Can molecular networking be a powerful tool to target specific bioactive scaffolds? Case study of New Caledonian Euphorbiaceae species

Olivon, Florent; Allard, PM; Koval, Alexey; Leyssen, Pieter; Dumontet, Vincent; Roussi, Fanny; Cachet, Xavier; Touboul, David; Wolfender, Jean‐Luc; Katanaev, Vladimir L.; Litaudon, Marc

doi:10.1055/s-0036-1596108

Cited by 1 publication

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“…Natural and semisynthetic tigliane diterpenoids from the plant Euphorbia dracunculoides inhibited Wnt signaling in a luciferase assay in HEK293 cells, reducing the expression of Wnt target genes Axin2, c-myc and cyclin D; phosphorylation and degradation of β-catenin were similarly observed in HEK293W cells incubated with tigliane diterpenoids [177]. Euphorbiaceae plants are otherwise famous for phorbol esters, of which several, of the New Caledonian origin, have produced strong Wnt-inhibiting activities in triple-negative breast cancer cells [152,178]. Similarly, diterpene esters-phorbol 12-myristate 13-acetate (PMA) and PEP005-isolated from Euphorbia croton tiglium and Euphorbia peplus, respectively, inhibited Wnt signaling in colon cancer cells [179].…”

Section: Wnt Inhibitors From Natural Sourcesmentioning

confidence: 94%

Small Molecule Wnt Pathway Modulators from Natural Sources: History, State of the Art and Perspectives

Blagodatski

Klimenko

Jia

et al. 2020

Cells

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The Wnt signaling is one of the major pathways known to regulate embryonic development, tissue renewal and regeneration in multicellular organisms. Dysregulations of the pathway are a common cause of several types of cancer and other diseases, such as osteoporosis and rheumatoid arthritis. This makes Wnt signaling an important therapeutic target. Small molecule activators and inhibitors of signaling pathways are important biomedical tools which allow one to harness signaling processes in the organism for therapeutic purposes in affordable and specific ways. Natural products are a well known source of biologically active small molecules with therapeutic potential. In this article, we provide an up-to-date overview of existing small molecule modulators of the Wnt pathway derived from natural products. In the first part of the review, we focus on Wnt pathway activators, which can be used for regenerative therapy in various tissues such as skin, bone, cartilage and the nervous system. The second part describes inhibitors of the pathway, which are desired agents for targeted therapies against different cancers. In each part, we pay specific attention to the mechanisms of action of the natural products, to the models on which they were investigated, and to the potential of different taxa to yield bioactive molecules capable of regulating the Wnt signaling.

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