Hybrid Ammonium-M(II) Hydrogenophosphite Hydrates as Bioactive Metal Complexes: Synthesis, DFT and Hirshfeld Surface Analysis, and Anticancer and Anti-Inflammatory Activities

Background/Objectives: Metal-based coordination compounds are attracting attention in medicinal inorganic chemistry because changes in the metal centre can influence their physicochemical properties and biological responses. This study aimed to evaluate two isostructural ammonium-M(II) hydrogenophosphite hydrates, (NH4)2[Mg(H2O)6]3(HPO3)4 (complex 1) and (NH4)2[Co(H2O)6]3(HPO3)4 (complex 2), as bioactive systems with potential anticancer and anti-inflammatory properties. Methods: The complexes were synthesized and characterized by X-ray powder diffraction (XRPD), Fourier-transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), density functional theory (DFT) calculations, and Hirshfeld surface analysis. Their cytotoxic activity was evaluated against B16-F10, HT29, HepG2, and HL-60 tumour cell lines. For complex 2, apoptosis, cell-cycle distribution, and mitochondrial membrane potential were analysed by flow cytometry. Nitric oxide production was measured in LPS-stimulated RAW 264.7 macrophages. Results: Complex 2 showed the highest cytotoxic activity, particularly against HL-60 leukaemia cells (IC50 = 36.98 μg/mL), whereas complex 1 displayed weaker activity. Complex 2 increased apoptotic cell populations, altered cell-cycle distribution, and induced mitochondrial membrane depolarization in HL-60 cells. Both complexes reduced nitric oxide production, with complex 2 showing the strongest effect (IC50 NO = 22.46 μg/mL), exceeding that of diclofenac under the experimental conditions, while complex 1 showed comparable activity to the reference drug. DFT descriptors indicated higher electronic reactivity for complex 2. Conclusions: Replacement of Mg(II) by Co(II) enhances the biological activity of this hydrogenophosphite framework. Complex 2 combines cytotoxic activity against HL-60 cells with apoptosis-associated mitochondrial dysfunction and NO-inhibitory activity in activated macrophages, supporting hydrogenophosphite-based metal complexes as bioactive coordination compounds with potential as multifunctional agents.

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Journal
Pharmaceuticals
Published
2026-08-20
DOI
https://doi.org/10.3390/ph19081315
Primary Topic
Metal complexes synthesis and properties
Type
article
Field-Weighted Citation Impact
0.00

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article

Hybrid Ammonium-M(II) Hydrogenophosphite Hydrates as Bioactive Metal Complexes: Synthesis, DFT and Hirshfeld Surface Analysis, and Anticancer and Anti-Inflammatory Activities

Juan Sáinz, Meryem Hrimla, Mohammed Lachkar, Fernando J. Reyes‐Zurita et al.
Pharmaceuticals
Metal complexes synthesis and properties
article

Hybrid Ammonium-M(II) Hydrogenophosphite Hydrates as Bioactive Metal Complexes: Synthesis, DFT and Hirshfeld Surface Analysis, and Anticancer and Anti-Inflammatory Activities

Juan Sáinz, Meryem Hrimla, Mohammed Lachkar, Fernando J. Reyes‐Zurita, Mustapha Ait Elhad, Rachid Chahboun, Houda Zentar, Safaa Hidaoui, Mohammed Zerrouk, Zineb Ariba, M. Er-rajy, Rachid Ouarsal
article en

Abstract

Background/Objectives: Metal-based coordination compounds are attracting attention in medicinal inorganic chemistry because changes in the metal centre can influence their physicochemical properties and biological responses. This study aimed to evaluate two isostructural ammonium-M(II) hydrogenophosphite hydrates, (NH4)2[Mg(H2O)6]3(HPO3)4 (complex 1) and (NH4)2[Co(H2O)6]3(HPO3)4 (complex 2), as bioactive systems with potential anticancer and anti-inflammatory properties. Methods: The complexes were synthesized and characterized by X-ray powder diffraction (XRPD), Fourier-transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), density functional theory (DFT) calculations, and Hirshfeld surface analysis. Their cytotoxic activity was evaluated against B16-F10, HT29, HepG2, and HL-60 tumour cell lines. For complex 2, apoptosis, cell-cycle distribution, and mitochondrial membrane potential were analysed by flow cytometry. Nitric oxide production was measured in LPS-stimulated RAW 264.7 macrophages. Results: Complex 2 showed the highest cytotoxic activity, particularly against HL-60 leukaemia cells (IC50 = 36.98 μg/mL), whereas complex 1 displayed weaker activity. Complex 2 increased apoptotic cell populations, altered cell-cycle distribution, and induced mitochondrial membrane depolarization in HL-60 cells. Both complexes reduced nitric oxide production, with complex 2 showing the strongest effect (IC50 NO = 22.46 μg/mL), exceeding that of diclofenac under the experimental conditions, while complex 1 showed comparable activity to the reference drug. DFT descriptors indicated higher electronic reactivity for complex 2. Conclusions: Replacement of Mg(II) by Co(II) enhances the biological activity of this hydrogenophosphite framework. Complex 2 combines cytotoxic activity against HL-60 cells with apoptosis-associated mitochondrial dysfunction and NO-inhibitory activity in activated macrophages, supporting hydrogenophosphite-based metal complexes as bioactive coordination compounds with potential as multifunctional agents.

PharmaceuticalsVol. 19(8)
Universidad de Granada (ES), Abdelmalek Essaâdi University (MA), Instituto de Investigación Biosanitaria de Granada (ES), Pfizer-University of Granada-Junta de Andalucía Centre for Genomics and Oncological Research (ES), Centro de Investigación Biomédica en Red de Epidemiología y Salud Pública (ES), Sidi Mohamed Ben Abdellah University (MA)
Universidad de Granada
Openalex Percentile: Top 12%
Metal complexes synthesis and properties
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