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<p><i>Ilex paraguariensis</i> (mate) is a popular South American plant with a documented phytochemical profile, but comparative data on extracts obtained with solvents of different polarity remain limited. In this regard, this study aimed to characterize methanol, ethanol, and ethyl acetate extracts for phenolic composition by the total phenol and total flavonoid content colorimetric methods, followed by high-performance liquid chromatography with diode-array detection (HPLC-DAD), antioxidant capacity, enzyme inhibition, toxicity, antiproliferative effects, antimicrobial properties, and in silico target prediction using the Search Tool for Interactions of Chemicals (STITCH). The methanol extract showed the highest measured total phenolic content (72.37&#xa0;mg gallic acid equivalents/g), and total flavonoid content (36.78&#xa0;mg rutin equivalents/g). It also contained higher measured levels of chlorogenic acid and catechin than the other extracts, reaching ~ 27.9&#xa0;mg/g and ~ 1.2&#xa0;mg/g, respectively, and displayed a more pronounced radical-scavenging and reducing capacity. Despite its lower phenolic content, the ethyl acetate extract showed the highest measured metal-chelating activity (8.54&#xa0;mg ethylenediaminetetraacetic acid equivalents/g), whereas the ethanol extract showed higher measured inhibitory activity against cholinesterases, tyrosinase, and α-glucosidase. All extracts had half-maximal lethal concentration values above 5&#xa0;mg/mL in <i>Artemia salina</i> and reduced human colorectal carcinoma HCT116 cell viability, with half-maximal inhibitory concentration values of 134–172&#xa0;µg/mL. Broad antifungal and selective antibacterial activity were observed, with minimum inhibitory concentrations of 0.18–2.20&#xa0;mg/mL. STITCH analysis identified chlorogenic acid and catechin as putative ligands for caspase-3 and cyclooxygenase-2. Collectively, the findings herein indicated that extraction solvent strongly influences the phytochemical and bioactivity profile of mate extracts.</p>

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Influence of solvent polarity on the phenolic composition, antioxidant, enzyme inhibitory, antiproliferative, and antimicrobial activities of Ilex paraguariensis leaf extracts

  • 期刊论文

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  • 发表日期：

    2026年7月11日

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  • Adrian-Gabriel Moroșan,
  • Oleg Frumuzachi,
  • Andrei Mocan,
  • Mariachiara Gabriele,
  • Simonetta Cristina Di Simone,
  • Gianina Crișan,
  • Luigi Menghini,
  • Gokhan Zengin,
  • Dejan Stojković,
  • Marija Ivanov,
  • Claudio Ferrante

摘要

Ilex paraguariensis (mate) is a popular South American plant with a documented phytochemical profile, but comparative data on extracts obtained with solvents of different polarity remain limited. In this regard, this study aimed to characterize methanol, ethanol, and ethyl acetate extracts for phenolic composition by the total phenol and total flavonoid content colorimetric methods, followed by high-performance liquid chromatography with diode-array detection (HPLC-DAD), antioxidant capacity, enzyme inhibition, toxicity, antiproliferative effects, antimicrobial properties, and in silico target prediction using the Search Tool for Interactions of Chemicals (STITCH). The methanol extract showed the highest measured total phenolic content (72.37 mg gallic acid equivalents/g), and total flavonoid content (36.78 mg rutin equivalents/g). It also contained higher measured levels of chlorogenic acid and catechin than the other extracts, reaching ~ 27.9 mg/g and ~ 1.2 mg/g, respectively, and displayed a more pronounced radical-scavenging and reducing capacity. Despite its lower phenolic content, the ethyl acetate extract showed the highest measured metal-chelating activity (8.54 mg ethylenediaminetetraacetic acid equivalents/g), whereas the ethanol extract showed higher measured inhibitory activity against cholinesterases, tyrosinase, and α-glucosidase. All extracts had half-maximal lethal concentration values above 5 mg/mL in Artemia salina and reduced human colorectal carcinoma HCT116 cell viability, with half-maximal inhibitory concentration values of 134–172 µg/mL. Broad antifungal and selective antibacterial activity were observed, with minimum inhibitory concentrations of 0.18–2.20 mg/mL. STITCH analysis identified chlorogenic acid and catechin as putative ligands for caspase-3 and cyclooxygenase-2. Collectively, the findings herein indicated that extraction solvent strongly influences the phytochemical and bioactivity profile of mate extracts.