Abstract
Usnic acid (UA), a lichen secondary substance, has considerable anticancer activity in vitro, whereas its effect in vivo is limited. Here, potassium usnate (KU) was prepared by the salinization of UA to enhance its water solubility. KU showed increased bioavailability compared with UA in the tumor, liver, and plasma of a CT26 syngeneic mouse tumor xenograft model after oral administration, as determined by LC-MS/MS analysis. KU exhibited potent anticancer effects on colorectal cancer cells and inhibited liver metastasis in an orthotopic murine colorectal cancer model. KU treatment downregulated the epithelial-mesenchymal markers Twist, Snail, and Slug and the metastasis-related genes CAPN1, CDC42, CFL1, IGF1, WASF1, and WASL in cells and tumor tissues. The present results suggest the potential application of the water-soluble form of UA, KU, in anticancer therapy.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Administration, Oral
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Animals
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Antineoplastic Agents / administration & dosage*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacokinetics
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Benzofurans / administration & dosage*
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Benzofurans / chemistry
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Benzofurans / pharmacokinetics
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Biological Availability
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Cell Line, Tumor / transplantation
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Cell Movement / drug effects
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Cell Proliferation / drug effects
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Colorectal Neoplasms / drug therapy*
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Colorectal Neoplasms / genetics
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Colorectal Neoplasms / pathology
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Disease Models, Animal
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Drug Screening Assays, Antitumor
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Epithelial-Mesenchymal Transition / drug effects
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Gene Expression Regulation, Neoplastic / drug effects*
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Humans
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Male
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Mice
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Neoplasm Invasiveness / pathology
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Neoplasm Invasiveness / prevention & control
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Potassium / chemistry
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Selenic Acid / administration & dosage
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Selenic Acid / pharmacokinetics*
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Treatment Outcome
Substances
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Antineoplastic Agents
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Benzofurans
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usnic acid
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Selenic Acid
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Potassium