Inhibition of ANO1 by luteolin and its cytotoxicity in human prostate cancer PC-3 cells

Yohan Seo, Kunhi Ryu, Jinhong Park, Dong Kyu Jeon, Sungwoo Jo, Ho K. Lee, Wan Namkung

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

Anoctamin 1 (ANO1), a calcium-activated chloride channel, is highly amplified in prostate cancer, the most common form of cancer and leading causes of cancer death in men, and downregulation of ANO1 expression or its functional activity is known to inhibit cell proliferation, migration and invasion in prostate cancer cells. Here, we performed a cell-based screening for the identification of ANO1 inhibitors as potential anticancer therapeutic agents for prostate cancer. Screening of 300 selected bioactive natural products revealed that luteolin is a novel potent inhibitor of ANO1. Electrophysiological studies indicated that luteolin potently inhibited ANO1 chloride channel activity in a dose-dependent manner with an IC50 value of 9.8 μM and luteolin did not alter intracellular calcium signaling in PC-3 prostate cancer cells. Luteolin inhibited cell proliferation and migration of PC-3 cells expressing high levels of ANO1 more potently than that of ANO1-deficient PC-3 cells. Notably, luteolin not only inhibited ANO1 channel activity, but also strongly decreased protein expression levels of ANO1. Our results suggest that downregulation of ANO1 by luteolin is a potential mechanism for the anticancer effect of luteolin.

Original languageEnglish
Article numbere0174935
JournalPloS one
Volume12
Issue number3
DOIs
Publication statusPublished - 2017 Mar 1

Fingerprint

Luteolin
luteolin
prostatic neoplasms
Cytotoxicity
cytotoxicity
Prostatic Neoplasms
chloride channels
cells
Chloride Channels
Cells
Cell proliferation
Cell Movement
cell proliferation
Screening
Down-Regulation
Cell Proliferation
screening
neoplasms
Calcium Signaling
Biological Products

All Science Journal Classification (ASJC) codes

  • Biochemistry, Genetics and Molecular Biology(all)
  • Agricultural and Biological Sciences(all)

Cite this

Seo, Yohan ; Ryu, Kunhi ; Park, Jinhong ; Jeon, Dong Kyu ; Jo, Sungwoo ; Lee, Ho K. ; Namkung, Wan. / Inhibition of ANO1 by luteolin and its cytotoxicity in human prostate cancer PC-3 cells. In: PloS one. 2017 ; Vol. 12, No. 3.
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Inhibition of ANO1 by luteolin and its cytotoxicity in human prostate cancer PC-3 cells. / Seo, Yohan; Ryu, Kunhi; Park, Jinhong; Jeon, Dong Kyu; Jo, Sungwoo; Lee, Ho K.; Namkung, Wan.

In: PloS one, Vol. 12, No. 3, e0174935, 01.03.2017.

Research output: Contribution to journalArticle

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AU - Lee, Ho K.

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