[Experimental substantiation of medical device design for mechanical processing of adipose tissue].

Objective: To substantiate the medical device design for mechanical processing of adipose tissue.

Material And Methods: Enzymatic method using collagenase and mechanical method for obtaining the stromal vascular fraction (SVF) are compared. The authors emphasized the disadvantages of enzymatic method, such as high cost and duration of process.

Naphthoindole-2-carboxamides as a lipophilic chemotype of hetarene-anthraquinones potent against P-gp resistant tumor cells.

The acquisition of multidrug resistance (MDR) to chemotherapy is a major obstacle to successful cancer treatment. Aiming to improve the potency of anthraquinone-derived antitumor compounds against MDR cancer cells, we employed a rational design approach to develop new heteroarene-fused anthraquinones. Shifting the carboxamide group in the naphtho[2,3-f]indole scaffold from the 3-position to 2 increased the lipophilicity and P-glycoprotein (P-gp) binding of the derivatives, potentially enhancing their ability to circumvent P-gp-mediated MDR.

Hapten Synthesis, Antibody Generation, and Immunoassay Development for Linezolid Therapeutic Monitoring.

Linezolid (LNZ) is a broad-spectrum antibiotic used for the treatment of severe Gram+ infections. Significant pharmacokinetic variability in different groups of patients requires therapeutic drug monitoring (TDM) to ensure optimal therapy. This article presents the first description of the development of immunoanalytical TDM systems for LNZ.

Evaluation of Minimum-to-Severe Global and Macrovesicular Steatosis in Human Liver Specimens: A Portable Ambient Light-Compatible Spectroscopic Probe.

Background And Aims: Hepatic steatosis (HS), particularly macrovesicular steatosis (MaS), influences transplant outcomes. Accurate assessment of MaS is crucial for graft selection. While traditional assessment methods have limitations, non-invasive spectroscopic techniques like Raman and reflectance spectroscopy offer promise.

Synthesis and antiproliferative activity of thiazole-fused anthraquinones.

Heterocyclic derivatives of anthraquinone demonstrated a high potential for the development of new antitumor compounds. In this study, we report a scheme for the synthesis of thiazole-fused anthraquinones and the results of their antiproliferative activity. A convenient metal-free method for the thiolation of anthraquinone derivatives has been proposed for the preparation of the key intermediates.

Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells.

The antibiotic heliomycin (resistomycin), which is generated from , has multiple activities, including anticancer effects. Heliomycin was first described in the 1960s, but its clinical applications have been hindered by extremely low solubility. A series of 4-aminomethyl derivatives of heliomycin were synthesized to increase water solubility; studies showed that they had anti-proliferative effects, but the drug targets remained unknown.

Hybrid Molecules of Azithromycin with Chloramphenicol and Metronidazole: Synthesis and Study of Antibacterial Properties.

The sustained rise of antimicrobial resistance (AMR) causes a strong need to develop new antibacterial agents. One of the methods for addressing the problem of antibiotic resistance is through the design of hybrid antibiotics. In this work, we proposed a synthetic route for the conjugation of an azithromycin derivative with chloramphenicol and metronidazole hemisuccinates and synthesized two series of new hybrid molecules - and -.

Thiadiazole-, selenadiazole- and triazole-fused anthraquinones as G-quadruplex targeting anticancer compounds.

G-quadruplex (G4) ligands attract considerable attention as potential anticancer therapeutics. In this study we proposed an original scheme for synthesis of azole-fused anthraquinones and prepared a series of G4 ligands carrying amino- or guanidinoalkylamino side chains. The heterocyclic core and structure of the terminal groups strongly affect on binding to G4-forming oligonucleotides, cellular accumulation and antitumor potency of compounds.

An interferometric-based tensile tester to resolve damage events within reconstituted multi-filaments collagen bundles.

Understanding how mechanical damage propagates in load-bearing tissues such as skin, tendons and ligaments, is key to developing regenerative medicine solutions for when these tissues fail. For collagenous tissues in particular, damage is typically assessed after mechanical testing using a broad range of microscopy techniques because standard tensile testing systems do not have the time and force sensitivity to resolve mechanical damage events. Here we introduce an interferometric detection scheme to measure the displacement of a cantilever with a resolution of 0.

Synthesis and antitumor activity of cyclopentane-fused anthraquinone derivatives.

In our pursuit of developing novel analogs of anthracyclines with enhanced antitumor efficacy and safety, we have designed a synthesis scheme for 4,11-dihydroxy-5,10-dioxocyclopenta[b]anthracene-2-carboxamides. These newly synthesized compounds exhibit remarkable antiproliferative potency against various mammalian tumor cell lines, including those expressing activated mechanisms of multidrug resistance. The structure of the diamine moiety in the carboxamide side chain emerges as a critical determinant for anticancer activity and interaction with key targets such as DNA, topoisomerase 1, and ROS induction.

Identification of Key Genes Involved in Response to or spp. Infections in Human Cell Lines and in Mouse Organs.

Bacterial infections represent an unsolved problem today since bacteria can evade antibiotics and suppress the host's immune response. A family of TRIM proteins is known to play a role in antiviral defense. However, the data on the involvement of the corresponding genes in the antibacterial response are limited.

Evaluation of the Information Content for Determining the Vascular Tone Type of the Lower Extremities in Varicose Veins: A Case Study.

The incidence of cardiovascular diseases is continuously increasing around the world. Therefore, the study of new methods for diagnosing cardiovascular diseases is very important. Early diagnosis and evaluation of the effectiveness of treatments are among the most important tasks.

Design, Synthesis and In Vitro Investigation of Cabozantinib-Based PROTACs to Target c-Met Kinase.

(1) Background: This investigation aimed at developing a series of c-Met-targeting cabozantinib-based PROTACs. (2) Methods: Purification of intermediate and target compounds was performed using column chromatography, in vitro antiproliferation activity was measured using a standard MTT assay and a c-Met degradation assay was performed via the immunoblotting technique. (3) Results: Several compounds exhibited antiproliferative activity towards different cell lines of breast cancer (T47D, MDA-MB-231, SKBR3, HCC1954 and MCF7) at the same level as parent cabozantinib and 7-demethyl cabozantinib.

Real-time assessment of liver fat content using a filter-based Raman system operating under ambient light through lock-in amplification.

During liver procurement, surgeons mostly rely on their subjective visual inspection of the liver to assess the degree of fatty infiltration, for which misclassification is common. We developed a Raman system, which consists of a 1064 nm laser, a handheld probe, optical filters, photodiodes, and a lock-in amplifier for real-time assessment of liver fat contents. The system performs consistently in normal and strong ambient light, and the excitation incident light penetrates at least 1 mm into duck fat phantoms and duck liver samples.

Computational and Biophysical Characterization of Heterocyclic Derivatives of Anthraquinone against Human Aurora Kinase A.

Human Aurora kinase A (AurA) has recently garnered the attention of researchers worldwide as a promising effective mitotic drug target for its involvement in cancer and related inflammatory anomalies. This study has explored the binding affinity of newly identified heteroarene-fused anthraquinone derivatives against AurA. Molecular docking analyses showed that all the heteroanthraquinone compounds bind to AurA with different affinities.

Bis(chloroacetamidino)-Derived Heteroarene-Fused Anthraquinones Bind to and Cause Proteasomal Degradation of tNOX, Leading to c-Flip Downregulation and Apoptosis in Oral Cancer Cells.

Anthraquinone-based intercalating compounds, namely doxorubicin and mitoxantrone, have been used clinically based on their capacity to bind DNA and induce DNA damage. However, their applications have been limited by side effects and drug resistance. New-generation anthraquinone derivatives fused with different heterocycles have been chemically synthesized and screened for higher anticancer potency.

Heterocyclic ring expansion yields anthraquinone derivatives potent against multidrug resistant tumor cells.

Chemical modifications of anthraquiones are aimed at novel derivatives with improved antitumor properties. Emergence of multidrug resistance (MDR) due to overexpression of transmembrane ATP binding cassette transporters, in particular, MDR1/P-glycoprotein (Pgp), can limit the use of anthraquinone based drugs. Previously we have demonstrated that annelation of modified five-membered heterocyclic rings with the anthraquinone core yielded a series of compounds with optimized antitumor properties.

Photosensitization of pancreatic cancer cells by cationic alkyl-porphyrins in free form or engrafted into POPC liposomes: The relationship between delivery mode and mechanism of cell death.

Cationic porphyrins bearing an alkyl side chain of 14 (2b) or 18 (2d) carbons dramatically inhibit proliferation of pancreatic cancer cells following treatment with light. We have compared two different ways of delivering porphyrin 2d: either in free form or engrafted into palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine liposomes (L-2d). Cell cytometry shows that while free 2d is taken up by pancreatic cancer cells by active (endocytosis) and passive (membrane fusion) transports, L-2d is internalized solely by endocytosis.

Possible risks for the functioning of cyclic processes in the experimental model of a closed ecosystem.

The purpose of the present study is to consider a number of possible risks that may emerge when processed human wastes are involved into mass exchange processes as fertilizers for plants cultivated in the experimental model of the closed ecosystem (CEEM). The problems relating to the disruption of cycling processes in closed ecosystems can be tentatively divided into two groups: the problems that can be rather easily overcome and the chronic problems. Addition of plant inedible biomass to the soil-like substrate (SLS) can result in a decrease in plant productivity because of allelopathic interactions and enhanced growth of microorganisms.

Modeling a lunar base mushroom farm.

To calculate the equivalent system mass of mushrooms, a conceptual configuration of a mushroom farm as part of a bioregenerative life support system on an inhabited lunar base was designed. The mushroom farm consists of two connected modules. Each module is a double-shell rigid pipe-in-pipe aluminum structure.

Antibiotic heliomycin and its water-soluble 4-aminomethylated derivative provoke cell death in T24 bladder cancer cells by targeting sirtuin 1 (SIRT1).

Bladder cancer is one of the most frequent cancers among males, and a poor survival rate reflects problems with aggressiveness and chemo-resistance. Accumulating evidence indicates that SIRT1 is involved in bladder cancer tumorigenesis and is positively associated with chemo-resistance and poor prognosis. We recently synthesized water-soluble chemical derivatives of heliomycin, an antibiotic from , and demonstrated that they possess anticancer properties.

Multi-Channel Bioimpedance System for Detecting Vascular Tone in Human Limbs: An Approach.

Vascular tone plays a vital role in regulating blood pressure and coronary circulation, and it determines the peripheral vascular resistance. Vascular tone is dually regulated by the perivascular nerves and the cells in the inside lining of blood vessels (endothelial cells). Only a few methods for measuring vascular tone are available.

Determination of the Geometric Parameters of Electrode Systems for Electrical Impedance Myography: A Preliminary Study.

The electrical impedance myography method is widely used in solving bionic control problems and consists of assessing the change in the electrical impedance magnitude during muscle contraction in real time. However, the choice of electrode systems sizes is not always properly considered when using the electrical impedance myography method in the existing approaches, which is important in terms of electrical impedance signal expressiveness and reproducibility. The article is devoted to the determination of acceptable sizes for the electrode systems for electrical impedance myography using the Pareto optimality assessment method and the electrical impedance signals formation model of the forearm area, taking into account the change in the electrophysical and geometric parameters of the skin and fat layer and muscle groups when performing actions with a hand.

Bioregenerative life support space diet and nutrition requirements: still seeking accord.

The capability of "dish" and "ingredient in dish" modeling to reduce the number of nutrition imbalances in bioregenerative life support diet was compared. Masses of dishes were assumed to be the independent variables in the 'dish' model, while in the 'ingredient in dish' model the independent variables were the total masses of the ingredients in a one-day menu and masses of ingredients in the dishes. The objective function in both models was minimization of discrepancy between the calculated nutrition intakes and the daily nutrition requirements of NASA for long duration space missions.

Heterocycloalkynes Fused to a Heterocyclic Core: Searching for an Island with Optimal Stability-Reactivity Balance.

In the search for fundamentally new, active, stable, and readily synthetically accessible cycloalkynes as strain-promoted azide-alkyne cycloaddition (SPAAC) reagents for bioorthogonal bioconjugation, we integrated two common approaches: the reagent destabilization by the increase of a ring strain and the transition state stabilization through electronic effects. As a result new SPAAC reagents, heterocyclononynes fused to a heterocyclic core, were created. These compounds can be obtained through a general synthetic route based on four crucial steps: the electrophile-promoted cyclization, Sonogashira coupling, Nicholas reaction, and final deprotection of Co-complexes of cycloalkynes from cobalt.