Please use this identifier to cite or link to this item: http://hdl.handle.net/2445/53049
Title: Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug. (-)-C75 has antitumour activity
Author: 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
Keywords: Obesitat
Càncer
Estereoquímica
Enantiòmers
Medicaments antineoplàstics
Obesity
Cancer
Stereochemistry
Enantiomers
Antineoplastic agents
Issue Date: May-2013
Publisher: Wiley
Abstract: 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.
Note: Versió preprint del document publicat a: http://dx.doi.org/10.1002/chir.22139
It is part of: Chirality, 2013, vol. 25, num. 5, p. 281-287
Related resource: http://dx.doi.org/10.1002/chir.22139
URI: http://hdl.handle.net/2445/53049
ISSN: 0899-0042
Appears in Collections:Articles publicats en revistes (Química Inorgànica i Orgànica)
Articles publicats en revistes (Bioquímica i Biomedicina Molecular)

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