Calotropis gigantea stem bark extract activates HepG2 cell apoptosis through ROS and its effect on cytochrome P450

IC50 Gigantea
DOI: 10.1016/j.heliyon.2023.e16375 Publication Date: 2023-05-18T03:00:25Z
ABSTRACT
The 95% ethanolic extract of the dry powder Calotropis gigantea (C. gigantea) stem bark was separated by fractionation with different solutions to yield 4 fractions: dichloromethane (CGDCM), ethyl acetate (CGEtOAc), and water (CGW). This research focused on CGDCM-induced apoptosis in HepG2 cells IC50 above-IC50 values, which provide useful information for future anticancer applications. CGDCM had lower cytotoxicity normal lung fibroblast IMR-90 than cells. Apoptotic induction mediated decreased fatty acid ATP synthesis while increasing reactive oxygen species production. effects four extracts activity major CYP450 isoforms (CYP1A2, CYP2C9, CYP2E1 CYP3A4) were determined using CYP-specific model each isoform. All fractions shown be poor inhibitors CYP1A2 (IC50 > 1000 μg/mL) moderate CYP3A4 = 56.54–296.9 μg/mL). CGW exerted inhibition activities CYP2C9 59.56 46.38 μg/mL, respectively), but CGEtOH CGEtOAc exhibited strong 12.11 20.43 respectively). It is proposed that C. at high doses have potential further studies develop alternative Inhibiting may also lead drug-herb interactions.
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