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Development and synthesis of diffractaic acid analogs as potent inhibitors of colorectal cancer stem cell traits
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Development and synthesis of diffractaic acid analogs as potent inhibitors of colorectal cancer stem cell traits
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Development and synthesis of diffractaic acid analogs as potent inhibitors of colorectal cancer stem cell traits
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Journal Article
Development and synthesis of diffractaic acid analogs as potent inhibitors of colorectal cancer stem cell traits
2025
Overview
In recent years, evidence for the anti-cancer activity of lichen secondary metabolites has been rapidly increasing. In this study, we synthesised analogues of diffractaic acid, a lichen secondary metabolite, and evaluated their ability to suppress colorectal cancer stem potential. Among the 10 compounds after H/CH₃/benzylation of the diffractaic acid structure or modifications in an aromatic hydrophobic domain, TU3 has a more inhibition effect on the stem potential of colorectal cancer compared to other compounds. The compound TU3 targets ALDH1 and suppresses key signalling pathways such as WNT, STAT3, NF-κB, Hedgehog, and AP-1. Inhibition of these signalling pathways by TU3 contribute to attenuate the survival mechanisms of colorectal cancer stem cell and thus inhibit cancer progression.
Publisher
Nature Publishing Group UK,Nature Publishing Group,Nature Portfolio
Subject
/ 631/67
/ 692/4017
/ Acids
/ Aldehyde Dehydrogenase 1 Family
/ ALDH1
/ Antineoplastic Agents - chemical synthesis
/ Antineoplastic Agents - chemistry
/ Antineoplastic Agents - pharmacology
/ Cancer
/ Cell Proliferation - drug effects
/ Colorectal cancer stem cells
/ Colorectal Neoplasms - drug therapy
/ Colorectal Neoplasms - metabolism
/ Colorectal Neoplasms - pathology
/ Humanities and Social Sciences
/ Humans
/ Lichen secondary metabolites
/ Lichens
/ Melanoma
/ Neoplastic Stem Cells - drug effects
/ Neoplastic Stem Cells - metabolism
/ Neoplastic Stem Cells - pathology
/ Retinal Dehydrogenase - antagonists & inhibitors
/ Retinal Dehydrogenase - metabolism
/ Science
/ Signal Transduction - drug effects
