Gallium complexes as new promising metallodrug candidates

Lessa, Josane A.; Parrilha, Gabrieli L.; Beraldo, Heloísa

doi:10.1016/j.ica.2012.06.003

Cited by 95 publications

(56 citation statements)

References 60 publications

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“…Interestingly, this complex is not destroyed in the blood (Enyedy et al, 2012(Enyedy et al, , 2015Hummer et al, 2012). It shows in vitro a cytotoxic activity higher than that of gallium nitrate (Lessa et al, 2012). The cytotoxicity mechanism involves p53 activation mediated by Ca 2+ -signalling and ROS production (Gogna et al, 2012;Madan et al, 2013).…”

Section: Galliummentioning

confidence: 95%

Coordination compounds in cancer: Past, present and perspectives

Trudu¹,

Amato

Vaňhara³

et al. 2015

J Appl Biomed

136

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Section: Galliummentioning

confidence: 95%

Coordination compounds in cancer: Past, present and perspectives

Trudu¹,

Amato

Vaňhara³

et al. 2015

J Appl Biomed

136

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“…Currently, the efficacy and safety of a variety of compounds containing gallium that are widely used to treat cancer and hypercalcemia, have been conrmed. [16][17][18][19][20] The rst investigation of the antimicrobial action of gallium was published in 1931. 21 It has been reported that gallium (Ga 3+ ) exerts a signicant inhibitory activity against numerous bacteria including Staphylococcus aureus, methicillin-resistant S. aureus, Rhodococcus equi, Pseudomonas aeruginosa, Acinetobacter baumannii and Escherichia coli.…”

mentioning

confidence: 99%

Antimicrobial effect of gallium nitrate against bacteria encountered in burn wound infections

Zhao

Chen

et al. 2017

RSC Adv.

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Recently, biomaterials have been increasingly used for burn wound healing, but burn wound infections and biomaterial-associated infections still need to be addressed. As a novel inorganic antimicrobial, the antimicrobial effect of gallium nitrate was investigated, and the minimum inhibitory concentration (MIC) of gallium nitrate against bacteria that are common in infected burn wounds was determined with a Microbial Viability Assay Kit-WST. The results showed that the MIC of Ga(NO 3 ) 3 against E. coli and E.faecalis was 256 mg mL À1, and it was 512 mg mL À1 against P. aeruginosa, K. pneumonia, E. cloacae, A.baumannii, S. maltophilia, S. aureus and S. epidermidis. Meanwhile, transmission electron microscopy (TEM) found similar visual evidence of the mechanism by which the gallium ion attacks both Gramnegative and Gram-positive bacteria, which was in agreement with the MIC results. By TEM observation, it was found that detachment of the cell membrane and wall and the appearance of an electron-light region containing condensed substances occurred in both Ga 3+ -treated E. coli and Ga 3+ -treated S.aureus cells, with smaller morphological changes in Ga 3+ -treated S. aureus compared with E. coli. This research shows the effective and wide-spectrum antimicrobial properties of gallium nitrate against most bacteria encountered in burn wound infections. Gallium(III) could be a good choice when fighting an infected burn wound, and it is a promising candidate for modifying biomaterials or medical devices to prevent infection in burn wounds.

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“…On the other hand, interaction of Ga(III) with Tf might be modulated by the application of carrier ligands since competition can occur between the protein and the coordinating ligands, and this process strongly depends on the type of the donor atoms and the stability of the Ga(III) complexes. Additionally, the complexation can protect the Ga(III) ion against hydrolysis, and thus the formation of kinetically more inert gallate, and can modify the hydrophilic-lipophilic character as well [12,13]. Therefore, the distinct pharmacokinetics of the gallium salts compared with that of the complexes is based on their different physical-chemical properties.…”

mentioning

confidence: 99%

“…Chemical shifts (δ) are reported in parts per million from 4,4-dimethyl-4-silapentane-1-sulfonic acid. All 1 H NMR spectra were recorded with the WATER-GATE water suppression pulse scheme using 4,4-dimethyl-4-silapentane-1-sulfonic acid as an internal standard.H (for KP46) and STD NMR measurements were performed using a 600 MHz Bruker Avance III spectrometer equipped with a 5 mm cryo-TXI ( 1 H,13 C, 15 N) probe with z-gradient at 7 °C. The protein and HQ (or KP46) were dissolved in 20 mM phosphate buffer [pH 7.4, 10 % (v/v) D 2 O and H 2 O] and an incubation time of 24 h was applied.…”

mentioning

confidence: 99%

Interaction of the anticancer gallium(III) complexes of 8-hydroxyquinoline and maltol with human serum proteins

et al. 2014

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Tris(8-quinolinolato)gallium(III) (KP46) and tris(maltolato)gallium(III) (GaM) are promising orally active antitumor metallodrugs currently undergoing clinical trials. Their interaction with human serum albumin (HSA) and transferrin (Tf) was studied in detail in aqueous solution by the combination of various methods such as spectrofluorometry, UV-vis spectrophotometry, (1)H and saturation transfer difference NMR spectroscopy, and ultrafiltration-UV-vis spectrophotometry. Binding data were evaluated quantitatively. Tf was found to replace the original ligand much less efficiently in KP46 than in GaM, whereas a significant noncovalent binding of KP46 with HSA (log K' = 4.04) retaining the coordination environment around gallium(III) was found. The interaction between HSA and KP46 was also confirmed by protein-complex modeling calculations. On the basis of the conditional stability constants, the distribution of gallium(III) in serum was computed and compared for these metallodrugs under physiological conditions, and revealed the prominent role of HSA in the case of KP46 and that of Tf for GaM.

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Gallium complexes as new promising metallodrug candidates

Cited by 95 publications

References 60 publications

Coordination compounds in cancer: Past, present and perspectives

Coordination compounds in cancer: Past, present and perspectives

Antimicrobial effect of gallium nitrate against bacteria encountered in burn wound infections

Interaction of the anticancer gallium(III) complexes of 8-hydroxyquinoline and maltol with human serum proteins

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