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The Biological Impact of Some Phosphonic and Phosphinic Acid Derivatives on Human Osteosarcoma.
Khaled, Zakzak; Ilia, Gheorghe; Watz, Claudia; Macașoi, Ioana; Draghici, George; Simulescu, Vasile; Merghes, Petru Eugen; Varan, Narcis Ion; Dehelean, Cristina Adriana; Vlaia, Lavinia; Sima, Laurențiu.
Afiliación
  • Khaled Z; Pharmaceutical Technology, Faculty of Pharmacy, "Victor Babes" University of Medicine and Pharmacy, 2nd Eftimie Murgu Square, 300041 Timisoara, Romania.
  • Ilia G; Formulation and Technology of Drugs Research Center, "Victor Babes" University of Medicine and Pharmacy, 2nd Eftimie Murgu Square, 300041 Timisoara, Romania.
  • Watz C; Department of Biology-Chemistry, Faculty of Chemistry, Biology, Geography, West University Timisoara, 16 Pestalozzi Street, 300115 Timisoara, Romania.
  • Macașoi I; Department of Pharmaceutical Physics, Faculty of Pharmacy, "Victor Babes" University of Medicine and Pharmacy of Timisoara, 2nd Eftimie Murgu Square, 300041 Timisoara, Romania.
  • Draghici G; Research Center for Pharmaco-Toxicological Evaluation, "Victor Babes" University of Medicine and Pharmacy Timisoara, 2nd Eftimie Murgu Square, 300041 Timisoara, Romania.
  • Simulescu V; Research Center for Pharmaco-Toxicological Evaluation, "Victor Babes" University of Medicine and Pharmacy Timisoara, 2nd Eftimie Murgu Square, 300041 Timisoara, Romania.
  • Merghes PE; Department of Toxicology and Drug Industry, Faculty of Pharmacy, "Victor Babes" University of Medicine and Pharmacy Timisoara, 2nd Eftimie Murgu Square, 300041 Timisoara, Romania.
  • Varan NI; Research Center for Pharmaco-Toxicological Evaluation, "Victor Babes" University of Medicine and Pharmacy Timisoara, 2nd Eftimie Murgu Square, 300041 Timisoara, Romania.
  • Dehelean CA; Department of Toxicology and Drug Industry, Faculty of Pharmacy, "Victor Babes" University of Medicine and Pharmacy Timisoara, 2nd Eftimie Murgu Square, 300041 Timisoara, Romania.
  • Vlaia L; Department of Biology-Chemistry, Faculty of Chemistry, Biology, Geography, West University Timisoara, 16 Pestalozzi Street, 300115 Timisoara, Romania.
  • Sima L; Department of Physical Education and Sport, "King Mihai I" University of Life Sciences from Timisoara, Calea Aradului 119, 300645 Timisoara, Romania.
Curr Issues Mol Biol ; 46(5): 4815-4831, 2024 May 15.
Article en En | MEDLINE | ID: mdl-38785558
ABSTRACT
Osteosarcoma malignancy currently represents a major health problem; therefore, the need for new therapy approaches is of great interest. In this regard, the current study aims to evaluate the anti-neoplastic potential of a newly developed phosphinic acid derivative (2-carboxyethylphenylphosphinic acid) and, subsequently, to outline its pharmaco-toxicological profile by employing two different in vitro human cell cultures (keratinocytes-HaCaT-and osteosarcoma SAOS-2 cells), employing different techniques (MTT assay, cell morphology assessment, LDH assay, Hoechst staining and RT-PCR). Additionally, the results obtained are compared with three commercially available phosphorus-containing compounds (P1, P2, P3). The results recorded for the newly developed compound (P4) revealed good biocompatibility (cell viability of 77%) when concentrations up to 5 mM were used on HaCaT cells for 24 h. Also, the HaCaT cultures showed no significant morphological alterations or gene modulation, thus achieving a biosafety profile even superior to some of the commercial products tested herein. Moreover, in terms of anti-osteosarcoma activity, 2-carboxyethylphenylphosphinic acid expressed promising activity on SAOS-2 monolayers, the cells showing viability of only 55%, as well as apoptosis features and important gene expression modulation, especially Bid downregulation. Therefore, the newly developed compound should be considered a promising candidate for further in vitro and in vivo research related to osteosarcoma therapy.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Curr Issues Mol Biol Asunto de la revista: BIOLOGIA MOLECULAR Año: 2024 Tipo del documento: Article País de afiliación: Rumanía Pais de publicación: Suiza

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Curr Issues Mol Biol Asunto de la revista: BIOLOGIA MOLECULAR Año: 2024 Tipo del documento: Article País de afiliación: Rumanía Pais de publicación: Suiza