Cytoprotective Effects and Intranuclear Localization of Sulfur-Containing Derivative of Buckminsterfullerene.

Background: There is a growing interest in exploring the biological characteristics of nanoparticles and exploring their potential applications. However, there is still a lack of research into the potential genotoxicity of fullerene derivatives and their impact on gene expression in human cells. In this study, we investigated the effects of a water-soluble fullerene derivative, C60[C6H4SCH2COOK]5H (F1), on human embryonic lung fibroblasts (HELF).

Buckyballs to fight pandemic: Water-soluble fullerene derivatives with pendant carboxylic groups emerge as a new family of promising SARS-CoV-2 inhibitors.

Herein, we present the first experimental study of individual water-soluble fullerene derivatives proving their ability to inhibit SARS-CoV-2 in vitro. The initial screening allowed us to identify a few new compounds that have demonstrated pronounced antiviral activity with IC values as low as 390 nM and selectivity indexes reaching 214. Time-of-addition analysis and molecular docking results suggested that the viral protease and/or the spike protein are the most probable targets inhibited by the fullerene derivatives.

Determination of Macrolides in Water Using Solid-Phase Extraction and Supercritical Fluid Chromatography-Tandem Mass Spectrometry.

Macrolides are a group of compounds used to treat bacterial infections in humans and animals. Their widespread use results in the contamination of the water environment, which, on the one hand, has a detrimental effect on aquatic organisms and, on the other hand, can lead to the emergence of resistant strains of microorganisms. All of the above determines the need for monitoring of these compounds in the environment, particularly, in water objects.

Analysis of pentacyclic triterpenoids and phytosterols in cloudberry () by LC-MS/MS.

Cloudberry (.) is a plant rich in various biologically active compounds. In this work, the composition and concentrations of pentacyclic triterpenoids (PCTs) and phytosterols in various parts of cloudberries were studied using high-performance liquid chromatography-tandem mass spectrometry by multiple reaction monitoring mode (MRM, targeted analysis) and precursor ion scan mode (non-targeted analysis and semi-quantitative determination).

Chiral Fluorescent Antifungal Azole Probes Detect Resistance, Uptake Dynamics, and Subcellular Distribution in Species.

Azoles are essential for fungal infection treatment, yet the increasing resistance highlights the need for innovative diagnostic tools and strategies to revitalize this class of antifungals. We developed two enantiomers of a fluorescent antifungal azole probe ( and ), analyzing 60 strains via live-cell microscopy. A database of azole distribution images in strains of , , and , among the most important pathogenic species, was established and analyzed.

Analysis of Softwood Lignans by Comprehensive Two-Dimensional Liquid Chromatography.

Lignans constitute a large group of phenolic plant secondary metabolites possessing high bioactivity. Their accurate determination in plant extracts with a complex chemical composition is challenging and requires advanced separation techniques. In the present study, a new approach to the determination of lignans in coniferous knotwood extracts as the promising industrial-scale source of such compounds based on comprehensive two-dimensional liquid chromatography separation and UV spectrophotometric detection is proposed.

Chromatography-like propagation of water along raw material bed in supercritical fluid extraction.

A chromatography-like propagation of water through the material bed was observed while performing supercritical fluid extraction of aroma plants having high moisture content. While parts of raw material bed placed at the inlet of the extraction vessel get dried after appropriate extraction time, the parts closer to the outlet not only stay wet but, in fact, gain more moisture than initial raw material. Presumably, water and other extractables with limited solubility in supercritical CO, get re-adsorbed onto the plant material surface along the extraction column and then desorbed further on.

Year-Round Presence of Microcystins and Toxin-Producing in the Water Column and Ice Cover of a Eutrophic Lake Located in the Continuous Permafrost Zone (Yakutia, Russia).

This study aimed to test the hypothesis of the year-round presence of toxigenic and cyanotoxins in the water and ice of the shallow eutrophic Lake Ytyk-Kyuyol located in the continuous permafrost zone. Three independent approaches-mass-spectrometry, molecular methods and light microscopy-were applied in the study. The cyanobacterial biomass ranged from 1.

Determination of Pentacyclic Triterpenoids in Plant Biomass by Porous Graphitic Carbon Liquid Chromatography-Tandem Mass Spectrometry.

Pentacyclic triterpenoids (PCTs), which possess a number of bioactive properties, are considered one of the most important classes of secondary plant metabolites. Their chromatographic determination in plant biomass is complicated by the need to separate a large number of structurally similar compounds belonging to several classes that differ greatly in polarity (monools, diols, and triterpenic acids). This study proposes a rapid, sensitive, and low-cost method for the simultaneous quantification of ten PCTs (3-taraxerol, lupeol, -amyrin, -amyrin, betulin, erythrodiol, uvaol, betulinic, oleanolic, and ursolic acids) by high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) using porous graphitic carbon (Hypercarb) as a stationary phase capable of hydrophobic retention and specific interactions with analytes.

Clinical classification of torus and effectiveness of two-layer bases in removable dentures.

Aim: To study and systematize the complaints of patients with removable prostheses, paying attention to the clinical manifestation of the torus and its sensitivity, and to determine the effectiveness of the use of two-layer bases in removable prosthetics.

Methods: In the clinic of orthopedic dentistry, 104 people were examined and received orthopedic treatment, including 37 patients in the comparison group. The main number of patients up to 55.

Supercritical Fluid Chromatography-Tandem Mass Spectrometry for Rapid Quantification of Pentacyclic Triterpenoids in Plant Extracts.

Pentacyclic triterpenoids (PCTs) are a widely distributed class of plant secondary metabolites. These compounds have high bioactive properties, primarily antitumor and antioxidant activity. In this study, a method was developed for the quantitative analysis of pentacyclic triterpenoids in plants using supercritical fluid chromatography-tandem mass spectrometry (SFC-MS/MS).

Identification of potential descriptors of water-soluble fullerene derivatives responsible for antitumor effects on lung cancer cells via QSAR analysis.

Water-soluble fullerene derivatives are actively investigated as potential drugs for cancer treatment due to their favorable membranotropic properties. Herein, cytotoxic effects of twenty fullerene derivatives with different solubilizing addends were evaluated in three different types of non-small-cell lung carcinoma (NSCLC). The potential structural descriptors of the solubilizing addends related to the inhibitory activities on each type of lung cancer cell were investigated by the quantitative structure-activity relationship (QSAR) approach.

Change in the Dominant Side of Chewing as a Serious Factor for Adjusting the Prophylaxis Strategy for Implant-Supported Fixed Dental Prosthesis of Bounded Lateral Defects.

Objective:  The main purpose of this article is to study the effect of a change in the dominant side of chewing after prosthetics with fixed structures on implants on the main indicators of osseointegration, adaptation to dentures, and the clinical dental status of patients.

Materials And Methods:  In a clinical trial, an analysis was made of the adaptation of 64 patients to intraosseous implant-supported fixed dentures and 56 apparently healthy volunteers. The examination complex included determination of the functionally dominant side of chewing, gnathodynamometry and electromyography indicators of masticatory muscles, and radiological osseointegration criteria.

Fullerene Derivatives as Lung Cancer Cell Inhibitors: Investigation of Potential Descriptors Using QSAR Approaches.

Background: Nanotechnology-based strategies in the treatment of cancer have potential advantages because of the favorable delivery of nanoparticles into tumors through porous vasculature.

Materials And Methods: In the current study, we synthesized a series of water-soluble fullerene derivatives and observed their anti-tumor effects on human lung carcinoma A549 cell lines. The quantitative structure-activity relationship (QSAR) modeling was employed to investigate the relationship between anticancer effects and descriptors relevant to peculiarities of molecular structures of fullerene derivatives.

[Comparative clinical evaluation of the prosthetic treatment quality of molars restored by chairside manufactured CAD/CAM crowns].

Aim: A comparative clinical evaluation of the results of prosthetic treatment with chairside CAD/CAM crowns for molars made from hybrid ceramics VITA Enamic, blocks of feldspatic ceramics VITABlocs Mark II, blocks of leucite glass IPS Empress CAD.

Material And Methods: The study involved 30 patients aged from 19 to 60 years old with defects in hard tissues of molars. For clinical evaluation we used 'Clinical criteria for evaluation of direct and indirect restorations' developed by FDI in 2007, which included the assessment of several aesthetic, functional and biological parameters.

Novel c.G630A TCIRG1 mutation causes aberrant splicing resulting in an unusually mild form of autosomal recessive osteopetrosis.

Autosomal recessive osteopetrosis (ARO) is a severe genetic bone disease characterized by high bone density due to mutations that affect formation or function of osteoclasts. Mutations in the a3 subunit of the vacuolar-type H -ATPase (encoded by T-cell immune regulator 1 [TCIRG1]) are responsible for ~50% of all ARO cases. We identified a novel TCIRG1 (c.

Antioxidant Properties of Fullerene Derivatives Depend on Their Chemical Structure: A Study of Two Fullerene Derivatives on HELFs.

Oxidative stress is a major issue in a wide number of pathologies (neurodegenerative, cardiovascular, immune diseases, and cancer). Because of this, the search for new antioxidants is an important issue. One of the potential antioxidants that has been enthusiastically discussed in the past twenty years is fullerene and its derivatives.

Genotoxicity of (+)- and (-)-usnic acid in mice.

Usnic acid, which is the most widespread and well-studied secondary lichen compound, has antibacterial and cytotoxic effects. Usnic acid is present in lichens as the (+)- and (-)-enantiomers, which have different biological activities. We used a DNA-comet assay to determine the genotoxic effect of (+)- and (-)-usnic acid in the liver and kidney cells of mice.

Synthesis and Antiviral Activity of Water-Soluble Polycarboxylic Derivatives of [60]Fullerene Loaded with 3,4-Dichlorophenyl Units.

We have synthesized a series of water-soluble polycarboxylic derivatives of [60]fullerene with a gradually changed polarity by combining three to five polar (ionic) malonate addends with two to zero hydrophobic dichlorobenzene units and explored their antiviral activity. It has been shown that decreasing the number of the ionogenic carboxylic groups in the molecules enhanced their antiviral activity against HIV-1 and suppressed their action against HIV-2. The obtained results implied that the charged states and hydrophobicity of the water-soluble polycarboxylic fullerene derivatives affect significantly their biological properties.

Activity-independent targeting of mTOR to lysosomes in primary osteoclasts.

Mammalian target of rapamycin (mTOR) is activated by numerous stimuli, including amino acids and growth factors. This kinase is part of the mTOR complex 1 (mTORC1) which regulates cell proliferation, differentiation, and autophagy. Active mTORC1 is located on lysosomes and has been reported to disassociate from the lysosomal surface in the absence of amino acids.

V-ATPases Containing a3 Subunit Play a Direct Role in Enamel Development in Mice.

Vacuolar H -ATPases (V-ATPases) are ubiquitous multisubunit proton pumps responsible for organellar pH maintenance. Mutations in the a3 subunit of V-ATPases cause autosomal recessive osteopetrosis, a rare disease due to impaired bone resorption. Patients with osteopetrosis also display dental anomalies, such as enamel defects; however, it is not clear whether these enamel abnormalities are a direct consequence of the a3 mutations.

Water-Soluble Fullerene Derivatives as Brain Medicine: Surface Chemistry Determines If They Are Neuroprotective and Antitumor.

Delivering drugs to the central nervous system (CNS) is a major challenge in treating CNS-related diseases. Nanoparticles that can cross blood-brain barrier (BBB) are potential tools. In this study, water-soluble C fullerene derivatives with different types of linkages between the fullerene cage and the solubilizing addend were synthesized (compounds 1-3: C-C bonds, compounds 4-5: C-S bonds, compound 6: C-P bonds, and compounds 7-9: C-N bonds).

Functionalized Fullerene Increases NF-κB Activity and Blocks Genotoxic Effect of Oxidative Stress in Serum-Starving Human Embryo Lung Diploid Fibroblasts.

The influence of a water-soluble [60] fullerene derivative containing five residues of 3-phenylpropionic acid and a chlorine addend appended to the carbon cage (F-828) on serum-starving human embryo lung diploid fibroblasts (HELFs) was studied. Serum deprivation evokes oxidative stress in HELFs. Cultivation of serum-starving HELFs in the presence of 0.

Influence of Lyophilized Amaranthus retroflexus Extract on Radioresistance of Laboratory Mice after Single X-Ray Exposure.

Radioprotective therapeutic effect of lyophilized extract ofAmaranthus retroflexus on the resistance of the albino laboratory male mice exposed to X-ray radiation at a one-time dose of LD(100/30) is studied. It was established that a 30-day use of a lyophilized extract of the vegetative parts of A. retroflexus at a dose of 50 mg/kg after X-ray exposure increases the survival rate of mice by 80%, enhances the recovery in the radiation period of the number of leukocytes, neutrophils, lymphocytes in the peripheral blood of the animals and the normalization of the intensity of peroxide oxidation of lipids in liver cells.

Toxic and DNA damaging effects of a functionalized fullerene in human embryonic lung fibroblasts.

Water-soluble fullerenes have been studied as potential nanovectors and therapeutic agents, but their possible toxicity is of concern. We have studied the effects of F-828, a soluble fullerene [C60] derivative, on diploid human embryonic lung fibroblasts (HELFs) in vitro. F-828 causes complex time-dependent changes in ROS levels.