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<p>Hairy root cultures of <i>Linum leonii</i> F.W. Schultz, Linaceae, are a valuable biotechnological source for producing bioactive secondary metabolites, particularly due to the therapeutic relevance of <i>Linum</i> species and the efficiency of hairy roots in metabolite biosynthesis. From ethylacetate extract of <i>in vitro</i> hairy roots of <i>Linum leonii</i> F.W.Schultz, Linaceae, were isolated and identified seven compounds. Amoung them, two are novel natural compounds: cilinaphthalide C and leonsiferon. Five other were identified as arylnaphthalide lignans derivatives: diphyllin, phyllantusmin C, cilinaphthalide C, mono- and biglycosylated derivatives of 7-oxyginated arylnaphthalide lactone diphyllin, tuberculatin and reticulatuside A. Furthermore, two other metabolites have been isolated: nimbinone and bis-norditerpene from isopisiferin type leonsiferon. The podocarpane nimbinone has been previously reported only once from natural sources. Notably, the occurrence of all seven compounds, except diphyllin, have not been reported from family Linaceae. Anticarcinogenic and cytoprotective activity were evaluated in <i>Saccharomyces cerevisiae</i> model. Most prominent anticarcinogenic and cytoprotective activity was found for nimbinone, and the two novel compounds, cilinaphthalide C, and leonsiferon. The discovery of these compounds supports the use of <i>L. leonii</i> hairy roots in drug discovery and further investigation into their pharmacological potential.</p> Graphical Abstract <p></p>

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Discovery of Novel Compounds from Linum leonii Hairy Roots with Anticarcinogenic and Cytoprotective Potential

  • 期刊论文

  • 发表日期：

    2025年5月28日

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  • Yancho Zarev,
  • Rada Nedelcheva,
  • Teodora Todorova,
  • Krassimir Boyadzhiev,
  • Martin Dimitrov,
  • Iliana Ionkova

摘要

Hairy root cultures of Linum leonii F.W. Schultz, Linaceae, are a valuable biotechnological source for producing bioactive secondary metabolites, particularly due to the therapeutic relevance of Linum species and the efficiency of hairy roots in metabolite biosynthesis. From ethylacetate extract of in vitro hairy roots of Linum leonii F.W.Schultz, Linaceae, were isolated and identified seven compounds. Amoung them, two are novel natural compounds: cilinaphthalide C and leonsiferon. Five other were identified as arylnaphthalide lignans derivatives: diphyllin, phyllantusmin C, cilinaphthalide C, mono- and biglycosylated derivatives of 7-oxyginated arylnaphthalide lactone diphyllin, tuberculatin and reticulatuside A. Furthermore, two other metabolites have been isolated: nimbinone and bis-norditerpene from isopisiferin type leonsiferon. The podocarpane nimbinone has been previously reported only once from natural sources. Notably, the occurrence of all seven compounds, except diphyllin, have not been reported from family Linaceae. Anticarcinogenic and cytoprotective activity were evaluated in Saccharomyces cerevisiae model. Most prominent anticarcinogenic and cytoprotective activity was found for nimbinone, and the two novel compounds, cilinaphthalide C, and leonsiferon. The discovery of these compounds supports the use of L. leonii hairy roots in drug discovery and further investigation into their pharmacological potential.

Graphical Abstract