Background: The present study aimed to comprehensively evaluate the anticancer, anti-inflammatory, and antioxidant properties of Globularia cordifolia L.

Samples: The plant material was collected and extracted using the maceration method. Antioxidant activities were assessed through DPPH (i.e. 2,2-diphenyl-1-picrylhydrazyl) and iron chelation assays, whereas phenolic and flavonoid contents were measured using spectrophotometric methods. Gas chromatography-mass spectrometry analysis was performed to identify biologically active compounds. The cytotoxic effect on colon cancer cells was evaluated using MTT [i.e. 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide] assays, and inflammatory cytokine levels were measured through an enzyme-linked immunosorbent assay. Molecular docking studies investigated the interactions of bioactive compounds with the 4UYA protein, and ADME (i.e. absorption, distribution, metabolism, excretion and toxicity) modeling predicted their toxicity.

Results: The study revealed that the extract exhibited strong antioxidant activity with a median 50% inhibitory concentration (IC) value of 39.48 ± 2.15 μg mL in the DPPH assay and an effective iron chelation capacity with an IC value of 4.28 ± 0.19 mg mL. The total phenolic content was 662.51 ± 20.95 mg gallic acid equivalents g, and the flavonoid content was 114.99 ± 0.51 mg quercetin equivalents g, demonstrating the extract's richness in phenolic and flavonoid compounds. Significant antiproliferative effects were observed in colon cancer cells at a dose of 250 μg mL. Inflammatory cytokine analysis indicated a reduction in pro-inflammatory responses. Molecular docking studies showed strong binding affinities between the bioactive compounds and the 4UYA protein, suggesting the mechanisms of action.

Conclusion: The findings indicate that G. cordifolia extract exhibits strong antioxidant, anti-inflammatory and antiproliferative properties, making it a promising biomolecular agent for colon cancer therapy. The high phenolic and flavonoid contents, combined with the bioactive compounds' interactions with key molecular targets, underscore its potential therapeutic applications. © 2024 Society of Chemical Industry.

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