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Potassium usnate, a water-soluble usnic acid salt, shows enhanced bioavailability and inhibits invasion and metastasis in colorectal cancer

Yang, Yi ; Bae, Woo Kyun ; Lee, Ji-Yoon ; Choi, Yong Jae ; Lee, Kyung Hwa ; Park, Myong-Suk ; Yu, Young Hyun ; Park, So-Yeon ; Zhou, Rui and Taş, İsa LU , et al. (2018) In Scientific Reports 8. p.1-11
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... (More)

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.

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publishing date
type
Contribution to journal
publication status
published
keywords
Administration, Oral, Animals, Antineoplastic Agents/administration & dosage, Benzofurans/administration & dosage, Biological Availability, Cell Line, Tumor/transplantation, Cell Movement/drug effects, Cell Proliferation/drug effects, Colorectal Neoplasms/drug therapy, Disease Models, Animal, Drug Screening Assays, Antitumor, Epithelial-Mesenchymal Transition/drug effects, Gene Expression Regulation, Neoplastic/drug effects, Humans, Male, Mice, Neoplasm Invasiveness/pathology, Potassium/chemistry, Selenic Acid/administration & dosage, Treatment Outcome
in
Scientific Reports
volume
8
article number
16234
pages
1 - 11
publisher
Nature Publishing Group
external identifiers
  • scopus:85056060587
  • pmid:30390003
ISSN
2045-2322
DOI
10.1038/s41598-018-34709-9
language
English
LU publication?
no
id
e4eed27c-c3a5-4866-a28a-da6dde8f6595
date added to LUP
2022-08-25 14:37:12
date last changed
2024-04-03 09:35:20
@article{e4eed27c-c3a5-4866-a28a-da6dde8f6595,
  abstract     = {{<p>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.</p>}},
  author       = {{Yang, Yi and Bae, Woo Kyun and Lee, Ji-Yoon and Choi, Yong Jae and Lee, Kyung Hwa and Park, Myong-Suk and Yu, Young Hyun and Park, So-Yeon and Zhou, Rui and Taş, İsa and Gamage, Chathurika and Paik, Man-Jeong and Lee, Jae Hyuk and Chung, Ik Joo and Kim, Kyung Keun and Hur, Jae-Seoun and Kim, Sang Kyum and Ha, Hyung-Ho and Kim, Hangun}},
  issn         = {{2045-2322}},
  keywords     = {{Administration, Oral; Animals; Antineoplastic Agents/administration & dosage; Benzofurans/administration & dosage; Biological Availability; Cell Line, Tumor/transplantation; Cell Movement/drug effects; Cell Proliferation/drug effects; Colorectal Neoplasms/drug therapy; Disease Models, Animal; Drug Screening Assays, Antitumor; Epithelial-Mesenchymal Transition/drug effects; Gene Expression Regulation, Neoplastic/drug effects; Humans; Male; Mice; Neoplasm Invasiveness/pathology; Potassium/chemistry; Selenic Acid/administration & dosage; Treatment Outcome}},
  language     = {{eng}},
  month        = {{11}},
  pages        = {{1--11}},
  publisher    = {{Nature Publishing Group}},
  series       = {{Scientific Reports}},
  title        = {{Potassium usnate, a water-soluble usnic acid salt, shows enhanced bioavailability and inhibits invasion and metastasis in colorectal cancer}},
  url          = {{http://dx.doi.org/10.1038/s41598-018-34709-9}},
  doi          = {{10.1038/s41598-018-34709-9}},
  volume       = {{8}},
  year         = {{2018}},
}