Labelling of bleomycin with Auger-emitter increases cytotoxicity in squamous-cell cancer cell lines
Purpose: To investigate the cytotoxicity of bleomycin (BLM), two Auger-emitting bleomycin complexes (indium-111 (111In)-BLMC) and 111InCl3 in three squamous cell cancer (SCC) cell lines. Material and methods: Three recently established SCC cell lines were investigated using the 96-well clonogenic as...
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| Veröffentlicht in: | International journal of radiation biology 1998-05, Vol.73 (5), p.565-570 |
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| container_title | International journal of radiation biology |
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| creator | Jääskelä-Saari, H A Kairemo, K J Ramsay, H A Grénman, R |
| description | Purpose: To investigate the cytotoxicity of bleomycin (BLM), two Auger-emitting bleomycin complexes (indium-111 (111In)-BLMC) and 111InCl3 in three squamous cell cancer (SCC) cell lines. Material and methods: Three recently established SCC cell lines were investigated using the 96-well clonogenic assay. Concentrations causing 50% inhibition in cell survival (IC) were calculated for BLM and two specific activities of 111In BLMC (40 MBq/mg BLM (low) and 195 MBq/mg BLM (high)). Results: 111In-BLMC (low) was the most toxic to the SCC cell lines. 111In-BLMC containing 4.9-fold more activity of 111In (195 MBq/mg BLM) was more effective than BLM (p=0.0029), but not as toxic as 111In-BLMC (low) (p=0.0023). UT-SCC-19A had a IC50 value for BLM as low as 4.1 nm, whereas IC50 values for 111In-BLMC (low) and 111In-BLMC (high) were 2.0 nm and 2.6 nm, respectively. The most chemoresistant cell line UT-SCC-12A had a IC value for BLM of 18.8 nm, for 111In50 BLMC (low) 10.7 nm and for 111In-BLMC (high) 12.7 nm. 111InCl3 had no cell killing effect. Conclusions: This study shows that 111In-BLMC is superior in SCC cell killing compared with BLM. These data provide the basis for further clinical investigations of 111In-BLMC. |
| doi_str_mv | 10.1080/095530098142121 |
| format | Article |
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Material and methods: Three recently established SCC cell lines were investigated using the 96-well clonogenic assay. Concentrations causing 50% inhibition in cell survival (IC) were calculated for BLM and two specific activities of 111In BLMC (40 MBq/mg BLM (low) and 195 MBq/mg BLM (high)). Results: 111In-BLMC (low) was the most toxic to the SCC cell lines. 111In-BLMC containing 4.9-fold more activity of 111In (195 MBq/mg BLM) was more effective than BLM (p=0.0029), but not as toxic as 111In-BLMC (low) (p=0.0023). UT-SCC-19A had a IC50 value for BLM as low as 4.1 nm, whereas IC50 values for 111In-BLMC (low) and 111In-BLMC (high) were 2.0 nm and 2.6 nm, respectively. The most chemoresistant cell line UT-SCC-12A had a IC value for BLM of 18.8 nm, for 111In50 BLMC (low) 10.7 nm and for 111In-BLMC (high) 12.7 nm. 111InCl3 had no cell killing effect. Conclusions: This study shows that 111In-BLMC is superior in SCC cell killing compared with BLM. These data provide the basis for further clinical investigations of 111In-BLMC.</description><identifier>ISSN: 0955-3002</identifier><identifier>EISSN: 1362-3095</identifier><identifier>DOI: 10.1080/095530098142121</identifier><identifier>PMID: 9652815</identifier><language>eng</language><publisher>London: Informa UK Ltd</publisher><subject>Antimetabolites, Antineoplastic - pharmacology ; Biological and medical sciences ; Bleomycin - pharmacology ; Carcinogenesis, carcinogens and anticarcinogens ; Carcinoma, Squamous Cell - drug therapy ; Carcinoma, Squamous Cell - radiotherapy ; Combined Modality Therapy ; Drug Screening Assays, Antitumor ; Head and Neck Neoplasms - drug therapy ; Head and Neck Neoplasms - radiotherapy ; Humans ; Indium - administration & dosage ; Indium - pharmacology ; Indium Radioisotopes - pharmacology ; Isotope Labeling ; Medical sciences ; Physical agents ; Tumor Cells, Cultured - radiation effects ; Tumors</subject><ispartof>International journal of radiation biology, 1998-05, Vol.73 (5), p.565-570</ispartof><rights>1998 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted 1998</rights><rights>1998 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c453t-552ed795807dc0ff1defdda11fafe3ac78dd40a88326754a67f8a448473c78343</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.1080/095530098142121$$EPDF$$P50$$Ginformahealthcare$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.1080/095530098142121$$EHTML$$P50$$Ginformahealthcare$$H</linktohtml><link.rule.ids>314,776,780,27903,27904,59624,59730,60413,60519,61198,61233,61379,61414</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2261322$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9652815$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Jääskelä-Saari, H A</creatorcontrib><creatorcontrib>Kairemo, K J</creatorcontrib><creatorcontrib>Ramsay, H A</creatorcontrib><creatorcontrib>Grénman, R</creatorcontrib><title>Labelling of bleomycin with Auger-emitter increases cytotoxicity in squamous-cell cancer cell lines</title><title>International journal of radiation biology</title><addtitle>Int J Radiat Biol</addtitle><description>Purpose: To investigate the cytotoxicity of bleomycin (BLM), two Auger-emitting bleomycin complexes (indium-111 (111In)-BLMC) and 111InCl3 in three squamous cell cancer (SCC) cell lines. Material and methods: Three recently established SCC cell lines were investigated using the 96-well clonogenic assay. Concentrations causing 50% inhibition in cell survival (IC) were calculated for BLM and two specific activities of 111In BLMC (40 MBq/mg BLM (low) and 195 MBq/mg BLM (high)). Results: 111In-BLMC (low) was the most toxic to the SCC cell lines. 111In-BLMC containing 4.9-fold more activity of 111In (195 MBq/mg BLM) was more effective than BLM (p=0.0029), but not as toxic as 111In-BLMC (low) (p=0.0023). UT-SCC-19A had a IC50 value for BLM as low as 4.1 nm, whereas IC50 values for 111In-BLMC (low) and 111In-BLMC (high) were 2.0 nm and 2.6 nm, respectively. The most chemoresistant cell line UT-SCC-12A had a IC value for BLM of 18.8 nm, for 111In50 BLMC (low) 10.7 nm and for 111In-BLMC (high) 12.7 nm. 111InCl3 had no cell killing effect. Conclusions: This study shows that 111In-BLMC is superior in SCC cell killing compared with BLM. These data provide the basis for further clinical investigations of 111In-BLMC.</description><subject>Antimetabolites, Antineoplastic - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Bleomycin - pharmacology</subject><subject>Carcinogenesis, carcinogens and anticarcinogens</subject><subject>Carcinoma, Squamous Cell - drug therapy</subject><subject>Carcinoma, Squamous Cell - radiotherapy</subject><subject>Combined Modality Therapy</subject><subject>Drug Screening Assays, Antitumor</subject><subject>Head and Neck Neoplasms - drug therapy</subject><subject>Head and Neck Neoplasms - radiotherapy</subject><subject>Humans</subject><subject>Indium - administration & dosage</subject><subject>Indium - pharmacology</subject><subject>Indium Radioisotopes - pharmacology</subject><subject>Isotope Labeling</subject><subject>Medical sciences</subject><subject>Physical agents</subject><subject>Tumor Cells, Cultured - radiation effects</subject><subject>Tumors</subject><issn>0955-3002</issn><issn>1362-3095</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kM1r3DAQxUVpSbZJzj0VfCi9udGnLfcWlvQDFnppz2ZWGmUVbCuRZBL_99F2t4EUcpph3m8ej0fIB0a_MKrpJe2UEpR2mknOOHtDVkw0vBbl_pas9mrZKT8l71O6pWWjQp-Qk65RXDO1ImYDWxwGP91UwVXbAcO4GD9VDz7vqqv5BmONo88ZY-UnExESpsosOeTw6I3PSzlX6X6GMcypNsWqMjCZgv_dizGmc_LOwZDw4jjPyJ9v17_XP-rNr-8_11eb2kglcq0UR9t2StPWGuocs-isBcYcOBRgWm2tpKC14E2rJDSt0yCllq0ompDijHw--N7FcD9jyv3o0z4GTFjS9ayRkgquCnh5AE0MKUV0_V30I8SlZ7Tf19r_V2v5-Hi0nrcj2mf-2GPRPx11SAYGF0sHPj1jnDdMcF6wrwfMTy7EER5CHGyfYRlC_PcjXs_QvXjeIQx5ZyBifxvmOJVqX83_BJYRpKE</recordid><startdate>19980501</startdate><enddate>19980501</enddate><creator>Jääskelä-Saari, H A</creator><creator>Kairemo, K J</creator><creator>Ramsay, H A</creator><creator>Grénman, R</creator><general>Informa UK Ltd</general><general>Taylor & Francis</general><scope>IQODW</scope><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>7U7</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>P64</scope><scope>RC3</scope></search><sort><creationdate>19980501</creationdate><title>Labelling of bleomycin with Auger-emitter increases cytotoxicity in squamous-cell cancer cell lines</title><author>Jääskelä-Saari, H A ; Kairemo, K J ; Ramsay, H A ; Grénman, R</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c453t-552ed795807dc0ff1defdda11fafe3ac78dd40a88326754a67f8a448473c78343</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Antimetabolites, Antineoplastic - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Bleomycin - pharmacology</topic><topic>Carcinogenesis, carcinogens and anticarcinogens</topic><topic>Carcinoma, Squamous Cell - drug therapy</topic><topic>Carcinoma, Squamous Cell - radiotherapy</topic><topic>Combined Modality Therapy</topic><topic>Drug Screening Assays, Antitumor</topic><topic>Head and Neck Neoplasms - drug therapy</topic><topic>Head and Neck Neoplasms - radiotherapy</topic><topic>Humans</topic><topic>Indium - administration & dosage</topic><topic>Indium - pharmacology</topic><topic>Indium Radioisotopes - pharmacology</topic><topic>Isotope Labeling</topic><topic>Medical sciences</topic><topic>Physical agents</topic><topic>Tumor Cells, Cultured - radiation effects</topic><topic>Tumors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Jääskelä-Saari, H A</creatorcontrib><creatorcontrib>Kairemo, K J</creatorcontrib><creatorcontrib>Ramsay, H A</creatorcontrib><creatorcontrib>Grénman, R</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Toxicology Abstracts</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Genetics Abstracts</collection><jtitle>International journal of radiation biology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Jääskelä-Saari, H A</au><au>Kairemo, K J</au><au>Ramsay, H A</au><au>Grénman, R</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Labelling of bleomycin with Auger-emitter increases cytotoxicity in squamous-cell cancer cell lines</atitle><jtitle>International journal of radiation biology</jtitle><addtitle>Int J Radiat Biol</addtitle><date>1998-05-01</date><risdate>1998</risdate><volume>73</volume><issue>5</issue><spage>565</spage><epage>570</epage><pages>565-570</pages><issn>0955-3002</issn><eissn>1362-3095</eissn><abstract>Purpose: To investigate the cytotoxicity of bleomycin (BLM), two Auger-emitting bleomycin complexes (indium-111 (111In)-BLMC) and 111InCl3 in three squamous cell cancer (SCC) cell lines. Material and methods: Three recently established SCC cell lines were investigated using the 96-well clonogenic assay. Concentrations causing 50% inhibition in cell survival (IC) were calculated for BLM and two specific activities of 111In BLMC (40 MBq/mg BLM (low) and 195 MBq/mg BLM (high)). Results: 111In-BLMC (low) was the most toxic to the SCC cell lines. 111In-BLMC containing 4.9-fold more activity of 111In (195 MBq/mg BLM) was more effective than BLM (p=0.0029), but not as toxic as 111In-BLMC (low) (p=0.0023). UT-SCC-19A had a IC50 value for BLM as low as 4.1 nm, whereas IC50 values for 111In-BLMC (low) and 111In-BLMC (high) were 2.0 nm and 2.6 nm, respectively. The most chemoresistant cell line UT-SCC-12A had a IC value for BLM of 18.8 nm, for 111In50 BLMC (low) 10.7 nm and for 111In-BLMC (high) 12.7 nm. 111InCl3 had no cell killing effect. Conclusions: This study shows that 111In-BLMC is superior in SCC cell killing compared with BLM. These data provide the basis for further clinical investigations of 111In-BLMC.</abstract><cop>London</cop><pub>Informa UK Ltd</pub><pmid>9652815</pmid><doi>10.1080/095530098142121</doi><tpages>6</tpages></addata></record> |
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| ispartof | International journal of radiation biology, 1998-05, Vol.73 (5), p.565-570 |
| issn | 0955-3002 1362-3095 |
| language | eng |
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| source | MEDLINE; Taylor & Francis Medical Library - CRKN; Taylor & Francis Journals Complete |
| subjects | Antimetabolites, Antineoplastic - pharmacology Biological and medical sciences Bleomycin - pharmacology Carcinogenesis, carcinogens and anticarcinogens Carcinoma, Squamous Cell - drug therapy Carcinoma, Squamous Cell - radiotherapy Combined Modality Therapy Drug Screening Assays, Antitumor Head and Neck Neoplasms - drug therapy Head and Neck Neoplasms - radiotherapy Humans Indium - administration & dosage Indium - pharmacology Indium Radioisotopes - pharmacology Isotope Labeling Medical sciences Physical agents Tumor Cells, Cultured - radiation effects Tumors |
| title | Labelling of bleomycin with Auger-emitter increases cytotoxicity in squamous-cell cancer cell lines |
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