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1.
ACS Omega ; 6(49): 33454-33461, 2021 Dec 14.
Artigo em Inglês | MEDLINE | ID: mdl-34926895

RESUMO

Human chronic latent magnesium deficiency is estimated to impact a substantive portion of the world's population. A number of magnesium compounds have been developed to combat this deficiency; however, none are ideal due to issues of solubility, absorption, side effects (e.g., laxation) and/or formulation. Here, we describe the pH-dependent synthesis, chemical characterization (inductively coupled plasma and thermal analysis, infrared and nuclear magnetic resonance (1D and 2D) spectroscopies, and electrospray mass spectrometry) and in vitro uptake (in a cell model of the large intestine (CaCo-2 cells)) of a magnesium complex of the glycine dimer (HG2). Results demonstrate that the HG2 ligand assumes a tridentate coordination mode with an N2O donor set and an octahedral coordination sphere completed with coordinated waters. The magnesium:HG2 complex exhibits significant solubility and cellular uptake.

2.
ACS Omega ; 6(44): 29713-29723, 2021 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-34778643

RESUMO

Magnesium deficiency and/or deficit (hypomagnesemia, <0.75 mmol/L in the blood) has become a recognized problem in healthcare and clinical settings. Concomitantly, supplementation has become recognized as the primary means of mitigating such deficiencies. Common magnesium supplements typically suffer from shortcomings: rapid dissociation and subsequent laxation (magnesium salts: e.g., magnesium chloride), poor water solubility (magnesium oxides and hydroxides), poor characterizability (magnesium chelates), and are/or use of non-natural ligands. To this end, there is a need for the development of fully characterized, water-soluble, all-natural magnesium compounds. Herein, we discuss the synthesis, solution and solid-state characterization, aqueous solubility, and cellular uptake of magnesium complexes of maltol and ethylmaltol, ligands whose magnesium complexes have yet to be fully explored.

3.
Molecules ; 26(9)2021 Apr 21.
Artigo em Inglês | MEDLINE | ID: mdl-33919285

RESUMO

Magnesium (Mg2+) plays a crucial role in over 80% of all metabolic functions. It is becoming increasingly apparent that magnesium deficiency (hypomagnesemia) may play an important role in chronic disease. To counteract magnesium deficiency, there is an unmet clinical need to develop new fully characterized, highly bioavailable, and substantially water-soluble magnesium supplements. To this end, triglycine (HG3), a tripeptide of the amino acid glycine, was chosen as a chelating ligand for magnesium, given its natural occurrence and water solubility, and entropically-driven metal binding. Herein, we discuss the synthesis, chemical and physical characterization, and cellular uptake of a magnesium triglycine chelate (MgG3), an octahedral complex with extraordinary water solubility and improved cellular uptake in CaCo-2 cells than select commonly used magnesium supplements.


Assuntos
Quelantes/química , Quelantes/farmacologia , Glicina/química , Magnésio/química , Oligopeptídeos/química , Oligopeptídeos/farmacologia , Linhagem Celular Tumoral , Células Cultivadas , Quelantes/síntese química , Técnicas de Química Sintética , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Oligopeptídeos/síntese química , Solubilidade , Relação Estrutura-Atividade
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