Paola Castillo-Juárez, Sebastián C. Sanchez, Alma D. Chávez-Blanco, Humberto L. Mendoza-Figueroa and José Correa-Basurto* Pages 1451 - 1459 ( 9 )
<p>Background and Objective: Histone Deacetylases (HDACs) are important therapeutic targets for many types of human cancers. A derivative of valproic acid, N-(2-hydroxyphenyl)-2-propylpentanamide (HOAAVPA), has antiproliferative properties on some cancer cell lines and inhibits the HDAC1 isoform. </P><P> Materials and Methods: In this work, HO-AAVPA was tested as an antiproliferative agent in U87-MG (human glioblastoma) and U-2 OS cells (human osteosarcoma), which are types of cancer that are difficult to treat, and its antiangiogenic properties were explored. </P><P> Results: HO-AAVPA had antiproliferative effects at 48h with an IC<sub>50</sub>=0.655mM in U87-MG cells and an IC<sub>50</sub>=0.453mM in U-2 OS cells. Additionally, in the colony formation assay, HO-AAVPA decreased the number of colonies by approximately 99% in both cell lines and induced apoptosis by 31.3% in the U-2 OS cell line and by 78.2% in the U87-MG cell line. Additionally, HO-AAVPA reduced the number of vessels in Chorioallantoic Membranes (CAMs) by approximately 67.74% and IL-6 levels in both cell lines suggesting that the biochemical mechanism on cancer cell of HO-AAVPA is different compared to VPA. </P><P> Conclusion: HO-AAVPA has antiproliferative effects on glioblastoma and osteosarcoma and antiangiogenic properties.</p>
Antiproliferative, proapoptotic, HO-AAVPA, antiangiogenic properties, U87-MG, U-2 OS.
Department of Microbiology, Escuela Nacional de Ciencias Biologicas, Instituto Politecnico Nacional, Carpio y Plan de Ayala S/N, Casco de Santo Tomas, Mexico, CDMX. 11340, Department of Microbiology, Escuela Nacional de Ciencias Biologicas, Instituto Politecnico Nacional, Carpio y Plan de Ayala S/N, Casco de Santo Tomas, Mexico, CDMX. 11340, Subdireccion de Investigacion Basica, Intituto Nacional de Cancerologia, Ciudad de Mexico, Laboratorio de Diseno y Desarrollo de Nuevos Farmacos e Innovacion Biotecnologica, Escuela Superior de Medicina, Instituto Politecnico Nacional, Plan de San Luis y Díaz Miron, Ciudad de Mexico 11340, Laboratorio de Diseno y Desarrollo de Nuevos Farmacos e Innovacion Biotecnologica, Escuela Superior de Medicina, Instituto Politecnico Nacional, Plan de San Luis y Díaz Miron, Ciudad de Mexico 11340