Metal Complexes in Diagnosis and Therapy

Tesauro, Diego

doi:10.3390/ijms23084377

Cited by 10 publications

(5 citation statements)

References 26 publications

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“…Firstly, isoquinoline N -oxide attacks 2-chloroimidazoline to form 2-((4,5-dihydro-1 H -imidazol-2-yl)oxy)isoquinolin-2-ium chloride ( Ia ), which, in the mesomeric form Ib , possesses a nucleophilic carbon atom in position 3 that is susceptible to the intramolecular attack of the nitrogen atom of the imidazoline ring. In the next step, the simultaneous re-aromatization of intermediate—3,4 a -dihydro-2 H -imidazo[1′,2′:4,5][ 1 , 2 , 4 ]oxadiazolo[2,3- b ]isoquinoline ( II ) followed by the elimination of hydrogen chloride leads to the formation of the desired 1-(isoquinolin-3-yl)imidazolidin-2-one ( Scheme 2 ). Upon the treatment of compound L2 with methyl or ethyl iodide in the presence of sodium hydroxide, the corresponding N -alkylated ligands L3 and L4 were synthesized in acceptable yields ( Scheme 2 ).…”

Section: Resultsmentioning

confidence: 99%

“…Since metal-based compounds play remarkable roles as therapeutic and diagnostic agents, the search for novel metallopharmaceuticals represents an area of significant interest in the field of medicinal chemistry [ 1 , 2 ]. The therapeutic potential of metal complexes has a long history; however, the discovery of the bacteriostatic and anticancer activity ruthenium(II) phenanthroline complexes by Francis Dwyer, followed by the discovery of the anticancer properties of cis -diaminodichloridoplatinum(II)— cisplatin by Barnet Rosenberg, was a milestone in the development of metal-containing drugs [ 1 ].…”

Section: Introductionmentioning

confidence: 99%

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Copper(II) Complexes with 1-(Isoquinolin-3-yl)heteroalkyl-2-ones: Synthesis, Structure and Evaluation of Anticancer, Antimicrobial and Antioxidant Potential

Balewski,

Plech,

Korona-Głowniak

et al. 2023

IJMS

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Four copper(II) complexes, C1–4, derived from 1-(isoquinolin-3-yl)heteroalkyl-2-one ligands L1–4 were synthesized and characterized using an elemental analysis, IR spectroscopic data as well as single crystal X-ray diffraction data for complex C1. The stability of complexes C1–4 under conditions mimicking the physiological environment was estimated using UV-Vis spectrophotometry. The antiproliferative activity of both ligands L1–4 and copper(II) compounds C1–4 were evaluated using an MTT assay on four human cancer cell lines, A375 (melanoma), HepG2 (hepatoma), LS-180 (colon cancer) and T98G (glioblastoma), and a non-cancerous cell line, CCD-1059Sk (human normal skin fibroblasts). Complexes C1–4 showed greater potency against HepG2, LS180 and T98G cancer cell lines than etoposide (IC50 = 5.04–14.89 μg/mL vs. IC50 = 43.21–>100 μg/mL), while free ligands L1–4 remained inactive in all cell lines. The prominent copper(II) compound C2 appeared to be more selective towards cancer cells compared with normal cells than compounds C1, C3 and C4. The treatment of HepG2 and T98G cells with complex C2 resulted in sub-G1 and G2/M cell cycle arrest, respectively, which was accompanied by DNA degradation. Moreover, the non-cytotoxic doses of C2 synergistically enhanced the cytotoxic effects of chemotherapeutic drugs, including etoposide, 5-fluorouracil and temozolomide, in HepG2 and T98G cells. The antimicrobial activities of ligands L2–4 and their copper(II) complexes C2–4 were evaluated using different types of Gram-positive bacteria, Gram-negative bacteria and yeast species. No correlation was found between the results of the antiproliferative and antimicrobial experiments. The antioxidant activities of all compounds were determined using the DPPH and ABTS radical scavenging methods. Antiradical tests revealed that among the investigated compounds, copper(II) complex C4 possessed the strongest antioxidant properties. Finally, the ADME technique was used to determine the physicochemical and drug-likeness properties of the obtained complexes.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Copper(II) Complexes with 1-(Isoquinolin-3-yl)heteroalkyl-2-ones: Synthesis, Structure and Evaluation of Anticancer, Antimicrobial and Antioxidant Potential

Balewski,

Plech,

Korona-Głowniak

et al. 2023

IJMS

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“…Although gold had high medical significance in Chinese and Middle East medicine centuries ago, scientists have only recently “rediscovered” its anti-inflammatory properties [ 16 ]. Anti-inflammatory effects have been documented in numerous gold(I) and (III) complexes.…”

Section: Discussionmentioning

confidence: 99%

A New Gold(III) Complex, TGS 703, Shows Potent Anti-Inflammatory Activity in Colitis via the Enzymatic and Non-Enzymatic Antioxidant System—An In Vitro, In Silico, and In Vivo Study

Włodarczyk

Krajewska

Szeleszczuk

et al. 2023

IJMS

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Inflammatory bowel diseases (IBD) and their main representatives, Crohn’s disease and ulcerative colitis, are worldwide health-care problems with constantly increasing frequency and still not fully understood pathogenesis. IBD treatment involves drugs such as corticosteroids, derivatives of 5-aminosalicylic acid, thiopurines, and others, with the goal to achieve and maintain remission of the disease. Nowadays, as our knowledge about IBD is continually growing, more specific and effective therapies at the molecular level are wanted. In our study, we tested novel gold complexes and their potential effect on inflammation and IBD in vitro, in silico, and in vivo. A series of new gold(III) complexes (TGS 404, 512, 701, 702, and 703) were designed and screened in the in vitro inflammation studies. In silico modeling was used to study the gold complexes’ structure vs. their activity and stability. Dextran sulphate sodium (DSS)-induced mouse model of colitis was employed to characterize the anti-inflammatory activity in vivo. Lipopolysaccharide (LPS)-stimulated RAW264.7 cell experiments proved the anti-inflammatory potential of all tested complexes. Selected on the bases of in vitro and in silico analyses, TGS 703 significantly alleviated inflammation in the DSS-induced mouse model of colitis, which was confirmed by a statistically significant decrease in the macro- and microscopic score of inflammation. The mechanism of action of TGS 703 was linked to the enzymatic and non-enzymatic antioxidant systems. TGS 703 and other gold(III) complexes present anti-inflammatory potential and may be applied therapeutically in the treatment of IBD.

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“…Gold, used as a therapeutic, had high medical significance in Chinese and Middle Eastern medicine centuries ago [ 21 ], but recently scientists “rediscovered” its beneficial properties. Anti-inflammatory effects have been well documented in numerous gold(I) and (III) complexes, also by our group [ 18 , 22 ].…”

Section: Discussionmentioning

confidence: 99%

New gold(III) complexes TGS 121, 404, and 702 show anti-tumor activity in colitis-induced colorectal cancer: an in vitro and in vivo study

Włodarczyk,

Krajewska,

Talar

et al. 2023

Pharmacol. Rep

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Background Chronic inflammation in the course of inflammatory bowel disease may result in colon cancer, or colitis-associated colorectal cancer (CACRC). It is well established that CACRC is associated with oxidative stress and secretion of multiple pro-inflammatory cytokines, e.g. tumor necrosis factor-α. Recently, we proved that the administration of gold(III) complexes resulted in the alleviation of acute colitis in mice. The aim of the current study was to assess the antitumor effect of a novel series of gold(III) complexes: TGS 121, 404, 512, 701, 702, and 703. Materials Analyzed gold(III) complexes were screened in the in vitro studies using colorectal cancer and normal colon epithelium cell lines, SW480, HT-29, and CCD 841 CoN, and in vivo, in the CACRC mouse model. Results Of all tested complexes, TGS 121, 404, and 702 exhibited the strongest anti-tumor effect in in vitro viability assay of colon cancer cell lines and in in vivo CACRC model, in which these complexes decreased the total number of colonic tumors and macroscopic score. We also evidenced that the mechanism of action was linked to the enzymatic antioxidant system and inflammatory cytokines. Conclusions TGS 121, 404, and 702 present anti-tumor potential and are an attractive therapeutic option for colorectal cancer.

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Metal Complexes in Diagnosis and Therapy

Abstract: The use of metal complexes for health and healing has been in use for over the last several millennia and perhaps longer [...]

Cited by 10 publications

References 26 publications

Copper(II) Complexes with 1-(Isoquinolin-3-yl)heteroalkyl-2-ones: Synthesis, Structure and Evaluation of Anticancer, Antimicrobial and Antioxidant Potential

Copper(II) Complexes with 1-(Isoquinolin-3-yl)heteroalkyl-2-ones: Synthesis, Structure and Evaluation of Anticancer, Antimicrobial and Antioxidant Potential

A New Gold(III) Complex, TGS 703, Shows Potent Anti-Inflammatory Activity in Colitis via the Enzymatic and Non-Enzymatic Antioxidant System—An In Vitro, In Silico, and In Vivo Study

New gold(III) complexes TGS 121, 404, and 702 show anti-tumor activity in colitis-induced colorectal cancer: an in vitro and in vivo study

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