Łukasz Popiołek

The many “faces” of copper in medicine and treatment

Copper (Cu) is an essential microelement found in all living organisms with the unique ability to adopt two different redox states—in the oxidized (Cu2+) and reduced (Cu+). It is required for survival and serves as an important catalytic cofactor in redox chemistry for proteins that carry out fundamental biological functions, important in growth and development. The deficit of copper can result in impaired energy production, abnormal glucose and cholesterol metabolism, increased oxidative damage, increased tissue iron (Fe) accrual, altered structure and function of circulating blood and immune cells, abnormal neuropeptides synthesis and processing, aberrant cardiac electrophysiology, impaired myocardial contractility, and persistent effects on the neurobehavioral and the immune system. Increased copper level has been found in several disorders like e.g.: Wilson’s disease or Menke’s disease. New findings with the great potential for impact in medicine include the use of copper-lowering therapy for antiangiogenesis, antifibrotic and anti-inflammatory purposes. The role of copper in formation of amyloid plaques in Alzheimer’s disease, and successful treatment of this disorder in rodent model by copper chelating are also of interest. In this work we will try to describe essential aspects of copper in chosen diseases. We will represent the evidence available on adverse effect derived from copper deficiency and copper excess. We will try to review also the copper biomarkers (chosen enzymes) that help reflect the level of copper in the body.

Synthesis and Antimicrobial Activity of New 1,3-Thiazolidin-4-one Derivatives Obtained from Carboxylic Acid Hydrazides

GRAPHICAL ABSTRACT Abstract This study presents the synthesis, spectral analysis, and antimicrobial evaluation of a new series of 1,3-thiazolidin-4-one derivatives. New compounds were prepared by the reaction of N-substituted carboxylic acid hydrazide derivatives with thioglycolic acid. The structures of the obtained compounds were confirmed by means of 1H NMR and 13C NMR. All the synthesized compounds were screened for their in vitro antibacterial and antifungal activities using the broth microdilution method against a panel of reference strains of 20 microorganisms, including 10 strains of Gram-positive bacteria, 7 strains of Gram-negative bacteria, and fungi belonging to 3 yeasts of Candida spp. Our results indicate that some of the investigated compounds showed good to mild bioactivity, with bacteriostatic or fungistatic effect against reference strains of Gram-positive bacteria, mainly M. luteus and yeast belonging to Candida spp., especially C. albicans.

Hydrazide–hydrazones as potential antimicrobial agents: overview of the literature since 2010

Hydrazide–hydrazone derivatives are present in many bioactive molecules and display a wide variety of biological activities, such as antibacterial, antitubercular, antifungal, anticancer, anti-inflammatory, anticonvulsant, antiviral, and antiprotozoal action. Therefore, many medicinal chemists synthesize various hydrazide–hydrazones and evaluate them for biological activities. Among biological properties of this class of compounds, antimicrobial activity is the most frequently encountered in scientific literature. This paper is focused on the overview of the literature findings of the last six years (2010–2016) covering the research on antimicrobial activity of hydrazide–hydrazone derivatives. This review may also serve as a useful guide for the development of new hydrazide–hydrazones as potential antimicrobial agents.

Characteristics of hematopoietic stem cells of umbilical cord blood

Umbilical cord blood collected from the postpartum placenta and cord is a rich source of hematopoietic stem cells (HSCs) and is an alternative to bone marrow transplantation. In this review we wanted to describe the differences (in phenotype, cytokine production, quantity and quality of cells) between stem cells from umbilical cord blood, bone marrow and peripheral blood. HSCs present in cord blood are more primitive than their counterparts in bone marrow or peripheral blood, and have several advantages including high proliferation. With using proper cytokine combination, HSCs can be effectively developed into different cell lines. This process is used in medicine, especially in hematology.

Synthesis and Antimicrobial Evaluation of New Schiff Base Hydrazones Bearing 1,2,4-Triazole Moiety

GRAPHICAL ABSTRACT Abstract This study presents the synthesis and spectral analysis of new Schiff base hydrazone derivatives. New compounds were prepared by the reaction of [(4-phenyl-5-substituted-4H-1,2,4-triazol-3-yl)sulfanyl] acetohydrazide with various aldehydes. The structures of the prepared compounds were confirmed by means of 1H NMR, 13C NMR, and elemental analyses. All synthesized compounds were screened for their in vitro antimicrobial activity by using the agar dilution technique against four reference strains of Gram-positive and Gram-negative bacteria and 12 yeasts belonging to Candida spp.

Hydrazide-hydrazones of 3-methoxybenzoic acid and 4-tert-butylbenzoic acid with promising antibacterial activity against Bacillus spp.

Abstract A series of 28 hydrazide-hydrazones of 3-methoxybenzoic and 4-tert-butylbenzoic acid were synthesized and screened in vitro against the panel of reference strains of bacteria and fungi with the use of the broth microdilution method according to EUCAST and CLSI guidelines. Five of the synthesized compounds were found to exhibit high bacteriostatic or bactericidal activity against Gram-positive bacteria. The antimicrobial activity of compounds 13, 14, and 16 against Bacillus spp. was higher than that of commonly used antibiotics, like cefuroxime or ampicillin.

Synthesis, antiproliferative and antimicrobial activity of new Mannich bases bearing 1,2,4-triazole moiety

Abstract This study presents the synthesis, antiproliferative and antimicrobial evaluation of a new series of Mannich base derivatives containing 1,2,4-triazole system. New compounds were prepared by the reaction of 4,5-disubstituted 1,2,4-triazole-3-thiones with formaldehyde and various amines. The structures of the prepared compounds were confirmed by means of 1H NMR, 13C NMR and elemental analyses. Twelve compounds were evaluated for their in vitro antiproliferative activities against six chosen cancer cell lines. All synthesized compounds were screened for their in vitro antimicrobial activity by using the agar dilution technique. For 17 potentially active compounds, their antibacterial activity was confirmed on the basis of MIC (minimal inhibitory concentration) by broth microdilution method using the reference Gram-positive and Gram-negative bacterial strains.

Synthesis and in vitro antimicrobial activity of new 4-phenyl-5-methyl-4H-1,2,4-triazole-3-thione derivatives

This study presents the synthesis, spectral analysis and antimicrobial evaluation of a new series of substituted 1,2,4-triazole (5a–i) and 1,3,4-thiadiazole derivatives (9a, c, g, h). New compounds were obtained by cyclization reaction of acyl thiosemicarbazide derivatives in the presence of alkaline and acidic media. All synthesized compounds were screened for their in vitro antimicrobial activities. Nine of the compounds had potential activity against Gram-positive bacteria (MIC = 3.91–500 µg/mL). Some compounds showed good activity especially against: Micrococcus luteus ATCC 10240 (MIC = 3.91−31.25 µg/mL), Bacillus subtilis ATCC 6633 (MIC = 15.63− 62.5 µg/mL), and Staphylococcus aureus ATCC 25923 (MIC = 15.63−125 µg/mL).

Design, synthesis, and in vitro antimicrobial activity of hydrazide-hydrazones of 2-substituted acetic acid.

In this study, 30 hydrazide–hydrazones of phenylacetic (3–10) and hydroxyacetic acid (11–32) were synthesized by the condensation reaction of appropriate 2‐substituted acetic acid hydrazide with different aromatic aldehydes. The obtained compounds were characterized by spectral data and evaluated in vitro for their potential antimicrobial activities against a panel of reference strains of micro‐organisms, including Gram‐positive bacteria, Gram‐negative bacteria, and fungi belonging to the Candida spp. The results from our antimicrobial assays indicated that among synthesized compounds 3–32, especially compounds 6, 14, and 26 showed high bactericidal activity (MIC = 0.488–7.81 μg/ml) against reference Gram‐positive bacteria, and in some cases, their activity was even better than that of commonly used antibiotics, such as cefuroxime or ampicillin.

Synthesis and investigation of antimicrobial activities of nitrofurazone analogues containing hydrazide-hydrazone moiety

Graphical abstract