) were the major sesquiterpenes. Differences were found between the terpene profiles of the sc-CO2 extracts and the essential oils obtained by conventional hydrodistillation and steam distillation, as well as between the distilled essential oils. Our results demonstrate the optimal conditions for the rapid and effective supercritical extraction of certain monoterpenes and sesquiterpenes from A. annua, which have promising antimicrobial, antioxidant, antiviral, anti-inflammatory and antitumor properties.