Inhibition of ANO1 by Cis - and Trans -Resveratrol and Their Anticancer Activity in Human Prostate Cancer PC-3 Cells

Anoctamin1 (ANO1), a calcium-activated chloride channel, is involved in the proliferation, migration, and invasion of various cancer cells including head and neck squamous cell carcinoma, lung cancer, and prostate cancer. Inhibition of ANO1 activity or downregulation of ANO1 expression in these canc...

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Veröffentlicht in:International journal of molecular sciences 2023-01, Vol.24 (2), p.1186
Hauptverfasser: Jeon, Dongkyu, Jo, Minjae, Lee, Yechan, Park, So-Hyeon, Phan, Hong Thi Lam, Nam, Joo Hyun, Namkung, Wan
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container_title International journal of molecular sciences
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Jo, Minjae
Lee, Yechan
Park, So-Hyeon
Phan, Hong Thi Lam
Nam, Joo Hyun
Namkung, Wan
description Anoctamin1 (ANO1), a calcium-activated chloride channel, is involved in the proliferation, migration, and invasion of various cancer cells including head and neck squamous cell carcinoma, lung cancer, and prostate cancer. Inhibition of ANO1 activity or downregulation of ANO1 expression in these cancer cells is known to exhibit anticancer effects. Resveratrol, a natural polyphenol abundant in wines, grapes, berries, soybeans, and peanuts, shows a wide variety of biological effects including anti-inflammatory, antioxidant, and anticancer activities. In this study, we investigated the effects of two stereoisomers of resveratrol on ANO1 activity and found that - and -resveratrol inhibited ANO1 activity with different potencies. - and -resveratrol inhibited ANO1 channel activity with IC values of 10.6 and 102 μM, respectively, and had no significant effect on intracellular calcium signaling at 10 and 100 μM, respectively. In addition, -resveratrol downregulated mRNA and protein expression levels of ANO1 more potently than -resveratrol in PC-3 prostate cancer cells. - and -resveratrol significantly reduced cell proliferation and cell migration in an ANO1-dependent manner, and both resveratrol isomers strongly increased caspase-3 activity, PARP cleavage, and apoptotic sub-G1 phase ratio in PC-3 cells. These results revealed that -resveratrol is a potent inhibitor of ANO1 and exhibits ANO1-dependent anticancer activity against human metastatic prostate cancer PC-3 cells.
doi_str_mv 10.3390/ijms24021186
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Inhibition of ANO1 activity or downregulation of ANO1 expression in these cancer cells is known to exhibit anticancer effects. Resveratrol, a natural polyphenol abundant in wines, grapes, berries, soybeans, and peanuts, shows a wide variety of biological effects including anti-inflammatory, antioxidant, and anticancer activities. In this study, we investigated the effects of two stereoisomers of resveratrol on ANO1 activity and found that - and -resveratrol inhibited ANO1 activity with different potencies. - and -resveratrol inhibited ANO1 channel activity with IC values of 10.6 and 102 μM, respectively, and had no significant effect on intracellular calcium signaling at 10 and 100 μM, respectively. In addition, -resveratrol downregulated mRNA and protein expression levels of ANO1 more potently than -resveratrol in PC-3 prostate cancer cells. - and -resveratrol significantly reduced cell proliferation and cell migration in an ANO1-dependent manner, and both resveratrol isomers strongly increased caspase-3 activity, PARP cleavage, and apoptotic sub-G1 phase ratio in PC-3 cells. 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Inhibition of ANO1 activity or downregulation of ANO1 expression in these cancer cells is known to exhibit anticancer effects. Resveratrol, a natural polyphenol abundant in wines, grapes, berries, soybeans, and peanuts, shows a wide variety of biological effects including anti-inflammatory, antioxidant, and anticancer activities. In this study, we investigated the effects of two stereoisomers of resveratrol on ANO1 activity and found that - and -resveratrol inhibited ANO1 activity with different potencies. - and -resveratrol inhibited ANO1 channel activity with IC values of 10.6 and 102 μM, respectively, and had no significant effect on intracellular calcium signaling at 10 and 100 μM, respectively. In addition, -resveratrol downregulated mRNA and protein expression levels of ANO1 more potently than -resveratrol in PC-3 prostate cancer cells. - and -resveratrol significantly reduced cell proliferation and cell migration in an ANO1-dependent manner, and both resveratrol isomers strongly increased caspase-3 activity, PARP cleavage, and apoptotic sub-G1 phase ratio in PC-3 cells. 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source MDPI - Multidisciplinary Digital Publishing Institute; MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; PubMed Central
subjects Anoctamin-1 - metabolism
Antitumor activity
Apoptosis
Biological effects
Calcium
Calcium (intracellular)
Calcium chloride
Calcium signalling
Caspase-3
Cell adhesion & migration
Cell growth
Cell proliferation
Channel gating
Chloride
Chloride channels (calcium-gated)
G1 phase
Gene expression
Head & neck cancer
Head and Neck Neoplasms
Humans
Inflammation
Intracellular signalling
Investigations
Isomers
Lung cancer
Lung carcinoma
Male
Metastases
Metastasis
mRNA
Neoplasm Proteins - metabolism
Pancreatic cancer
PC-3 Cells
Phase ratio
Prostate cancer
Prostatic Neoplasms - drug therapy
Prostatic Neoplasms - metabolism
Protein expression
Proteins
Resveratrol
Resveratrol - pharmacology
Squamous cell carcinoma
Stereoisomerism
Stereoisomers
title Inhibition of ANO1 by Cis - and Trans -Resveratrol and Their Anticancer Activity in Human Prostate Cancer PC-3 Cells
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