- Reaction score
- 95
[Published March 2nd, 2020:]
'Abstract: 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.
[...]
Aiming at a new hair growth-promoting drug, a screen of 800 extracts was conducted using the TOPFlash assay in HEK293 cells, and hits were tested for the ability to promote hair growth in cell-based and mouse models. Extracts from Aconitum ciliare were among the most active both in the TOPFlash and hair growth assays, positioning this medicinal plant for the identification of a promising Wnt activator [78]. Flavonoids from the plant Vernonia anthelmintica and their derivative emerged as Wnt pathway activators for melanin synthesis in vitiligo—a sickness manifested as skin depigmentation [41]. As a potential mechanism, phosphorylation and thus inhibition of GSK3β via crosstalk with the PI3K/Akt pathway was pinpointed [41]. In this context, it is interesting to mention that tobacco smoking-caused skin pigmentation was shown to increase β-catenin levels, the activity linked to the tobacco plant (Nicotiana tabacum) metabolites [79].
[...]
Extracts of Undariopsis peterseniana, edible brown algae, were tested in hair growth models in a search for drug candidates against androgenic alopecia and found to stimulate ex vivo hair-fiber growth in rat vibrissa follicles as well as in vivo hair growth in mice. It showed an increase in β-catenin accumulation and GSK3β phosphorylation in dermal papilla cells [98].'
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7140537/
https://www.mdpi.com/2073-4409/9/3/589/pdf
'Abstract: 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.
[...]
Aiming at a new hair growth-promoting drug, a screen of 800 extracts was conducted using the TOPFlash assay in HEK293 cells, and hits were tested for the ability to promote hair growth in cell-based and mouse models. Extracts from Aconitum ciliare were among the most active both in the TOPFlash and hair growth assays, positioning this medicinal plant for the identification of a promising Wnt activator [78]. Flavonoids from the plant Vernonia anthelmintica and their derivative emerged as Wnt pathway activators for melanin synthesis in vitiligo—a sickness manifested as skin depigmentation [41]. As a potential mechanism, phosphorylation and thus inhibition of GSK3β via crosstalk with the PI3K/Akt pathway was pinpointed [41]. In this context, it is interesting to mention that tobacco smoking-caused skin pigmentation was shown to increase β-catenin levels, the activity linked to the tobacco plant (Nicotiana tabacum) metabolites [79].
[...]
Extracts of Undariopsis peterseniana, edible brown algae, were tested in hair growth models in a search for drug candidates against androgenic alopecia and found to stimulate ex vivo hair-fiber growth in rat vibrissa follicles as well as in vivo hair growth in mice. It showed an increase in β-catenin accumulation and GSK3β phosphorylation in dermal papilla cells [98].'
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7140537/
https://www.mdpi.com/2073-4409/9/3/589/pdf
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