Influence of ligand structure on anticancer and antioxidant properties of rhenium cluster compounds

Досліджено протипухлинну активність системи реній-платину, що містить цис-дикарбоксилати ренію (ІІІ) із різними алкільними лігандами, кількість еритроцитів крові, їх морфологічний склад, еритроцитарну стійкість, концентрацію гемоглобіну крові, активність каталази, вміст ТБК-активних продуктів у плазмі крові щурів при розвитку карциноми Герена Т8 щурів. Показано, що система реній-платину має значний антиоксидантний ефект і пригнічує ріст пухлини, що є максимальним для сполуки з півалатним лігандомИсследованы противоопухолевая активность системы рений-платина, которая содержит цис-дикарбоксилаты рения (III) с разными алкильными лигандами, количество эритроцитов крови, их морфологический состав, эритроцитарная стойкость, концентрация гемоглобина в крови, активность каталазы, концентрация ТБК-активных продуктов плазмы крови крыс при развитии карциномы Герена Т8 крыс. Показано, что система рений-платина имеет значительный антиоксидантный эффект и угнетает рост опухоли, что является максимальным для соединения с пивалатным лигандом.Under the model growth of T8 Guerin’s carcinoma in rats we studied the anticancer activity of the system rhenium-platinum, which includes cis-dicarboxylates of rhenium (III) with different alkyl ligands, erythrocytes number and its morphological structure, erythrocytic stability, blood haemoglobin concentration, catalase activity and concentration of TBA-active products in the rats blood plasma. The renium-platinum system had considerable antioxidat effect and prevented the growth of tumour, that was maximal for a compound with the pivalate ligand

POTENTIAL OF BUSINESS ENTITIES: ESSENCE, ASSESSMENT AND ROLE IN NATIONAL DEVELOPMENT

The behavior of macroeconomic indicators (reflecting the development of both the national economy as a whole and that of individual economic sectors) testifies to the low current efficiency of the functioning of economic entities in the context of economic activities. This in turn necessitates scientific substantiation of developing and introducing theoretical and methodological recommendations to ensure innovative development of the country. One of the most effective ways to practically implement this task is to substantiate methods for quantitative assessment of potential in the context of economic activities. The practical value of applying these methods is that the results of the integrated assessment of potential can be used as a criterion for the priority development of certain economic sectors or economic activities

Bioengineered riboflavin in nanotechnology

Riboflavin (RF) is an essential water-soluble vitamin with unique biological and physicochemical properties such as transporterspecific cell internalization, implication in redox reactions, fluorescence and photosensitizing. Due to these features RF attracted researchers in various fields from targeted drug delivery and tissue engineering to optoelectronics and biosensors. In this review we will give a brief reminder of RF chemistry, its optical, photosensitizing properties, RF transporter systems and its role in pathologies. We will point a special attention on the recent findings concerning RF applications in nanotechnologies such as RF functionalized nanoparticles, polymers, biomolecules, carbon nanotubes, hydrogels and implants for tissue engineering

Вплив структури ліганду на протипухлинні та антиоксидантні властивості кластерних сполук ренію

Under the model growth of T8 Guerin’s carcinoma in rats we studied the anticancer activity of the system rhenium-platinum, which includes cis-dicarboxylates of rhenium (III) with different alkyl ligands, erythrocytes number and its morphological structure, erythrocytic stability, blood haemoglobin concentration, catalase activity and concentration of TBA-active products in the rats blood plasma. The renium-platinum system had considerable antioxidat effect and prevented the growth of tumour, that was maximal for a compound with the pivalate ligand

Mimicking photosystem I with a transmembrane light harvester and energy transfer-induced photoreduction in phospholipid bilayers

Photosystem I (PS I) is a transmembrane protein that assembles perpendicular to the membrane, and performs light harvesting, energy transfer, and electron transfer to a final, water-soluble electron acceptor. We present here a supramolecular model of it formed by a bicationic oligofluorene 1(2+) bound to the bisanionic photoredox catalyst eosin Y (EY2-) in phospholipid bilayers. According to confocal microscopy, molecular modeling, and time dependent density functional theory calculations, 1(2+) prefers to align perpendicularly to the lipid bilayer. In presence of EY2-, a strong complex is formed (K-a=2.1 +/- 0.1x10(6) m(-1)), which upon excitation of 1(2+) leads to efficient energy transfer to EY2-. Follow-up electron transfer from the excited state of EY2- to the water-soluble electron donor EDTA was shown via UV-Vis absorption spectroscopy. Overall, controlled self-assembly and photochemistry within the membrane provides an unprecedented yet simple synthetic functional mimic of PS I.Metals in Catalysis, Biomimetics & Inorganic Material

Photoacoustic imaging of tumor targeting with riboflavin-functionalized theranostic nanocarriers

Nataliia Beztsinna,1,* Yoanna Tsvetkova,2,* Jithin Jose,3 Boutayna Rhourri-Frih,1 Wa’el Al Rawashdeh,2 Twan Lammers,2 Fabian Kiessling,2 Isabelle Bestel1 1Institute of Chemistry & Biology of Membranes & Nanoobjects (CBMN), UMR 5248, University of Bordeaux, Pessac, France; 2Institute for Experimental Molecular Imaging, RWTH Aachen University Clinic, Aachen, Germany; 3Fujifilm VisualSonics BV, Amsterdam, the Netherlands *These authors contributed equally to this work Abstract: Photoacoustic imaging is an emerging method in the molecular imaging field, providing high spatiotemporal resolution and sufficient imaging depths for many clinical applications. Therefore, the aim of this study was to use photoacoustic imaging as a tool to evaluate a riboflavin (RF)-based targeted nanoplatform. RF is internalized by the cells through a specific pathway, and its derivatives were recently shown as promising tumor-targeting vectors for the drug delivery systems. Here, the RF amphiphile synthesized from a PEGylated phospholipid was successfully inserted into a long-circulating liposome formulation labeled with the clinically approved photoacoustic contrast agent – indocyanine green (ICG). The obtained liposomes had a diameter of 124 nm (polydispersity index =0.17) and had a negative zeta potential of –26 mV. Studies in biological phantoms indicated a stable and concentration-dependent photoacoustic signal (Vevo® LAZR) of the ICG-containing RF-functionalized liposomes. In A431 cells, a high uptake of RF-functionalized liposomes was found and could be blocked competitively. First, studies in mice revealed ~3 times higher photoacoustic signal in subcutaneous A431 tumor xenografts (P<0.05) after injection of RF-functionalized liposomes compared to control particles. In this context, the application of a spectral unmixing protocol confirmed the initial quantitative data and improved the localization of liposomes in the tumor. In conclusion, the synthesized RF amphiphile leads to efficient liposomal tumor targeting and can be favorably detected by photoacoustic imaging with a perspective of theranostic applications. Keywords: photoacoustic imaging, long-circulating liposomes, active targeting, riboflavin, indocyanine green&nbsp

Mimicking Photosystem I with a Transmembrane Light Harvester and Energy Transfer‐Induced Photoreduction in Phospholipid Bilayers

Photosystem I (PS I) is a transmembrane protein that assembles perpendicular to the membrane, and performs light harvesting, energy transfer, and electron transfer to a final, water-soluble electron acceptor. We present here a supramolecular model of it formed by a bicationic oligofluorene 1(2+) bound to the bisanionic photoredox catalyst eosin Y (EY2-) in phospholipid bilayers. According to confocal microscopy, molecular modeling, and time dependent density functional theory calculations, 1(2+) prefers to align perpendicularly to the lipid bilayer. In presence of EY2-, a strong complex is formed (K-a=2.1 +/- 0.1x10(6) m(-1)), which upon excitation of 1(2+) leads to efficient energy transfer to EY2-. Follow-up electron transfer from the excited state of EY2- to the water-soluble electron donor EDTA was shown via UV-Vis absorption spectroscopy. Overall, controlled self-assembly and photochemistry within the membrane provides an unprecedented yet simple synthetic functional mimic of PS I.Metals in Catalysis, Biomimetics & Inorganic Material

Quantitative analysis of receptor-mediated uptake and pro-apoptotic activity of mistletoe lectin-1 by high content imaging

Abstract Ribosome inactivating proteins (RIPs) are highly potent cytotoxins that have potential as anticancer therapeutics. Mistletoe lectin 1 (ML1) is a heterodimeric cytotoxic protein isolated from European Mistletoe and belongs to RIP class II. The aim of this project was to systematically study ML1 cell binding, endocytosis pathway(s), subcellular processing and apoptosis activation. For this purpose, state of the art cell imaging equipment and automated image analysis algorithms were used. ML1 displayed very fast binding to sugar residues on the membrane and energy-dependent uptake in CT26 cells. The co-staining with specific antibodies and uptake blocking experiments revealed involvement of both clathrin-dependent and -independent pathways in ML1 endocytosis. Co-localization studies demonstrated the toxin transport from early endocytic vesicles to Golgi network; a retrograde road to the endoplasmic reticulum. The pro-apoptotic and antiproliferative activity of ML1 were shown in time lapse movies and subsequently quantified. ML1 cytotoxicity was less affected in multidrug resistant tumor cell line 4T1 in contrast to commonly used chemotherapeutic drug (ML1 resistance index 6.9 vs 13.4 for doxorubicin; IC50: ML1 1.4 ng/ml vs doxorubicin 24000 ng/ml). This opens new opportunities for the use of ML1 as an alternative treatment in multidrug resistant cancers