[1-(2-Oxidobenzyl­idene)-4-phenyl­thio­semicarbazidato-κ3 O,N 1,S](pyridine-κN)copper(II)

In the structure of the title compound, [Cu(C14H11N3OS)(C5H5N)], the CuII atom exhibits a slightly distorted square-planar CuN2OS coordination polyhedron consisting of a phenyl O, an azomethine N and a thio­amide S atom from the tridentate thio­semicarbazonate dianion, and the N atom of a pyridine mol­ecule. The thio­semicarbazonate ligand exists in the thiol tautomeric form as an E isomer. Rotational disorder of the pyridine and phenyl rings in a 1:1 ratio of the respective components is observed. An extensive network of weak N—H⋯S, C—H⋯O, C—H⋯N and C—H⋯S hydrogen-bonding inter­actions consolidates the structure

Substitued (E)-b-(benzoyl)acrylic acids suppressed survival of neoplastic human HeLa cells

The bacteriostatic activity of some of alkyl substituted (E)-b-(benzoyl)acrylic acids was shown earlier. The aim of this study was to investigate the antiproliferative action of 19 alkyl-, or halogeno-, or methoxy-, or acetamido- substituted (E)-b-(benzoyl)acrylic acids, against human cervix carcinoma, HeLa, cells. Target HeLa cells were continuously treated with increasing concentrations of substituted (E)-b-(benzoyl)acrylic acids during two days. The MTT test was used for assessment of the antiproliferative action of this group of compounds. Treatment of HeLa cells with 4-methyl-, 4-fluoro-, 4-chloro-, 4-bromo- and 4-methoxy- derivatives of (E)-b-(benzoyl) acrylic acid leads to the expression of cytostatic activity against HeLa cells (IC50 were in the range from 31-40 µM). Their antiproliferative action was less than that of the basic compound (E)-b-(benzoyl)acrylic acid whose IC50 was 28.5 µM. The 3,4-dimethyl-, 2,4-dimethyl- and 2,5-dimethyl- derivatives as well as the 4-ethyl- and 3,4-dichloro- and 2,4-dichloro-derivatives, have stronger cytostatic activity than the correspoding monosubstituted and parent compound. Their IC50 were 18.5 µM; 17.5 µM; 17.0 mM; 17.5 µM; 22.0 µM and 18 µM, respectively. The 4-iso-propyl- and 4-n-butyl-derivatives exerted higher cytostatic activity than the compounds with a lower number of methylene -CH2- groups in the substitutent. Their IC50 were 14.5 µM and 6.5 µM respectively. The 2,5-di-iso-propyl- and 4-tert-butyl-derivatives expressed the most strong antiproliferative action against the investigated HeLa cells, IC50 being 4.5 µM and 5.5 µM, respectively. The investigated compounds affected the survival of HeLa cells, expressing a strong structure-activity relationship of the Hansch type

Evaluation of in vitro antioxidant, antimicrobial, genotoxic and anticancer activities of lichen Cetraria islandica

© 2014, Springer Science+Business Media Dordrecht. In this study, the antioxidant, antimicrobial, genotoxic and anticancer activities of Cetraria islandica methanol extract were determined by using free radical and superoxide anion scavenging activity, reducing power, determination of total phenolic compounds and flavonoid contents, broth microdilution minimal inhibitory concentration against five bacterial and five fungal species, cytokinesis block micronucleus (MN) assay on peripheral blood lymphocytes (PBLs) and the microculture tetrazolium test on FemX (human melanoma) and LS174 (human colon carcinoma) cell lines. As a result of the study, we found that C. islandica methanol extract exhibited moderate free-radical-scavenging activity with IC50 values 678.38 μg/ml. Moreover, the tested extract had effective reducing power and superoxide anion radical scavenging. The minimal inhibitory concentration values against the tested microorganisms ranged from 0.312 to 5 mg/ml. The extract increased MN frequency in a dose dependent manner, but it was significant in higher tested concentrations (50, 100 and 200 μg/ml). No significant differences were observed between NDI values in all treatments and untreated PBLs. In addition, the tested extract had strong anticancer activity towards both cell lines with IC50 values of 22.68 and 33.74 μg/ml. It can be concluded that the tested extract exhibited a certain level of in vitro antioxidant, antimicrobial, genotoxic and anticancer activities

Seasonal variation in biopharmaceutical activity and fatty acid content of endemic Fucus virsoides algae from Adriatic sea

© 2019 Polish Pharmaceutical Society. All rights reserved. Macroalgae from Fucus genus are a valuable source of bioactive components as they are abundant in complex polysaccharides, fatty acids and polyphenols. In this work, the biological activity and chemical composition of extracts and fractions obtained from endemic Fucus virsoides J. Agardh species collected in the summer and the fall were investigated. From dichloromethane:methanol (1: 1) extract three fractions were made: petroleum-ether, ethyl-acetate and n-butanol. The aim of the study was to examine the influence of the seasonal variations on algal composition and activity. The significant seasonal variation in content and biological activity of Fucus virsoides samples was found. Fall extract and fractions exerted higher cytotoxic effects on cancer cell lines in comparison with summer extract and fractions. The examined extracts and fractions showed higher cytotoxic activity towards cancer cells compared to normal fibroblast MRC-5 cells. Morphological evaluation and cell cycle distribution analysis demonstrated their proapoptotic activity in human cervical adenocarcinoma HeLa cells. Fall extract and fractions better suppressed the migration and tube formation of EA.hy926 cells in comparison with summer extract and fractions. Fall extract and fractions were more potent in inhibition of α-glucosidase enzymatic activity. Ethyl-acetate fractions, from both seasons, exhibited the best antibacterial and antifungal activity on all tested bacteria and fungi. In conclusion, the two fall fractions ethyl-acetate and petroleum-ether rich in polyphenols and polyunsaturated fatty acids were the most active and exhibited prominent anticancer and anti-α-glucosidase activities

Phytochemical study and antioxidant, antimicrobial and anticancer activities of Melanelia subaurifera and Melanelia fuliginosa lichens

© 2016, Association of Food Scientists & Technologists (India). The aim of this study was to investigate antioxidant, antimicrobial and anticancerous activity of Melanelia subaurifera and Melanelia fuliginosa. The phytochemical analysis was determined by HPLC–UV method. Antioxidant activity was evaluated by DPPH and reducing power assay while antimicrobial activity was determined by minimal inhibitory concentration. The cytotoxic activity was tested using MTT method. The method for quantification of 2′-O-methyl anziaic acid and lecanoric acid in these lichens using RF-HPLC was also developed and validated. The depsides (lecanoric acid, gyrophoric acid, atranorin, anziaic acid and 2′-O-methyl anziaic acid), and dibenzofurane (usnic acid) were identified in these lichens. The antioxidant activity (IC50) of lichens extracts ranged from 121.52 to 424.51 μg/ml. 2′-O-Methyl anziaic acid showed the highest antimicrobial activity with MIC ranging from 0.0625 to 1 mg/ml. M. subaurifera extract showed the highest cytotoxic activity against the tested cell lines (IC50 = 9.88 to 31.64 μg/ml)

Synthesis, characterization, antimicrobial and cytotoxic activity and DNA-binding properties of d-metal complexes with hydrazones of Girard’s T and P reagents

Abstract: In this work synthesis, characterization and crystal structures of 1, Zn(II) complex ([ZnL1(NCS)2]), with (E)-1-(2-oxo-2-(2-(quinolin-2-ylmethylene)hydrazinyl)ethyl)pyridin-1-ium chloride (HL1Cl) and 2, Bi(III) complex ([BiHL2Cl4] × 1/2CH3OH), with (E)-N,N,N-trimethyl-2-oxo-2-(2-(1-(thiazol-2-yl)ethylidene)hydrazinyl)ethan-1-aminium chloride (HL2Cl), have been reported. Zn(II) complex possesses a distorted trigonal bipyramidal geometry while surroundings around Bi(III) ion are extended pentagonal bipyramidal. Antimicrobial activity, brine shrimp assay and DPPH radical scavenging activity of both complexes, including previously synthesized complexes with HL2Cl ligand (Zn(II) and Ni(II)) and complexes with (E)-N,N,N-trimethyl-2-oxo-2-(2-(1-(pyridin-2-yl)ethylidene)hydrazinyl)ethan-1-aminium chloride (HL3Cl) (Zn(II), Cu(II), Cd(II), Co(II), Fe(III), Ni(II)), were evaluated. For the most active complexes, cytotoxic activity against five malignant cancer cell lines (HeLa, A375, MCF7, PC-3 and A549) and normal cell line HaCaT, as well as generation of reactive oxygen species (ROS), was tested. Graphic abstract: [Figure not available: see fulltext.