Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug. (-)-C75 has antitumour activity
C75 is a synthetic compound described as having antitumoral properties. It produces hypophagia and weight loss in rodents, limiting its use in cancer therapy but identify- ing it as a potential anti-obesity drug. C75 is a fatty acid synthase (FAS) inhibitor and, through its coenzyme A (CoA) derivati...
| Autores: | , , , , , , , , |
|---|---|
| Tipo de recurso: | artículo |
| Estado: | Versión enviada para evaluación y publicación |
| Fecha de publicación: | 2013 |
| País: | España |
| Institución: | Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya) |
| Repositorio: | Recercat. Dipósit de la Recerca de Catalunya |
| OAI Identifier: | oai:recercat.cat:2445/53049 |
| Acceso en línea: | https://hdl.handle.net/2445/53049 |
| Access Level: | acceso abierto |
| Palabra clave: | Obesitat Càncer Estereoquímica Enantiòmers Medicaments antineoplàstics Obesity Cancer Stereochemistry Enantiomers Antineoplastic agents |
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Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug. (-)-C75 has antitumour activityMakowski, KamilMera Nanín, PaulaParedes Fortuny, DavidHerrero Rodríguez, LauraAriza Piquer, XavierAsins Muñoz, GuillerminaGarcía Hegardt, FaustoGarcía Gómez, JordiSerra i Cucurull, DolorsObesitatCàncerEstereoquímicaEnantiòmersMedicaments antineoplàsticsObesityCancerStereochemistryEnantiomersAntineoplastic agentsC75 is a synthetic compound described as having antitumoral properties. It produces hypophagia and weight loss in rodents, limiting its use in cancer therapy but identify- ing it as a potential anti-obesity drug. C75 is a fatty acid synthase (FAS) inhibitor and, through its coenzyme A (CoA) derivative, it acts as a carnitine palmitoyltransferase (CPT) 1 inhibitor. Racemic mixtures of C75 have been used in all the previous studies; however, the potential dif- ferent biological activities of C75 enantiomers have not been examined yet. To address this question we synthesized the two C75 enantiomers separately. Our results showed that ( )- C75 inhibits FAS activity in vitro and has a cytotoxic effect on tumor cell lines, without affecting food consumption. (+)-C75 inhibits CPT1 and its administration produces anorexia, suggesting that central inhibition of CPT1 is essential for the anorectic effect of C75. The differential activity of C75 enantiomers may lead to the development of potential new specific drugs for cancer and obesity.Wiley2014202220132014info:eu-repo/semantics/articleinfo:eu-repo/semantics/submittedVersion35 p.application/pdfapplication/pdfhttps://hdl.handle.net/2445/53049Articles publicats en revistes (Bioquímica i Biomedicina Molecular)reponame:Recercat. Dipósit de la Recerca de Catalunyainstname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)InglésVersió preprint del document publicat a: http://dx.doi.org/10.1002/chir.22139Chirality, 2013, vol. 25, num. 5, p. 281-287http://dx.doi.org/10.1002/chir.22139(c) Wiley, 2013info:eu-repo/semantics/openAccessoai:recercat.cat:2445/530492026-05-29T05:05:01Z |
| dc.title.none.fl_str_mv |
Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug. (-)-C75 has antitumour activity |
| title |
Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug. (-)-C75 has antitumour activity |
| spellingShingle |
Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug. (-)-C75 has antitumour activity Makowski, Kamil Obesitat Càncer Estereoquímica Enantiòmers Medicaments antineoplàstics Obesity Cancer Stereochemistry Enantiomers Antineoplastic agents |
| title_short |
Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug. (-)-C75 has antitumour activity |
| title_full |
Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug. (-)-C75 has antitumour activity |
| title_fullStr |
Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug. (-)-C75 has antitumour activity |
| title_full_unstemmed |
Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug. (-)-C75 has antitumour activity |
| title_sort |
Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug. (-)-C75 has antitumour activity |
| dc.creator.none.fl_str_mv |
Makowski, Kamil Mera Nanín, Paula Paredes Fortuny, David Herrero Rodríguez, Laura Ariza Piquer, Xavier Asins Muñoz, Guillermina García Hegardt, Fausto García Gómez, Jordi Serra i Cucurull, Dolors |
| author |
Makowski, Kamil |
| author_facet |
Makowski, Kamil Mera Nanín, Paula Paredes Fortuny, David Herrero Rodríguez, Laura Ariza Piquer, Xavier Asins Muñoz, Guillermina García Hegardt, Fausto García Gómez, Jordi Serra i Cucurull, Dolors |
| author_role |
author |
| author2 |
Mera Nanín, Paula Paredes Fortuny, David Herrero Rodríguez, Laura Ariza Piquer, Xavier Asins Muñoz, Guillermina García Hegardt, Fausto García Gómez, Jordi Serra i Cucurull, Dolors |
| author2_role |
author author author author author author author author |
| dc.subject.none.fl_str_mv |
Obesitat Càncer Estereoquímica Enantiòmers Medicaments antineoplàstics Obesity Cancer Stereochemistry Enantiomers Antineoplastic agents |
| topic |
Obesitat Càncer Estereoquímica Enantiòmers Medicaments antineoplàstics Obesity Cancer Stereochemistry Enantiomers Antineoplastic agents |
| description |
C75 is a synthetic compound described as having antitumoral properties. It produces hypophagia and weight loss in rodents, limiting its use in cancer therapy but identify- ing it as a potential anti-obesity drug. C75 is a fatty acid synthase (FAS) inhibitor and, through its coenzyme A (CoA) derivative, it acts as a carnitine palmitoyltransferase (CPT) 1 inhibitor. Racemic mixtures of C75 have been used in all the previous studies; however, the potential dif- ferent biological activities of C75 enantiomers have not been examined yet. To address this question we synthesized the two C75 enantiomers separately. Our results showed that ( )- C75 inhibits FAS activity in vitro and has a cytotoxic effect on tumor cell lines, without affecting food consumption. (+)-C75 inhibits CPT1 and its administration produces anorexia, suggesting that central inhibition of CPT1 is essential for the anorectic effect of C75. The differential activity of C75 enantiomers may lead to the development of potential new specific drugs for cancer and obesity. |
| publishDate |
2013 |
| dc.date.none.fl_str_mv |
2013 2014 2014 2022 |
| dc.type.none.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/submittedVersion |
| format |
article |
| status_str |
submittedVersion |
| dc.identifier.none.fl_str_mv |
https://hdl.handle.net/2445/53049 |
| url |
https://hdl.handle.net/2445/53049 |
| dc.language.none.fl_str_mv |
Inglés |
| language_invalid_str_mv |
Inglés |
| dc.relation.none.fl_str_mv |
Versió preprint del document publicat a: http://dx.doi.org/10.1002/chir.22139 Chirality, 2013, vol. 25, num. 5, p. 281-287 http://dx.doi.org/10.1002/chir.22139 |
| dc.rights.none.fl_str_mv |
(c) Wiley, 2013 info:eu-repo/semantics/openAccess |
| rights_invalid_str_mv |
(c) Wiley, 2013 |
| eu_rights_str_mv |
openAccess |
| dc.format.none.fl_str_mv |
35 p. application/pdf application/pdf |
| dc.publisher.none.fl_str_mv |
Wiley |
| publisher.none.fl_str_mv |
Wiley |
| dc.source.none.fl_str_mv |
Articles publicats en revistes (Bioquímica i Biomedicina Molecular) reponame:Recercat. Dipósit de la Recerca de Catalunya instname:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya) |
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Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya) |
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Recercat. Dipósit de la Recerca de Catalunya |
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Recercat. Dipósit de la Recerca de Catalunya |
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1869404559325003776 |
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15,811543 |