SYNTHESIS, CHARACTERIZATION AND CYTOTOXICITY EVALUATION OF Ni(II), Cu(II) AND Zn(II) COMPLEXES WITH DEOXYCHOLATE LIGAND

Abstract

Three new complexes of Ni(II), Cu(II) and Zn(II) with deoxycholate anion, of the type M(DCA) 2 • nH 2 O (M = Cu(II) n = 4, M = Ni(II) n = 3 and M = Zn(II) n = 2) have been synthesized and characterized on the basis of elemental analysis, FTIR and UV-Vis spectroscopy, thermal analysis, molar conductivity and magnetic measurements. The cytotoxicity of the synthesized complexes was tested against HT29 human colorectal cancer cells. Applied at a concentration range of 10 -200 µg/mL, sodium deoxycholate and its metal complexes have been found to decrease viability and growth of cultured HT29 cells in a time-and concentration-dependent manner in short-term and long-term experiments. The ability of the complexes to induce pathological changes, genotoxicity and apoptosis in the treated cells has also been proved. In addition, the complexes demonstrated a cytotoxic effect in HT29-OxPt (resistant to oxaliplatin) cells, allowing to conclude that they are more pronounced cytotoxic agents as compared to the sodium deoxycholate alone. RezumatTrei noi complecși ai Ni(II), Cu(II) și Zn(II) cu anionul deoxicolat, de tipul M(DCA) 2 • nH 2 O (M = Cu(II) n = 4, M = Ni(II) n = 3 și M = Zn(II) n = 2), au fost sintetizați și caracterizați pe baza analizei elementale, a spectroscopiei FTIR și UV-Vis, analizei termice, conductivității molare și a măsurătorilor magnetice. Citotoxicitatea complecșilor sintetizați a fost testată pe celule canceroase colorectale umane HT29. La concentrații de 10 -200 µg/mL, s-a observat că deoxicolatul de sodiu și complecșii săi metalici scad viabilitatea și dezvoltarea celulelor colorectale umane HT29 cultivate, într-o manieră dependentă de timp și concentrație, în experimente pe termen scurt și pe termen lung. Capacitatea complecșilor de a induce modificări patologice, genotoxicitate și apoptoză în celulele tratate a fost de asemenea dovedită. În plus, complecșii au demonstrat un efect citotoxic asupra celulelor HT29-OxPt (rezistente la oxaliplatină), permițându-ne să concluzionăm că sunt agenți citotoxici mai puternici comparativ cu deoxicolatul de sodiu.

Optimization of a Flow Cytometry Protocol for Pd-1/Ctla-4 Immune Checkpoints Receptors Detection in Colorectal Cancer Tumour Microenvironment

“…The mean number of T cells (CD3 positive cells) in our cohort was about 6.8% of which 3.41% revealed PD-1 positive expression and 2% expressed CTLA-4. Despite the low number of patients enrolled in this preliminary study, our data is in accordance with the available literature [20], sustaining the potential interest of flow cytometry for the CRC TME characterization. Interestingly, 4.1% of the EpCam + cells also expressed PD-1 and 24.6% of the EpCam + cells also expressed CTLA-4.…”

In Vitro Assessment of the Potential Cytotoxic Effect of Metformin on Colorectal Cancer Cells

“…In order to determine CCD 841 CoN, HCT 116 and HT-29 cellular viability, MTT assay was conducted at 72 h following Met treatment, according to the following protocol [2,3]. In brief, 96-well plates were seeded with 1 × 10 4 /200 µL cells/well and after reaching 90% confluence, Met test solutions were added.…”

New Metal Complexes With Aril-Acetic Structure: Preparation, Characterization, and in Vitro Antiinflammatory Effects

“…The diclofenac hydrazone Schiff bases (1a-d) were synthesised by the reaction of some hydroxylated aromatic aldehydes (2-hydroxy/2,3-dihydroxy/2,4dihydroxy/2,5-dihydroxy-benzaldehyde) (7.5 mmol) and diclofenac hydrazide (DH) (5 mmol), by refluxing (for 2 -8 h) in absolute ethanol (100 mL), in the presence of glacial acetic acid (1 mmol) (Figure 1). The resulting product was separated by vacuum filtration, and then purified by silica gel column chromatography (petroleum ether:ethyl acetate solvent system = 8:2, v/v) [12,15]. To prepare the metal complexes, the diclofenac hydrazones (1a-d, 2 mmol) were dissolved in ethanol (30 mL), and after that, the bivalent metal salts (Cu(CH3COO)2•H2O, Zn(CH3COO)2•2H2O and Ni(CH3COO)2•4H2O (1 mmol) as an ethanolic solution (10 mL) were added [40,42,48].…”