Chloroquine is a zinc ionophore.
Chloroquine is an established antimalarial agent that has been recently tested in clinical trials for its anticancer activity. The favorable effect of chloroquine appears to be due to its ability to sensitize cancerous cells to chemotherapy, radiation therapy, and induce apoptosis. The present study...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Public Library of Science (PLoS)
2014-01-01
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| Series: | PLoS ONE |
| Online Access: | http://europepmc.org/articles/PMC4182877?pdf=render |
| _version_ | 1828420611272081408 |
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| author | Jing Xue Amanda Moyer Bing Peng Jinchang Wu Bethany N Hannafon Wei-Qun Ding |
| author_facet | Jing Xue Amanda Moyer Bing Peng Jinchang Wu Bethany N Hannafon Wei-Qun Ding |
| author_sort | Jing Xue |
| collection | DOAJ |
| description | Chloroquine is an established antimalarial agent that has been recently tested in clinical trials for its anticancer activity. The favorable effect of chloroquine appears to be due to its ability to sensitize cancerous cells to chemotherapy, radiation therapy, and induce apoptosis. The present study investigated the interaction of zinc ions with chloroquine in a human ovarian cancer cell line (A2780). Chloroquine enhanced zinc uptake by A2780 cells in a concentration-dependent manner, as assayed using a fluorescent zinc probe. This enhancement was attenuated by TPEN, a high affinity metal-binding compound, indicating the specificity of the zinc uptake. Furthermore, addition of copper or iron ions had no effect on chloroquine-induced zinc uptake. Fluorescent microscopic examination of intracellular zinc distribution demonstrated that free zinc ions are more concentrated in the lysosomes after addition of chloroquine, which is consistent with previous reports showing that chloroquine inhibits lysosome function. The combination of chloroquine with zinc enhanced chloroquine's cytotoxicity and induced apoptosis in A2780 cells. Thus chloroquine is a zinc ionophore, a property that may contribute to chloroquine's anticancer activity. |
| first_indexed | 2024-12-10T15:16:13Z |
| format | Article |
| id | doaj.art-0cd229fbd9784ee59452981dfb45642f |
| institution | Directory Open Access Journal |
| issn | 1932-6203 |
| language | English |
| last_indexed | 2024-12-10T15:16:13Z |
| publishDate | 2014-01-01 |
| publisher | Public Library of Science (PLoS) |
| record_format | Article |
| series | PLoS ONE |
| spelling | doaj.art-0cd229fbd9784ee59452981dfb45642f2022-12-22T01:43:48ZengPublic Library of Science (PLoS)PLoS ONE1932-62032014-01-01910e10918010.1371/journal.pone.0109180Chloroquine is a zinc ionophore.Jing XueAmanda MoyerBing PengJinchang WuBethany N HannafonWei-Qun DingChloroquine is an established antimalarial agent that has been recently tested in clinical trials for its anticancer activity. The favorable effect of chloroquine appears to be due to its ability to sensitize cancerous cells to chemotherapy, radiation therapy, and induce apoptosis. The present study investigated the interaction of zinc ions with chloroquine in a human ovarian cancer cell line (A2780). Chloroquine enhanced zinc uptake by A2780 cells in a concentration-dependent manner, as assayed using a fluorescent zinc probe. This enhancement was attenuated by TPEN, a high affinity metal-binding compound, indicating the specificity of the zinc uptake. Furthermore, addition of copper or iron ions had no effect on chloroquine-induced zinc uptake. Fluorescent microscopic examination of intracellular zinc distribution demonstrated that free zinc ions are more concentrated in the lysosomes after addition of chloroquine, which is consistent with previous reports showing that chloroquine inhibits lysosome function. The combination of chloroquine with zinc enhanced chloroquine's cytotoxicity and induced apoptosis in A2780 cells. Thus chloroquine is a zinc ionophore, a property that may contribute to chloroquine's anticancer activity.http://europepmc.org/articles/PMC4182877?pdf=render |
| spellingShingle | Jing Xue Amanda Moyer Bing Peng Jinchang Wu Bethany N Hannafon Wei-Qun Ding Chloroquine is a zinc ionophore. PLoS ONE |
| title | Chloroquine is a zinc ionophore. |
| title_full | Chloroquine is a zinc ionophore. |
| title_fullStr | Chloroquine is a zinc ionophore. |
| title_full_unstemmed | Chloroquine is a zinc ionophore. |
| title_short | Chloroquine is a zinc ionophore. |
| title_sort | chloroquine is a zinc ionophore |
| url | http://europepmc.org/articles/PMC4182877?pdf=render |
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