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Anti-Cancer Agents in Medicinal Chemistry

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ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

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General Research Article

Apoptotic Effects of N-(2-Hydroxyphenyl)-2-Propylpentanamide on U87-MG and U-2 OS Cells and Antiangiogenic Properties

Author(s): Paola Castillo-Juárez, Sebastián C. Sanchez, Alma D. Chávez-Blanco, Humberto L. Mendoza-Figueroa and José Correa-Basurto*

Volume 21, Issue 11, 2021

Published on: 28 July, 2020

Page: [1451 - 1459] Pages: 9

DOI: 10.2174/1871520620666200728125356

Price: $65

Abstract

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.

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.

Results: HO-AAVPA had antiproliferative effects at 48h with an IC50=0.655mM in U87-MG cells and an IC50=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.

Conclusion: HO-AAVPA has antiproliferative effects on glioblastoma and osteosarcoma and antiangiogenic properties.

Keywords: Antiproliferative, proapoptotic, HO-AAVPA, antiangiogenic properties, U87-MG, U-2 OS.

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