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 (HO-AAVPA), 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 48 h with an IC50 = 0.655 mM in U87-MG cells and an IC50 = 0.453
mM 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 chorioallantoid 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.
In Vitro and In Vivo Radiosensitizing Effect of Valproic Acid on Fractionated Irradiation