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<p>Burdock, <i>Arctium </i><i>lappa Linn.</i> (Asteraceae), is cultivated in East Asian for its edible roots, and its seeds are used in a herbal medicine. Burdock seeds and roots exhibit anti-adipogenic activity. However, the anti-adipogenic activity of the aboveground parts of burdock remains underexplored. Therefore, this study determined the anti-adipogenic effects of burdock leaf extract on 3T3-L1 adipocytes. Seventy percent ethanol (EtOH) extract of burdock leaves, which inhibited lipid accumulation, was fractionated into five fractions using Diaion<sup>®</sup> HP-20. EtOH eluted fractions (40 and 80%) strongly inhibited lipid accumulation. A common compound in these fractions was onopordopicrin (OPP), and purified OPP suppressed lipid accumulation and inhibited adipocyte differentiation. α, β-unsaturated carbonyl structure of OPP suggests potential electrophilic reactivity with polyfunctional thiol-trapping agents like cysteine residues. Indeed, the anti-adipogenic effects of OPP disappeared with the addition of cysteamine, which possesses a thiol group. Rhodamine-maleimide assay showed that OPP binds to the cysteine residues of adipocyte-specific transcription factor, peroxisome proliferator-activated receptor γ (PPARγ). Hence, our findings suggest that OPP exerts its anti-adipogenic action via binding to cysteine residues in signal proteins like PPARγ, inhibiting their activation. Thus, burdock leaf extract is a potential source of OPP, a bioactive compound with anti-obesity activity.</p>

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Japanese Leaf Burdock Extract Inhibits Adipocyte Differentiation in 3T3-L1 Cells

  • 期刊论文

  • 发表日期：

    2025年1月7日

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  • Maeta Akihiro,
  • Okamoto Yuka,
  • Ishikawa Honoka,
  • Matsunaga Tetsuro,
  • Takahashi Kyoko

摘要

Burdock, Arctium lappa Linn. (Asteraceae), is cultivated in East Asian for its edible roots, and its seeds are used in a herbal medicine. Burdock seeds and roots exhibit anti-adipogenic activity. However, the anti-adipogenic activity of the aboveground parts of burdock remains underexplored. Therefore, this study determined the anti-adipogenic effects of burdock leaf extract on 3T3-L1 adipocytes. Seventy percent ethanol (EtOH) extract of burdock leaves, which inhibited lipid accumulation, was fractionated into five fractions using Diaion® HP-20. EtOH eluted fractions (40 and 80%) strongly inhibited lipid accumulation. A common compound in these fractions was onopordopicrin (OPP), and purified OPP suppressed lipid accumulation and inhibited adipocyte differentiation. α, β-unsaturated carbonyl structure of OPP suggests potential electrophilic reactivity with polyfunctional thiol-trapping agents like cysteine residues. Indeed, the anti-adipogenic effects of OPP disappeared with the addition of cysteamine, which possesses a thiol group. Rhodamine-maleimide assay showed that OPP binds to the cysteine residues of adipocyte-specific transcription factor, peroxisome proliferator-activated receptor γ (PPARγ). Hence, our findings suggest that OPP exerts its anti-adipogenic action via binding to cysteine residues in signal proteins like PPARγ, inhibiting their activation. Thus, burdock leaf extract is a potential source of OPP, a bioactive compound with anti-obesity activity.