Antiplasmodial activity of targeted zinc(II)-dipicolylamine complexes
[Display omitted] This study measured the antiplasmodial activity of nine zinc-dipicolylamine (ZnDPA) complexes against three strains of Plasmodium falciparum, the causative parasite of malaria. Growth inhibition assays showed significant activity against all tested strains, with 50% inhibitory conc...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2017-05, Vol.25 (10), p.2754-2760 |
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| container_title | Bioorganic & medicinal chemistry |
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| creator | Rice, Douglas R. de Lourdes Betancourt Mendiola, María Murillo-Solano, Claribel Checkley, Lisa A. Ferdig, Michael T. Pizarro, Juan C. Smith, Bradley D. |
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This study measured the antiplasmodial activity of nine zinc-dipicolylamine (ZnDPA) complexes against three strains of Plasmodium falciparum, the causative parasite of malaria. Growth inhibition assays showed significant activity against all tested strains, with 50% inhibitory concentrations between 5 and 600nM and almost no toxic effect against host cells including healthy red blood cells. Fluorescence microscopy studies with a green-fluorescent ZnDPA probe showed selective targeting of infected red blood cells. The results suggest that ZnDPA coordination complexes are promising antiplasmodial agents with potential for targeted malaria treatment. |
| doi_str_mv | 10.1016/j.bmc.2017.03.050 |
| format | Article |
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This study measured the antiplasmodial activity of nine zinc-dipicolylamine (ZnDPA) complexes against three strains of Plasmodium falciparum, the causative parasite of malaria. Growth inhibition assays showed significant activity against all tested strains, with 50% inhibitory concentrations between 5 and 600nM and almost no toxic effect against host cells including healthy red blood cells. Fluorescence microscopy studies with a green-fluorescent ZnDPA probe showed selective targeting of infected red blood cells. The results suggest that ZnDPA coordination complexes are promising antiplasmodial agents with potential for targeted malaria treatment.</description><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmc.2017.03.050</identifier><identifier>PMID: 28377170</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Animals ; Antimalarials - chemical synthesis ; Antimalarials - chemistry ; Antimalarials - therapeutic use ; Antimalarials - toxicity ; Antiplasmodial drugs ; Cell Proliferation - drug effects ; CHO Cells ; Coordination Complexes - chemical synthesis ; Coordination Complexes - chemistry ; Coordination Complexes - therapeutic use ; Coordination Complexes - toxicity ; Cricetinae ; Cricetulus ; Erythrocytes - drug effects ; Erythrocytes - parasitology ; Fluorescence microscopy ; Hemolysis - drug effects ; Humans ; Malaria ; Malaria - drug therapy ; Microscopy, Fluorescence ; Organometallic Compounds - chemistry ; Picolines - chemistry ; Plasmodium falciparum - drug effects ; Zinc dipicolylamine</subject><ispartof>Bioorganic & medicinal chemistry, 2017-05, Vol.25 (10), p.2754-2760</ispartof><rights>2017 Elsevier Ltd</rights><rights>Copyright © 2017 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c451t-dcb19e1a9859c7c4faed9a8d512c2c1d2a884e5d9167405ed7908d8989a610cf3</citedby><cites>FETCH-LOGICAL-c451t-dcb19e1a9859c7c4faed9a8d512c2c1d2a884e5d9167405ed7908d8989a610cf3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S096808961730295X$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>230,314,776,780,881,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/28377170$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Rice, Douglas R.</creatorcontrib><creatorcontrib>de Lourdes Betancourt Mendiola, María</creatorcontrib><creatorcontrib>Murillo-Solano, Claribel</creatorcontrib><creatorcontrib>Checkley, Lisa A.</creatorcontrib><creatorcontrib>Ferdig, Michael T.</creatorcontrib><creatorcontrib>Pizarro, Juan C.</creatorcontrib><creatorcontrib>Smith, Bradley D.</creatorcontrib><title>Antiplasmodial activity of targeted zinc(II)-dipicolylamine complexes</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem</addtitle><description>[Display omitted]
This study measured the antiplasmodial activity of nine zinc-dipicolylamine (ZnDPA) complexes against three strains of Plasmodium falciparum, the causative parasite of malaria. Growth inhibition assays showed significant activity against all tested strains, with 50% inhibitory concentrations between 5 and 600nM and almost no toxic effect against host cells including healthy red blood cells. Fluorescence microscopy studies with a green-fluorescent ZnDPA probe showed selective targeting of infected red blood cells. The results suggest that ZnDPA coordination complexes are promising antiplasmodial agents with potential for targeted malaria treatment.</description><subject>Animals</subject><subject>Antimalarials - chemical synthesis</subject><subject>Antimalarials - chemistry</subject><subject>Antimalarials - therapeutic use</subject><subject>Antimalarials - toxicity</subject><subject>Antiplasmodial drugs</subject><subject>Cell Proliferation - drug effects</subject><subject>CHO Cells</subject><subject>Coordination Complexes - chemical synthesis</subject><subject>Coordination Complexes - chemistry</subject><subject>Coordination Complexes - therapeutic use</subject><subject>Coordination Complexes - toxicity</subject><subject>Cricetinae</subject><subject>Cricetulus</subject><subject>Erythrocytes - drug effects</subject><subject>Erythrocytes - parasitology</subject><subject>Fluorescence microscopy</subject><subject>Hemolysis - drug effects</subject><subject>Humans</subject><subject>Malaria</subject><subject>Malaria - drug therapy</subject><subject>Microscopy, Fluorescence</subject><subject>Organometallic Compounds - chemistry</subject><subject>Picolines - chemistry</subject><subject>Plasmodium falciparum - drug effects</subject><subject>Zinc dipicolylamine</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1Lw0AQhhdRtFZ_gBfJUQ-JM8km2UUQivhRKHjR87KdneiWfJHEYv31RqqiF09zmPd9hnmEOEGIEDC7WEXLiqIYMI8giSCFHTFBmckwSTTuignoTIWgdHYgDvt-BQCx1LgvDmKV5DnmMBE3s3rwbWn7qnHeloGlwa_9sAmaIhhs98wDu-Dd13Q2n5-HzreemnJT2srXHFBTtSW_cX8k9gpb9nz8Nafi6fbm8fo-XDzcza9ni5BkikPoaIma0WqVaspJFpadtsqlGFNM6GKrlOTUacxyCSm7XINySittMwQqkqm42nLb12XFjrgeOluatvOV7Tamsd783dT-xTw3a5NKmSQyGwG4BVDX9H3HxU8XwXw6NSszOjWfTg0kZnQ6dk5_H_1pfEscA5fbAI-vrz13pifPNbHzHdNgXOP_wX8AGvqJbg</recordid><startdate>20170515</startdate><enddate>20170515</enddate><creator>Rice, Douglas R.</creator><creator>de Lourdes Betancourt Mendiola, María</creator><creator>Murillo-Solano, Claribel</creator><creator>Checkley, Lisa A.</creator><creator>Ferdig, Michael T.</creator><creator>Pizarro, Juan C.</creator><creator>Smith, Bradley D.</creator><general>Elsevier Ltd</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>5PM</scope></search><sort><creationdate>20170515</creationdate><title>Antiplasmodial activity of targeted zinc(II)-dipicolylamine complexes</title><author>Rice, Douglas R. ; de Lourdes Betancourt Mendiola, María ; Murillo-Solano, Claribel ; Checkley, Lisa A. ; Ferdig, Michael T. ; Pizarro, Juan C. ; Smith, Bradley D.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c451t-dcb19e1a9859c7c4faed9a8d512c2c1d2a884e5d9167405ed7908d8989a610cf3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Animals</topic><topic>Antimalarials - chemical synthesis</topic><topic>Antimalarials - chemistry</topic><topic>Antimalarials - therapeutic use</topic><topic>Antimalarials - toxicity</topic><topic>Antiplasmodial drugs</topic><topic>Cell Proliferation - drug effects</topic><topic>CHO Cells</topic><topic>Coordination Complexes - chemical synthesis</topic><topic>Coordination Complexes - chemistry</topic><topic>Coordination Complexes - therapeutic use</topic><topic>Coordination Complexes - toxicity</topic><topic>Cricetinae</topic><topic>Cricetulus</topic><topic>Erythrocytes - drug effects</topic><topic>Erythrocytes - parasitology</topic><topic>Fluorescence microscopy</topic><topic>Hemolysis - drug effects</topic><topic>Humans</topic><topic>Malaria</topic><topic>Malaria - drug therapy</topic><topic>Microscopy, Fluorescence</topic><topic>Organometallic Compounds - chemistry</topic><topic>Picolines - chemistry</topic><topic>Plasmodium falciparum - drug effects</topic><topic>Zinc dipicolylamine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Rice, Douglas R.</creatorcontrib><creatorcontrib>de Lourdes Betancourt Mendiola, María</creatorcontrib><creatorcontrib>Murillo-Solano, Claribel</creatorcontrib><creatorcontrib>Checkley, Lisa A.</creatorcontrib><creatorcontrib>Ferdig, Michael T.</creatorcontrib><creatorcontrib>Pizarro, Juan C.</creatorcontrib><creatorcontrib>Smith, Bradley D.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Rice, Douglas R.</au><au>de Lourdes Betancourt Mendiola, María</au><au>Murillo-Solano, Claribel</au><au>Checkley, Lisa A.</au><au>Ferdig, Michael T.</au><au>Pizarro, Juan C.</au><au>Smith, Bradley D.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Antiplasmodial activity of targeted zinc(II)-dipicolylamine complexes</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem</addtitle><date>2017-05-15</date><risdate>2017</risdate><volume>25</volume><issue>10</issue><spage>2754</spage><epage>2760</epage><pages>2754-2760</pages><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>[Display omitted]
This study measured the antiplasmodial activity of nine zinc-dipicolylamine (ZnDPA) complexes against three strains of Plasmodium falciparum, the causative parasite of malaria. Growth inhibition assays showed significant activity against all tested strains, with 50% inhibitory concentrations between 5 and 600nM and almost no toxic effect against host cells including healthy red blood cells. Fluorescence microscopy studies with a green-fluorescent ZnDPA probe showed selective targeting of infected red blood cells. The results suggest that ZnDPA coordination complexes are promising antiplasmodial agents with potential for targeted malaria treatment.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>28377170</pmid><doi>10.1016/j.bmc.2017.03.050</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - therapeutic use Antimalarials - toxicity Antiplasmodial drugs Cell Proliferation - drug effects CHO Cells Coordination Complexes - chemical synthesis Coordination Complexes - chemistry Coordination Complexes - therapeutic use Coordination Complexes - toxicity Cricetinae Cricetulus Erythrocytes - drug effects Erythrocytes - parasitology Fluorescence microscopy Hemolysis - drug effects Humans Malaria Malaria - drug therapy Microscopy, Fluorescence Organometallic Compounds - chemistry Picolines - chemistry Plasmodium falciparum - drug effects Zinc dipicolylamine |
| title | Antiplasmodial activity of targeted zinc(II)-dipicolylamine complexes |
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