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<p>While <i>Humulus lupulus</i> L. (hop) is extensively cultivated for the brewing industry, its seeds are largely treated as an underutilized byproduct, and their phytochemical and biological potential remains relatively less explored. This study aimed to characterize the chemical composition and evaluate preliminary biological activities of seed extracts obtained from a particular hop species growing in Iran. In this regard, polarity-guided extraction was performed using petroleum ether (PE), chloroform (CHL), and methanol (MeOH). The extracts were evaluated for antibacterial, antibiofilm, and antimalarial activities. Phytochemical profiles were determined using 1D and 2D NMR spectroscopy and Gas Chromatography–Mass Spectrometry (GC–MS). Finally, the cytotoxic and anti-migratory effects of the isolated constituents were assessed against MDA-MB-231 breast cancer cells via MTT assay. The MeOH extract and its fractions exhibited notable antibacterial and antibiofilm activities against <i>Staphylococcus aureus</i> and <i>Escherichia coli</i>, despite a modest antimalarial activity (IC₅₀ = 3.9 ± 0.036&#xa0;mg/mL). The ethyl acetate (EtOAc) fraction of the MeOH extract contained the highest total flavonoid and polyphenol content, correlating with improved antioxidant capacity (RC₅₀ = 127.7 ± 1.2&#xa0;µg/mL) compared to other fractions. NMR analysis identified epicatechin as major constituent of the polar extract, while GC–MS of the PE extract revealed fatty acids like linoleic, linolenic, and palmitic acid methyl esters in seeds. Moreover, the identified epicatechin demonstrated cytotoxicity against MDA-MB-231 cells (IC₅₀ ≈ 182&#xa0;µg/mL, 48&#xa0;h) and inhibited cell migration. The findings demonstrate that hop seeds contain essential fatty acids (FA) and polyphenols, particularly epicatechin which exhibited in vitro biological activities. Thus, transitioning hop seeds from industrial waste to a potential source of antioxidant constituents, with preliminary cytotoxic effects warranting further investigation, may provide a basis for future studies exploring nutraceutical relevance.</p>

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Humulus lupulus L. seed: an underrated source of valuable active phytochemicals

  • 期刊论文

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  • 发表日期：

    2026年8月1日

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  • Amirreza Nazemiyeh,
  • Hadi Ghanbari,
  • Mohammad Yousef Memar,
  • Samar Mahari,
  • Solmaz Asnaashari,
  • Zahra Eskandari,
  • Sedigheh Bamdad Moghadam,
  • Morteza Eskandani,
  • Sanaz Hamedeyazdan,
  • Hossein Nazemiyeh

摘要

While Humulus lupulus L. (hop) is extensively cultivated for the brewing industry, its seeds are largely treated as an underutilized byproduct, and their phytochemical and biological potential remains relatively less explored. This study aimed to characterize the chemical composition and evaluate preliminary biological activities of seed extracts obtained from a particular hop species growing in Iran. In this regard, polarity-guided extraction was performed using petroleum ether (PE), chloroform (CHL), and methanol (MeOH). The extracts were evaluated for antibacterial, antibiofilm, and antimalarial activities. Phytochemical profiles were determined using 1D and 2D NMR spectroscopy and Gas Chromatography–Mass Spectrometry (GC–MS). Finally, the cytotoxic and anti-migratory effects of the isolated constituents were assessed against MDA-MB-231 breast cancer cells via MTT assay. The MeOH extract and its fractions exhibited notable antibacterial and antibiofilm activities against Staphylococcus aureus and Escherichia coli, despite a modest antimalarial activity (IC₅₀ = 3.9 ± 0.036 mg/mL). The ethyl acetate (EtOAc) fraction of the MeOH extract contained the highest total flavonoid and polyphenol content, correlating with improved antioxidant capacity (RC₅₀ = 127.7 ± 1.2 µg/mL) compared to other fractions. NMR analysis identified epicatechin as major constituent of the polar extract, while GC–MS of the PE extract revealed fatty acids like linoleic, linolenic, and palmitic acid methyl esters in seeds. Moreover, the identified epicatechin demonstrated cytotoxicity against MDA-MB-231 cells (IC₅₀ ≈ 182 µg/mL, 48 h) and inhibited cell migration. The findings demonstrate that hop seeds contain essential fatty acids (FA) and polyphenols, particularly epicatechin which exhibited in vitro biological activities. Thus, transitioning hop seeds from industrial waste to a potential source of antioxidant constituents, with preliminary cytotoxic effects warranting further investigation, may provide a basis for future studies exploring nutraceutical relevance.