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We investigated the total phenolic and flavonoid contents and the anthocyanin profiles in aqueous, ethanol and acetone extracts of Prunus spinosa (Rosaceae) fruit, and their antioxidant, antibacterial, antifungal, antidiabetic and antitumor properties. The contribution of polyphenol contents to the bioactivity of the extracts was calculated and observed through Pearson’s coefficient of correlation. The acetone extract was the richest in phenols and anthocyanins and the ethanol extract in flavonoids. Cyanidin was the most abundant anthocyanin compound in all examined extracts. The ethanol extract showed the most promising antioxidant activity in DPPH, ABTS and FRAP assays. Tested bacteria were more affected by the ethanol than by the aqueous extract. Both the ethanol and aqueous extracts exhibited potential antidiabetic effects, observed as inhibition of α-amylase and α-glucosidase, enzymes linked with diabetes mellitus type II. The ethanol extract was a potent α-glucosidase-inhibitor with a significantly lower IC50 value than the positive control, glucobay, used to treat diabetes mellitus type II. Neither the ethanol nor the aqueous extracts had any effects on tested human malignant cell lines. Our results indicate that the ethanol extract showed the most pronounced in vitro antioxidant and antimicrobial effects, and a potential antidiabetic activity, which can be ascribed to its high flavonoid content. Our results indicate that research of compounds, particularly of flavonoids present in the ethanol extract and their anti-diabetic properties should be examined further. [Projects of the Serbian Ministry of Education, Science and Technological Development, Grant no. 173029, Grant no. 173032 and Grant no. 175011]

Two new complexes with the general formula [Cu2(L)tpmc] (ClO4)3·nH2O (tpmc = N,N′,N′′,N′′′-tetrakis(2-pyridylmethyl)- -1,4,8,11-tetraazacyclotetradecane, L = N-methylglycine, n = 3; L = N,N- -dimethylglycine, n = 2) were isolated and their composition, some physical and chemical properties and geometries were proposed based on elemental analysis (C, H, N), conductometric and magnetic measurements and spectroscopic data (UV–Vis, FTIR). It is evident that the complexes are binuclear and an exo coordination mode of the macrocyclic ligand in the boat conformation was proposed. The co-ligands are coordinated as a bridge using both oxygen atoms of the OCO- group. The cytotoxic activity of Cu(II) complexes as well as their Co(II) analogs, the starting ligands and the free salts were tested against human cervix adenocarcinoma cell line (HeLa), human chronic myelogenous leukemia cells (K562), human breast cancer cell line (MDA-MB-453), and a non-cancerous cell line, human embryonic lung fibroblast (MRC-5). The IC50 values for the Cu(II) complexes were from 21.6±0.04 to 66.1±0.8, and for the Co(II) analogs were within the range from 8.8±0.74 to 15.40±1.52. All four complexes were tested for their antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and the yeast Candida albicans. [Project of the Serbian Ministry of Education, Science and Technological Development, Grant no. 172014]

Two new p-cymene ruthenium(II) complexes containing as additional ligands N-methylpiperazine ([(η6-p-cymene)RuCl2(CH3NH(CH2)4NH)]PF6, complex 1) or vitamin K3-thiosemicarbazone ([(η6-p-cymene)RuCl2(K3tsc)], complex 2) were synthesized starting from [(η6-p-cymene)2RuCl2]2 and the corresponding ligand. The complexes were characterized by elemental analysis, IR, electronic absorption and NMR spectroscopy. The X-ray crystal structure determination of complex 1 revealed “piano-stool” geometry. The differences in the cytotoxic activity of the two complexes are discussed in terms of the ligand present.

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Abstract Background The aim of this research was to determine the intensity and mechanisms of the cytotoxic actions of five extracts isolated from the endemic plant species Helichrysum zivojinii Černjavski & Soška (family Asteraceae) against specific cancer cell lines. In order to evaluate the sensitivity of normal immunocompetent cells implicated in the antitumor immune response, the cytotoxicity of extracts was also tested against healthy peripheral blood mononuclear cells (PBMC). Methods The aerial parts of the plants were air-dried, powdered, and successively extracted with solvents of increasing polarity to obtain hexane, dichloromethane, ethyl-acetate, n-butanol and methanol extracts. The cytotoxic activities of the extracts against human cervix adenocarcinoma HeLa, human melanoma Fem-x, human myelogenous leukemia K562, human breast adenocarcinoma MDA-MB-361 cells and PBMC were evaluated by the MTT test. The mode of HeLa cell death was investigated by morphological analysis. Changes in the cell cycle of HeLa cells treated with the extracts were analyzed by flow cytometry. The apoptotic mechanisms induced by the tested extracts were determined using specific caspase inhibitors. Results The investigated Helichrysum zivojinii extracts exerted selective dose-dependent cytotoxic actions against selected cancer cell lines and healthy immunocompetent PBMC stimulated to proliferate, while the cytotoxic actions exerted on unstimulated PBMC were less pronounced. The tested extracts exhibited considerably stronger cytotoxic activities towards HeLa, Fem-x and K562 cells in comparison to resting and stimulated PBMC. It is worth noting that the cytotoxicity of the extracts was weaker against unstimulated PBMC in comparison to stimulated PBMC. Furthermore, each of the five extracts induced apoptosis in HeLa cells, through the activation of both intrinsic and extrinsic signaling pathways. Conclusion Extracts obtained from the endemic plant Helichrysum zivojinii may represent an important source of novel potential antitumor agents due to their pronounced and selective cytotoxic actions towards malignant cells.

In this work we investigated the direct or indirect (through ADCC) cytotoxic action of Herceptin, to two breast carcinoma cell lines: to MDA-MB 361, for HER-2, IHC score (3+) and to MDA-MB 453, IHC score (

Antiproliferative and antibacterial activities of nine glutarimide derivatives (1–9) were reported. Cytotoxicity of compounds was tested toward three human cancer cell lines, HeLa, K562 and MDA-MB-453 by MTT assay. Compound7(2-benzyl-2-azaspiro[5.11]heptadecane-1,3,7-trione), containing 12-membered ketone ring, was found to be the most potent toward all tested cell lines (IC50 = 9–27 μM). Preliminary screening of antibacterial activity by a disk diffusion method showed that Gram-positive bacteria were more susceptible to the tested compounds than Gram-negative bacteria. Minimum inhibitory concentration (MIC) determined by a broth microdilution method confirmed that compounds1,2,4,6–8and9inhibited the growth of all tested Gram-positive and some of the Gram-negative bacteria. The best antibacterial potential was achieved with compound9(ethyl 4-(1-benzyl-2,6-dioxopiperidin-3-yl)butanoate) againstBacillus cereus(MIC 0.625 mg/mL; 1.97 × 10−3 mol/L). Distinction between more and less active/inactive compounds was assessed from the pharmacophoric patterns obtained by molecular interaction fields. [ABSTRACT FROM PUBLISHER]