Apoptotic Effects of N-(2-Hydroxyphenyl)-2-Propylpentanamide on U87-MG and U-2 OS Cells and Antiangiogenic Properties
| Autor: | José Correa-Basurto, Alma Chavez-Blanco, Humberto L. Mendoza-Figueroa, Paola Castillo-Juárez, Sebastián C. Sanchez |
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| Rok vydání: | 2021 |
| Předmět: |
Cancer Research
Cell Survival Angiogenesis Inhibitors Antineoplastic Agents Apoptosis Structure-Activity Relationship Pentanes Tumor Cells Cultured medicine Humans U87 IC50 Cell Proliferation Pharmacology Dose-Response Relationship Drug Molecular Structure Neovascularization Pathologic biology Chemistry Cancer medicine.disease Amides Histone Cell culture Cancer cell biology.protein Cancer research Molecular Medicine Osteosarcoma Drug Screening Assays Antitumor |
| Zdroj: | Anti-Cancer Agents in Medicinal Chemistry. 21:1451-1459 |
| ISSN: | 1871-5206 |
| DOI: | 10.2174/1871520620666200728125356 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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