The endogenous lipoperoxidation product 9-hydroxystearic acid (9HSA) is an inhibitor of HDAC1 and its administration to HT29, a colon adenocarcinoma cell line, induces a proliferative arrest mediated by a direct activation of the p21WAF1 gene, bypassing p53 [1]. In a recent work the interaction of 9-HSA with the catalytic site of the 3D model of HDAC1 has been tested with a docking procedure. Noticeably, when interacting with the site, the (R)-9-enantiomer is more stable than the (S) one: in fact the energy of interaction is -8.45 kcal/mol and -1.97 kcal/mol for the (R) and (S) isomers, respectively, and the estimated free energy of binding is -6.31 kcal/mol and +4.98 kcal/mol for (R) and (S), respectively [2]. In this work (R)-9HSA was obtained and its biological activity was tested in HT29.

Antiproliferative activity of enantiomerically pure (R)-9-hydroxystearic acid in HT29 colon cancer cells.

PAROLIN, CAROLA ELEONORA;CALONGHI, NATALIA;PAGNOTTA, ELEONORA;BOGA, CARLA;MASOTTI, LANFRANCO
2005

Abstract

The endogenous lipoperoxidation product 9-hydroxystearic acid (9HSA) is an inhibitor of HDAC1 and its administration to HT29, a colon adenocarcinoma cell line, induces a proliferative arrest mediated by a direct activation of the p21WAF1 gene, bypassing p53 [1]. In a recent work the interaction of 9-HSA with the catalytic site of the 3D model of HDAC1 has been tested with a docking procedure. Noticeably, when interacting with the site, the (R)-9-enantiomer is more stable than the (S) one: in fact the energy of interaction is -8.45 kcal/mol and -1.97 kcal/mol for the (R) and (S) isomers, respectively, and the estimated free energy of binding is -6.31 kcal/mol and +4.98 kcal/mol for (R) and (S), respectively [2]. In this work (R)-9HSA was obtained and its biological activity was tested in HT29.
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C. Parolin; N. Calonghi; E. Pagnotta; C. Boga; L. Masotti
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11585/9390
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