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Identifying cell response to a chemotherapy drug treatment, in particular at the single cell level, is an important issue in patient management. This study aims at evaluating the effect of gemcitabine on single living cells using micro-Raman imaging. We used as a model the non-small lung cancer cell line, Calu-1, exposed to cytostatic doses (1 nM to 1 μM for 24 h and 48 h) of gemcitabine, an antitumor drug currently used in the treatment of lung cancer. Following drug treatment as a function of doses and incubation times, the Raman maps of single living cells were acquired. Cell biomolecules (DNA, RNA, and proteins) were chemically extracted and their spectral signatures used to evaluate their respective distribution in the cellular spectral information of control and treated cells. The quantification of these distributions reveals a significant effect of 100 nM gemcitabine at 48 h incubation (concomitant decrease of nucleic acids and increase of proteins). PCA analyses performed both on nuclear and extracted biomolecules spectra show a time-dependent effect of the drug. These promising results reveal that effects of subtoxic doses can be monitored at the single cell level highlighting the importance of such studies for clinical applications. [ABSTRACT FROM AUTHOR]

The use of synthetic short interfering RNAs (siRNAs) is currently a method of choice to manipulate gene expression in mammalian cells. Efforts aimed at improving siRNA biological activity, including increased silencing properties, higher substrate specificity and cellular stability, lower cytotoxicity, and improved target delivery, have been made through the introduction of various chemical modifications into the siRNA strands. In these studies, we present the synthesis of oligoribonucleotides with the single replacement of a cytidine unit for 2′,2′-difluoro-2′-deoxycytidine (gemcitabine, dFdC) and the use of them in a series of siRNAs for gene silencing experiments. The dFdC modifications are located in six different positions of the antisense strand, which are crucial for siRNA silencing activity. The results indicate a position-dependent tolerance for the dFdC modification. Gemcitabine units present in the “seed region”, at positions 1 or 8, resulted in only a ∼15% silencing activity in the corresponding duplexes. The dFdC unit at position 10 virtually switched off the silencing activity (below 10%), while the dFdC unit at the positions 2, 4 or 5 produced duplexes of silencing potential comparable to that of the non-modified duplex (70% silencing). The dFdC modification had little impact on the structure of the siRNA duplexes, as determined by circular dichroism analysis, while melting experiments showed their lower thermal stability. [ABSTRACT FROM AUTHOR]

The present study was carried out on Lipopolysaccride from Serratia rubidaea followed by its partial purification, characterization, evaluation of its Cytotoxicity on Lung Cancer Cell Line. LPS was extracted from Serratia rubidaea and detected by the addition of Schiff's reagent. The various subgroups such as 2-KDO, uronic acid and 4-amino arabinose were detected by paper chromatography and the subgroups such as Lipid A and free amino groups were detected by Thin layer chromatography. Partial purification of the extracted LPS was done by SDS-PAGE in which bands were obtained in ladder like patterns. The presence of fatty acids, esters, phosphates in LPS of S.rubidaea were revealed by GC-MS analysis. LPS was found to exhibit cytotoxicity on the lung cancer cell line NCI-H69. [ABSTRACT FROM AUTHOR]

Background Recently, naturally derived facial masks with beneficial biological properties have received increasing interest. In this study, silk sericin-releasing bacterial nanocellulose gel was developed to be applied as a bioactive mask for facial treatment. Results The silk sericin-releasing bacterial nanocellulose gel produced at a pH of 4.5 had an ultrafine and extremely pure fiber network structure. The mechanical properties and moisture absorption ability of the gel were improved, compared to those of the commercially available paper mask. Silk sericin could be control-released from the gel. A peel test with porcine skin showed that the gel was less adhesive than the commercially available paper mask, which would be removed from the face more easily without pain. The in vitro cytotoxicity test showed that the gel was not toxic to L929 mouse fibroblast and HaCaT human keratinocyte cells. Furthermore, when implanted subcutaneously and evaluated according to ISO10993-6 standard, the gel was not irritant to tissue. Conclusion The silk sericin-releasing bacterial nanocellulose gel had appropriate physical and biological properties and safety for the facial treatment application. [ABSTRACT FROM AUTHOR]

The thionamide antithyroid agents were discovered largely through observations carried out by various researchers in the 1940s that found that sulfhydryl-containing substances were goitrogenic in animals. Prof. Edwin B. Astwood started using these drugs to treat hyperthyroidism. In the current paper, we summarize the development background of these agents and the coordination possibility of 2-thiouracil and its derivatives, as well as the biological activities of some of its complexes. Some of them are used as agents for the treatment of tuberculosis, and arthritis, others have bactericidal and fungicidal activity, the third cytotoxic properties, and could be used to treat various types of cancer. [ABSTRACT FROM AUTHOR]

The article discusses research conducted by Dorian McGavern of the Scripps Research Institute and Jiyun Kim of New York University School of Medicine, along with colleagues, on the causes of viral meningitis. While scientists once believed that cytotoxic lymphocytes (CTLs) caused the condition, this study has found that CTLs actually recruit other immune cells that degrade the cells lining the brain.

The process of development is intricate and couple-dependent phenomenon. Accordingly, the study of molecular and cellular biology-based developmental toxicology biomarkers increasingly is becoming an important part of risk assessment and management of chemicals for detection of health outcomes and/or biological endpoint like cytotoxicity, cell death, etc. Since, the evolution of developmental toxicology field a number of tools/markers have been developed or addressed to deal with developmental outcomes, which can ultimately be used for the development of adverse outcome pathways (AOPs) of developmental toxicants. As a result, this paper provides an overview of the current state of developmental toxicology biomarkers and describes the strategies used in the selection and evaluation of such biomarkers in the context of developmental toxicity studies. Here, we discuss about the biological markers that are directly linked to developmental toxicity with respect to future revolutionary perspectives. Additionally, this chapter will address different associated outcomes of developmental exposure by intriguing advance techniques. The discussion focuses on the challenges associated with the development of biomarkers for developmental toxicity and highlights some of the recent advances in this area. Finally, the chapter concludes with a brief discussion of the future prospects for the use of molecular and cellular biology-based developmental toxicity biomarkers. Hope the present state of the art will provide a succinct summary of recent developments of biomarkers of developmental toxicology. [ABSTRACT FROM AUTHOR]

The risks associated to tobacco smoking are not ceased with smoke extinction. Many toxic compounds remain in the environment after the cigarette is extinguished and accumulated in the air or on surfaces. However, little is known about the risks of this exposure. The aim of this study was to evaluate procedures to collect thirdhand smoke (THS) and prepare the samples to perform threein vitrotoxicity tests. Cellulose papers and cotton wipes were used to impregnate with nicotine solution and smoke cigarette in a chamber or in smoker’s home. Samples were immersed in methanol or Dulbecco’s modified Eagle’s medium (DMEM) to expose Hep-2 cells. MTT, neutral red uptake (NRU) and trypan blue assays were performed. The concentration of nicotine in DMEM extract of THS in paper and cotton was similar to those in methanol extract (p > 0.05). Alterations in the mitochondrial and lysosomal functions were found in both paper and cotton samples; however, the cytotoxic effect was not always observed. There was a decrease of 21–31% in MTT assay and 38–56% in NRU assay (p < 0.003). There was a dose-response relationship between the amount of cigarettes and lysosomal viability; the correlation was higher for cotton samples (r = −0.843,p < 0.001). As a dose-response relationship was found only in NRU assay, this test may be a more suitable choice rather than the MTT assay. Paper and wipe sampling can be reliable markers of tobacco smoke contamination. Moreover, these materials, if properly prepared, can be used as substrate providers to perform cellular assays. [ABSTRACT FROM AUTHOR]

After the cigarette is extinguished, many toxic compounds remain in the environment and accumulate in the air or on surfaces. This exposure is termed thirdhand smoke (THS) and its risks are poorly known. The aim of the study was to evaluate the cellular effects of THS from smokers’ homes. Papers were placed in nine smoker’s home and three nonsmoker’s homes. An area equivalent to the paper size was cleaned with a cotton wipe. A549, Hep-2 and 3T3 cells were exposed to THS for 24 h and cellular functions were assessed by MTT, neutral red (NR) reuptake and trypan blue exclusion assays. High levels of nicotine were found in samples from smokers’ homes. Cellular proliferation was similar in almost all samples after THS exposure. Few changes in the cellular functions were observed, mainly higher mitochondrial activity, in paper samples. We are able to detect markers of THS collected from smokers’ homes, but a clear evidence of cellular toxicity cannot be demonstrated by the present assays. This is the first study to evaluate the cellular effects of THS samples collected from smokers’ homes. [ABSTRACT FROM AUTHOR]

Lichen planus is a chronic disease affecting the skin, appendages, and mucous membranes. A cutaneous lichen planus is a rare disease occurring in less than 1% of the general population, while oral illness is up to five times more prevalent; still, both forms equally impair the patient's quality of life. The etiology of lichen planus is not entirely understood. Yet, immune-mediated mechanisms have been recognized since environmental factors such as hepatitis virus infection, mechanical trauma, psychological stress, or microbiome changes can trigger the disease in genetically susceptible individuals. According to current understanding, lichen planus immunopathogenesis is caused by cell-mediated cytotoxicity, particularly cytotoxic T lymphocytes, whose activity is further influenced by Th1 and IL-23/Th-17 axis. However, other immunocytes and inflammatory pathways complement these mechanisms. This paper presents a comprehensive insight into the actual knowledge about lichen planus, with the causal genetic and environmental factors being discussed, the immunopathogenesis described, and the principal effectors of its inflammatory circuits identified. [ABSTRACT FROM AUTHOR]

Polylactic acid (PLA) is a well-known biomaterial on account of its biocompatibility and biodegradability. Zinc oxide (ZnO) nanofillers may endow PLA with advantageous antibacterial and tissue regenerative properties, but may also compromise the biocompatibility of PLA. Several strategies have been developed to improve the biomedical practicality of such composites. The importance of surface properties on amplifying the therapeutic properties and safety of a material enables two potential strategies: (i) surface modification of ZnO nanoparticles, and (ii) surface engineering of the PLA/ZnO composites. Moreover, the controllable biodegradation of PLA allows a third possible strategy: (iii) biodegradation-controlled release of ZnO. The first part of this review introduces the controllable degradation of PLA and the mechanisms of therapeutic properties and cytotoxicity of ZnO. Following this, the paper highlights current research trends regarding the biomedical application of PLA-based ZnO nanocomposites. The final section of this review discusses the potential use of ZnO in tuning the degradation rate of PLA, and the possibility of manipulating the surface properties of ZnO nanoparticles and PLA/ZnO composites in order to optimize the therapeutic properties and safe usage of PLA/ZnO composites in the biomedical field. [ABSTRACT FROM AUTHOR]

Background: Medicinal fern species represent a potentially important source for both food and medicinal applications. Previously, two underutilized tropical fern species (Blechnum orientale and Phymatopteris triloba) were reported with cytotoxic activities against selected cancer cell lines. However, the exact mechanism remains elusive. Objective: In this paper, we reported the identification of six differentially expressed proteins isolated from cancer cells, following exposure to the cytotoxic fern extracts. Materials and Methods: The identities of these cancer proteins were determined by matrix-assisted laser desorption ionization time-of-flight protein sequencing. Results: The cancer proteins were identified as follows: elongation factor 1-γ, glyceraldehydes-3-phosphate dehydrogenase, heat shock protein 90-β, heterogeneous nuclear ribonucleoprotein-A2/B1, truncated nucleolar phosphoprotein B23, and tubulin-β chain. To the best of our knowledge, this paper represents thefirst time these cancer proteins are being reported, following exposure to the aforementioned cytotoxic fern extracts. Conclusion: It is hoped that further efforts in this direction could lead to the identification and development of target-specific chemotherapeutic agents. Abbreviations used: EF: Elongation factor; HRP: Horseradish peroxidase; HSP: Heat shock protein; MALDI: Matrix-assisted laser desorption/ionization. [ABSTRACT FROM AUTHOR]

In this study, the long-term toxic effects of pyrethroids on the earthworm Eisenia fetida were evaluated. Earthworms were exposed to moist filter paper and soil for 14 days to evaluate the survival, exposed to soil for 56 days to assess the reproductive success and for 28 days to identify the cytotoxicity. Results showed that the earthworm survival rate decreased with increasing the concentration of either deltamethrin or fenvalerate in both filter paper test and soil test. No worms survived at 602.15 μg cm −2 of deltamethrin and 0.86 μg cm −2 of fenvalerate in the filter paper test, however 100–125 mg kg −1 of both chemicals resulted in the maximum mortality of 90% in the soil test. The CYP3A4 enzyme activity responded significantly to deltamethrin and fenvalerante in soil at low concentration levels, however, the toxicity response of worms under the long-term exposure conflicted with the degradation of deltamethrin and fenvalerate in soil, indicating the possible formation of more toxic pyrethroid metabolites. This study gave an insight into the toxicological effects profile of pyrethroids for a better risk assessment of pyrethroids deltamethrin and fenvalerante in soil. [ABSTRACT FROM AUTHOR]

This article reviews the use of Kojic Acid (KA) as a skin-lightening ingredient in the cosmetics industry. In 1907, Saito discovered KA, a natural product; it has since become one of the most investigated skin-lightening agents. This paper highlights the findings of the research conducted on this agent. It has been found that KA has certain disadvantages, and researchers have attempted to mitigate these disadvantages by designing new equivalents of KA that are more efficient in tyrosinase inhibition. These equivalents are also safe to use and have improved properties and solubility. The Cosmeceutical Ingredient Review (CIR) indicates that this ingredient can be safely used at a concentration not higher than 1% due to its cytotoxicity. Other scientific data also support its safety at a concentration of 2% or less. It was shown to be helpful in the treatment of hyper pigmentary disorders, such as freckles, age spots, post-inflammatory hyperpigmentation, and melasma, which has been proven clinically. [ABSTRACT FROM AUTHOR]

Tissue stromal cells interact with leukaemia cells and profoundly affect their viability and drug sensitivity. Here we show a biochemical mechanism by which bone marrow stromal cells modulate the redox status of chronic lymphocytic leukaemia (CLL) cells and promote cellular survival and drug resistance. Primary CLL cells from patients exhibit a limited ability to transport cystine for glutathione (GSH) synthesis owing to a low expression level of Xc-transporter. In contrast, bone marrow stromal cells effectively import cystine and convert it to cysteine, which is then released into the microenvironment for uptake by CLL cells to promote GSH synthesis. The elevated level of GSH enhances leukaemia cell survival and protects them from drug-induced cytotoxicity. Furthermore, disabling this protective mechanism significantly sensitizes CLL cells to drug treatment in the stromal environment. This stromal-leukaemia interaction is critical for CLL cell survival and represents a key biochemical pathway for effectively targeting leukaemia cells to overcome drug resistance in vivo. [ABSTRACT FROM AUTHOR]

Drug reaction with eosinophilia and systemic symptoms (DRESS) is an infrequent, but severe, adverse drug-induced reaction which occurs due to massive T-cell stimulation resulting in cytotoxicity and eosinophil activation and recruitment. The incidence is 0.4 cases per 100, 0000 in the general population; the mortality rate is up to 10%. Therefore, we believe that recognizing this syndrome is of particular importance. The problem we notice is that DRESS is often seen and described in patients receiving rheumatologic or anticonvulsant drugs, but very rarely in psychiatric hospitals, where Clozapine is frequently used, and that is the importance of this paper. DRESS Syndrome must be recognized promptly, and causative drugs withdrawn. Indeed, it has been reported that the earlier the drug withdrawal, the better the prognosis. In this paper, we present three cases of Clozapine-induced DRESS. All cases were recorded in the Multicenter Drug Safety Surveillance Project (AMSP). [ABSTRACT FROM AUTHOR]

Active control over the cell gradient is essential for understanding biological systems and the reconstitution of the functionality of many types of tissues, particularly for organ-on-a-chip. Here, we propose a three-dimensional (3D) microfluidic strategy for generating controllable cell gradients. In this approach, a homogeneous cell suspension is loaded into a 3D stair-shaped PDMS microchannel to generate a cell gradient within 10 min by sedimentation. We demonstrate that cell gradients of various profiles (exponential and piecewise linear) can be achieved by precisely controlling the height of each layer during the fabrication. With sequential seeding, we further demonstrate the generation of two overlapping cell gradients on the same glass substrate with pre-defined designs. The cell gradient-based QD cytotoxicity assay also demonstrated that cell behaviors and resistances were regulated by the changes in cell density. These results reveal that the proposed 3D microfluidic strategy provides a simple and versatile means for establishing controllable gradients in cell density, opening up a new avenue for reconstructing functional tissues. [ABSTRACT FROM AUTHOR]

Background: Idiopathic pulmonary fibrosis (IPF) is a rare form of immune-mediated interstitial lung disease characterized by progressive pulmonary fibrosis and scarring. The pathogenesis of IPF is still unclear. Gene fusion events exist universally during transcription and show alternated patterns in a variety of lung diseases. Therefore, the comprehension of the function of gene fusion in IPF might shed light on IPF pathogenesis research and facilitate treatment development. Methods: In this study, we included 91 transcriptome datasets from the National Center for Biotechnology Information (NCBI), including 52 IPF patients and 39 healthy controls. We detected fusion events in these datasets and probed gene fusion-associated differential gene expression and functional pathways. To obtain robust results, we corrected the batch bias across different projects. Results: We identified 1550 gene fusion events in all transcriptomes and studied the possible impacts of IL7 = AC083837.1 gene fusion. The two genes locate adjacently in chromosome 8 and share the same promoters. Their fusion is associated with differential expression of 282 genes enriched in six Kyoto Encyclopedia of Genes and Genomes (KEGG) pathways and 35 functional gene sets. Gene ontology (GO) enrichment analysis shows that IL7 = AC083837.1 gene fusion is associated with the enrichment of 187 gene sets. The co-expression network of interleukin-7 (IL7) indicates that decreased IL7 expression is associated with many pathways that regulate IPF progress. Conclusion: Based on the results, we conclude that IL7 = AC083837.1 gene fusion might exacerbate fibrosis in IPF via enhancing activities of natural killer cell-mediated cytotoxicity, skin cell apoptosis, and vessel angiogenesis, the interaction of which contributes to the development of fibrosis and the deterioration of respiratory function of IPF patients. Our work unveils the possible roles of gene fusion in regulating IPF and demonstrates that gene fusion investigation is a valid approach in probing immunologic mechanisms and searching potential therapeutic targets for treating IPF. The reviews of this paper are available via the supplemental material section. [ABSTRACT FROM AUTHOR]

To improve pathogenetic studies in cancer development and reliable preclinical testing of anti-cancer treatments, three-dimensional (3D) cultures, including spheroids, have been widely recognized as more physiologically relevant in vitro models of in vivo tumor behavior. Currently, the generation of uniformly sized spheroids is still challenging: different 3D cell culture methods produce heterogeneous populations in dimensions and morphology, that may strongly influence readouts reliability correlated to tumor growth rate or antitumor natural killer (NK) cell-mediated cytotoxicity. In this context, an increasing consensus claims the integration of microfluidic technologies within 3D cell culture, as the physical characterization of tumor spheroids is unavoidably demanded to standardize protocols and assays for in vitro testing. In this paper, we employed a flow-based method specifically conceived to measure weight, size and focused onto mass density values of tumor spheroids. These measurements are combined with confocal and digital imaging of such samples. We tested the spheroids of four colorectal cancer (CRC) cell lines that exhibit statistically relevant differences in their physical characteristics, even though starting from the same cell seeding density. These variations are seemingly cell line-dependent and associated with the number of growing cells and the degree of spheroid compaction as well, supported by different adenosine-triphosphate contents. We also showed that this technology can estimate the NK cell killing efficacy by measuring the weight loss and diameter shrinkage of tumor spheroids, alongside with the commonly used cell viability in vitro test. As the activity of NK cells relies on their infiltration rate, the in vitro sensitivity of CRC spheroids proved to be exposure time- and cell line-dependent with direct correlation to the cell viability reduction. All these functional aspects can be measured by the system and are documented by digital image analysis. In conclusion, this flow-based method potentially paves the way towards standardization of 3D cell cultures and its early adoption in cancer research to test antitumor immune response and set up new immunotherapy strategies. [ABSTRACT FROM AUTHOR]

Objectives: This systematic review aimed to compare the cytotoxicity of root canal filling materials (RCFMs) assessed using tetrazolium salt‐based tests (TSBT), including the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl tetrazolium bromide (MTT) assay, with those obtained using other cell viability assays. Methods: A search was performed on PubMed, Scopus, Web of Science and OpenGrey up to March 2019, followed by a manual search. According to the Participants, Exposure, Comparator and Outcomes (PECO) criteria, in vitro studies that evaluated the cytotoxic effect of RCFMss on animal and/or human cells through TSBT and at least one other viability assay were compared. The methodological quality of selected papers was assessed using ToxRTool® and SciRAP®. Data were analysed using Wilcoxon's signed‐rank test for paired samples and linear weighting kappa. Results: A total of 230 non‐duplicated records were identified. After applying the eligibility criteria, 55 studies were selected for methodological evaluation, seven were selected by manual searching, 22 were excluded for methodological reasons, and 40 were included. A total of 410 comparisons were performed between TSBT and distinct cell viability tests (DCVT). MTT had moderate concordance with DCVT using human cells (n = 138 samples) (P = 0.507; k = 0.4225) and animal cells (n = 122 samples) (P = 0.124; k = 0.5775). XTT had good concordance using human (n = 110 samples) (P = 0.507; k = 0.6336) and animal cells (n = 12 samples) (P = 0.564; k = 0.6604). MTT, XTT, WST and MTS assays showed moderate concordance with DCVT (n = 410 samples) (P = 0.375; k = 0.5138) and complete agreement in 226 samples. Discussion: The included studies had methodological heterogeneity that was minimized by the systematic review methodology. Conclusions: MTT and XTT do not cause over‐ or underestimation of cell viability during cytotoxicity screening of root canal filling materials, implying that these assays can be considered reliable for this purpose. Nonetheless, the development of protocols for the cytotoxic screening of these materials on 3D tissue‐like cultures aiming to improve their predictability in the clinical scenario is suggested. [ABSTRACT FROM AUTHOR]

In recent years, the presence of food-borne nanoparticles during food processing has been a controversial issue. In this paper, we introduced a class of extremely low-cytotoxicity carbon dots (CDs) extracted from grilled pike eel which have been consumed for thousands of years. These CDs are water-soluble, quasi-spherical, and nanosized (approximately 2.75 nm). UV illumination can excite CDs to emit a strong sapphire luminescence with a quantum yield as high as 68.7%. X-ray diffraction (XRD) analysis showed that these nanoparticles are amorphous attributed to the disordered carbon atoms. X-ray photoelectron spectroscopy (XPS) measurements showed that the CDs contain a predominant C1s peak at 284.43 eV and an O1s peak at 531.35 eV accompanied by a pronounced N1s peak at 399.34 eV, with the atomic percentages of 66.58%, 17.5% and 15.91%, respectively. Moreover, the CDs also have excellent biocompatibility and could ease into the cytoplasmic region of MC3T3-E1 cells without any seriously imposed toxicity against cells. [ABSTRACT FROM AUTHOR]

Background: Many smokers have recently turned to electronic cigarettes (e-cigarettes) because they have been marketed as a cheaper, safer smokeless alternative to traditional cigarettes and a possible smoking cessation tool. Although the safety of these electronic devices is still not fully known, there is evidence of their cytotoxicity on cells belonging to the oral cavity. In a previous study by the authors, the increase of reactive oxygen production and Bax expression, followed by the occurrence of apoptosis, was demonstrated in human gingival fibroblasts (HGFs). The aim of this paper is to further investigate the effects of the e-cigarette liquids (with and without nicotine) on the same experimental model.Methods: HGFs were treated with e-cigarette fluids containing nicotine (final concentration 1 mg/mL) and the equivalent volume of a fluid without nicotine, for periods ≤48 hours. Lactate dehydrogenase assay (LDH), electronic microscopy analysis, collagen I production, flow cytometry lysosome compartment evaluation, and western blotting light chain 3 (microtubule-associated protein 1A/1B-LC3) expression were performed.Results: Fluids containing nicotine exerted cytotoxicity as demonstrated by increased levels of LDH, in parallel to the presence of numerous vacuoles in the cytoplasm, a decrease in collagen I production, and augmented LC3 II expression. Autophagic vesicles and more procollagen I molecules were present in the cytoplasm of fibroblasts exposed to nicotine-free fluids. In the same samples, time-dependent activation of the lysosomal compartment with no changes in LC3 expression was detected.Conclusion: E-cigarette fluids (with and without nicotine) trigger molecular and morphologic responses in oral fibroblasts, raising concerns about their role in the pathogenesis of oral diseases. [ABSTRACT FROM AUTHOR]

In recent years, the concept of nanoparticles being used as an intelligent drug carrier has gained great attention. In this paper, the formulation of a liposome delivery system loaded with a novel benzothiazole-containing cisplatin derivative (CJM-Pt) was carried out. The particle size distributions were determined using dynamic light scattering, and the prepared liposomes showed a suitable size of around 98 nm. Stability studies showed that the CJM-Pt loaded liposomes were stable at 4 °C for more than four weeks. Investigation of triggered release indicated that the release performance of the prepared liposomes was controllable and the releasing effect was remarkable under low pH (＜pH 6.8) and high temperature (＞42 °C). To test the suitability of the chosen formulation, CJM-Pt loaded liposomes were investigated against several tumor cell lines: MGC-803, SGC-7901, MCF-7 and MDA-MB-231. Furthermore, the cell cycle arrest was examined. The CJM-Pt loaded liposomes have the potential to be applied in drug delivery systems (DDS) for breast cancer therapy. [ABSTRACT FROM AUTHOR]

Antibody-drug conjugates (ADCs) reflect a new promising approach in prostate cancer, even more so after the practicechanging results in other malignancies, either hematologic or solid. ADCs consist of monoclonal antibodies (mAb) targeted at specific antigens overly expressed on cancer cells compared to normal cells. A cytotoxic payload is attached to the mAb using a stable linker. In prostate cancer, PSMA, STEAP1, TROP2, CD46 and B7-H3 are antigens currently being studied as targets for ADCs. In this paper, we discuss the composition of ADCs and focus on their application and challenges as treatment options in prostate cancer. [ABSTRACT FROM AUTHOR]

Polymer hydrogels are three-dimensional networks formed of highly hydrophilic monomers cross-linked by hydrogen bonding, electrostatic attraction or covalent crosslinking. They may be formed of one (homo-) or multiple monomers (copolymer hydrogels). The specificity of hydrogels stems from their ability to bind large amounts of surrounding fluid, water, or biological fluids, due to their physical and / or chemical crosslinking, while remaining insoluble. Poly(1-vinyl-2-pyrrolidone) is a polar, hydrophilic, amphoteric polymer obtained from the monomer of 1-vinyl-2-pyrrolidone. The choice of synthesis conditions resulted in a large number of products of different molar masses (from several thousand to several million g/mol). It is used in many industries (in the production of adhesives, paper and detergents), especially because of its good solubility in water and in a large number of organic solvents. Poly(1-vinyl-2-pyrrolidone) are the widely used biocompatible homo polymer hydrogel carriers in drug delivery due to its water solubility and extremely low cytotoxicity. It is biocompatible and therefore safe for use in biological experiments. The aim of this work is to synthesize hydrogel based on 1-vinyl-2- pyrrolidone monomer using ethylene glycol dimethacrylate (1, 2 and 3 mol%) as crosslinker and 2,2'-azobis(2- methylpropionitrile) initiator by radical polymerization method with thermal initiation. Structural characterization of the obtained poly(1-vinyl-2-pyrrolidone) hydrogels was performed using Fourier transformation infrared spectroscopy (FTIR) methods. The synthesized hydrogels were purified from unreacted monomers, crosslinkers and initiators after extraction in methanol. The content of the residual reactants from the methanol extracts was examined using high pressure liquid chromatography (HPLC). Decanted methanolic extracts of synthesized poly(1- vinyl-2-pyrrolidone) hydrogels after 48h of residual reactant extraction were used for analysis. The extracts were filtered through a 0.45 μm cellulose membrane filter and used for HPLC analysis. After rinsing, hydrogels were dried to the constant mass in a drying oven at 40°C. In the FTIR spectra of poly(1-vinyl-2-pyrrolidone), there are no bands of valence vibrations of vinyl group 1-vinyl-2-pyrrolidone or ethylene glycol dimethacrylate, nor bands of valence C = C vibrations and deformation vibrations in the plane and out of plane of the vinyl group of monomers and crosslinkers. indicating the polymerization performed by breaking the double bonds. Residual reactant values are within acceptable limits (1.132 - 2.020% for 1-vinyl-2-pyrrolidone, 0.338 - 0.963% for ethylene glycol dimethacrylate, according to the initial amount in the reaction mixture), and also indicate a satisfactory product yield. [ABSTRACT FROM AUTHOR]

NK cell-mediated immunotherapy has received increasing attention in the past decade due to its efficacy and bio-safety. The composition and content of lipids in individual cells are closely related to NK cell-mediated cytotoxicity, especially polyunsaturated fatty acids (PUFA) which are oxidized during NK cell-mediated apoptosis. Here we investigated the changes of lipids in single HepG2 cells by label-free mass cytometry and obtained information on 53 lipids and 13 oxidized lipids after the interaction with NK92 MI cells. We found that the contents of lipids and oxidized lipids of HepG2 cells changed obviously during the NK cell-mediated apoptosis. The HepG2 cells could be classified into two phenotypes after co-culturing with NK92 MI cells based on the ratio of PC(38:6-2OH)/PC(38:6) in individual cells, which may serve as a feature to evaluate NK cell-mediated cytotoxicity. The present work used the lipids and oxidized lipids of individual cells to reveal the heterogeneity in NK cell-mediated apoptosis which would be a powerful method for evaluating the cytotoxicity of NK cells at the single-cell level. [ABSTRACT FROM AUTHOR]

In this paper we present a first insight into the cytotoxic action mode of copper(i) iodide or copper(i) thiocyanate complexes with a phosphine derivative of sparfloxacin (a 3rd generation fluoroquinolone antibiotic agent) and 2,9-dimethyl-1,10-phenanthroline or 2,2′-biquinoline as auxiliary ligands. The in vitro cytotoxic activity of the new complexes was tested against two cancer cell lines (CT26 – mouse colon carcinoma and A549 – human lung adenocarcinoma). An ICP-MS study revealed a marked time-dependent intracellular copper accumulation of the tested compounds. In addition, confocal microscopy imaging showed accumulation of the complexes inside whole cells and their emission of blue light. The complexes generate reactive oxygen species in the cancer cells, which was examined by using two different fluorescent probes. Moreover, (i) DNA intercalation studied by luminescence spectroscopy, circular dichroism and molecular docking, and (ii) plasmid DNA damage also demonstrate their significant cytotoxicity. All these observed biological effects contribute to the induction of apoptosis, observed at a great predominance. [ABSTRACT FROM AUTHOR]

Cytotoxicity and drug susceptibility tests are very similar tests, but they measure different parameters in cells. In cytotoxicity tests, compounds are measured against cells, usually eukaryote cells, for their toxicity, whereas, drug susceptibility tests measure the extent at which a compound can kill or inhibit the growth of organisms (usually prokaryote cells). However, the problem is that compounds contain many different type of chemical substances, and the mechanisms that are activated for cells to undergo arrest, differ between cell kinds and chemical compounds used when performing the mentioned tests. Furthermore, as to whether the result outcomes of cytotoxicity and drug susceptibility tests are trustworthy enough, could be a factor for consideration. In addition, cytotoxicity and drug susceptibility tests can only be considered to be successful if the chemical substance/s (i.e. compounds) under investigation triggers a cascade of cellular events, which are catalysed by enzymes. In eukaryote and bacterial cells, cytotoxicity and drug susceptibility test outcomes rely on nuclear events in order for the toxicity of the tested compound to be successfully determined after screening is completed. In this article, the conclusivity of cytotoxicity and drug susceptibility tests would form the focus of discussion, but emphasise on all the factors that affect the conclusivity of these tests would not form the basis of this paper. [ABSTRACT FROM AUTHOR]

Audiovestibular dysfunction in patients with systemic lupus erythematosus has been underestimated for decades. Systemic lupus erythematosus can affect both the auditory and vestibular systems simultaneously. Several potential pathophysiological mechanisms behind systemic lupus erythematosus-related audiovestibular dysfunction have been proposed, including antibody-mediated immune responses, cell-mediated cytotoxicity, immune complex deposition in microvessels, central involvement in the audiovestibular pathway, and ototoxicity from medications used in systemic lupus erythematosus treatment. Currently available tests to evaluate audiovestibular function in systemic lupus erythematosus patients are neither specific nor sensitive. Nevertheless, there is no consensus regarding the efficacy of treatments for audiovestibular dysfunction in such patients. In this systematic review, we electronically searched the PubMed, Embase, ClinicalKey, Web of Science, and ScienceDirect platforms to find eligible articles. The first inspection date was on 29 December 2023 and the final update search date was on 11 June 2024. Further, we rated the quality of the included articles with Newcastle–Ottawa Scale. Based upon the aforementioned systematic review process, we have summarized the currently available evidence on the characteristics, pathophysiology, examination, and treatment of audiovestibular dysfunction related to systemic lupus erythematosus. Furthermore, we have proposed a specific steroid treatment protocol to manage audiovestibular dysfunction related to systemic lupus erythematosus. Audiovestibular dysfunction related to systemic lupus erythematosus may be responsive to adequate treatments, potentially allowing for reversibility if the disease is recognized and managed in a timely manner. Therefore, to provide clinically relevant evidence to clinicians, we have organized this literature review article to summarize the available evidence on the characteristics, pathophysiology, examination, and treatment of audiovestibular dysfunction in patients with systemic lupus erythematosus. Finally, based on our modified steroid treatment protocol, we would like to provide a new treatment strategy to clinicians to manage systemic lupus erythematosus-related audiovestibular dysfunction. [ABSTRACT FROM AUTHOR]

Determining the safety of a newly developed experimental product is a crucial condition for its medical use, especially for clinical trials. In this regard, four hydrogel-type formulations were manufactured, all of which were based on carbomer (Blank-CP940) and encapsulated with caffeine (CAF-CP940), phosphorus derivatives (phenyl phosphinic (CAF-S1-CP940) and 2-carboxyethyl phenyl phosphinic acids (CAF-S2-CP940)). The main aim of this research was to provide a comprehensive outline of the biosafety profile of the above-mentioned hydrogels. The complex in vitro screening (cell viability, cytotoxicity, morphological changes in response to exposure, and changes in nuclei morphology) on two types of healthy skin cell lines (HaCaT—human keratinocytes and JB6 Cl 41-5a—murine epidermal cells) exhibited a good biosafety profile when both cell lines were treated for 24 h with 150 μg/mL of each hydrogel. A comprehensive analysis of the hydrogel's impact on the genetic profile of HaCaT cells sustains the in vitro experiments. The biosafety profile was completed with the in vivo and in ovo assays. The outcome revealed that the developed hydrogels exerted good biocompatibility after topical application on BALB/c nude mice's skin. It also revealed a lack of toxicity after exposure to the hen's chicken embryo. Further investigations are needed, regarding the in vitro and in vivo therapeutic efficacy and safety for long-term use and potential clinical translatability. [ABSTRACT FROM AUTHOR]

Abstract Although in vitro assay is an ideal alternative method for the in vivo toxicity prediction, different in vivo-in vitro correlations have been observed for the toxicity endpoints obtained from different levels of species. In this paper, theoretical in vivo-in vitro toxicity correlations have been developed for cytotoxicity versus human, mammalian and fish toxicity, respectively. These theoretical models were then used to investigate the correlations and the influencing factors between in vivo and in vitro toxicity. Bio-uptake equilibrium theory can well explain why there is a significant correlation between fish and cell toxicity (R2 = 0.70); why human toxicity is very close to fish toxicity; and why hydrophobic compounds exhibit relatively greater toxicity than reactive or specifically-acting compounds to human and fish as compared to cells. The kinetic theory can well explain why there is a very poor relationship between mammal and cell toxicity (R2 = 0.44). This paper reveals that polar and ionized compounds can more easily pass through cell membrane and have greater bioconcentration potential. Increasing of hydrophobicity and ionization can increase the cytotoxicity. Inclusion of descriptors representing hydrophobicity, ionization, acidity and absorption into the correlation equations can significantly improve the correlations of cytotoxicity with human and fish toxicity (R2 > 0.8), but not with mammal toxicity (R2 = 0.49). These descriptors reflect the differences of the toxicodynamics and toxicokinetics between cells and organisms. Graphical abstract Image 1 Highlights • Theoretical correlation equations are developed between in vivo and in vitro toxicity. • Human-cell and fish-cell toxicity correlations are dominated by equilibrium process. • Mammal-cell toxicity correlation is dominated by kinetic process. • Human and fish toxicity can well be predicted from cytotoxicity, not mammal toxicity. • Hydrophobicity, acidity and absorption can influence in vivo-in vitro correlations. [ABSTRACT FROM AUTHOR]

Vibrational spectroscopy, including Raman micro spectroscopy, has been widely used over the last few years to explore potential biomedical applications. Indeed, Raman micro spectroscopy has been demonstrated to be a powerful non-invasive tool in cancer diagnosis and monitoring. In confocal microscopic mode, the technique is also a molecularly specific analytical tool with optical resolution which has potential applications in subcellular analysis of biochemical processes, and therefore as an in vitro screening tool of the efficacy and mode of action of, for example, chemotherapeutic agents. In order to demonstrate and explore the potential in this field, established, model chemotherapeutic agents can be valuable. In this study paper, Raman micro spectroscopy coupled with confocal microscopy were used for the localization and tracking of the commercially available drug, doxorubicin (DOX), in the intracellular environment of the lung cancer cell line, A549. Cytotoxicity assays were employed to establish clinically relevant drug doses for 24 h exposure, and Confocal Laser Scanning Fluorescence Microscopy was conducted in parallel with Raman micro spectroscopy profiling to confirm the drug internalisation and localisation. Multivariate statistical analysis, consisting of PCA (principal components analysis) was used to highlight doxorubicin interaction with cancer cells and spectral variations due to its effects before and after DOX spectral features subtraction from nuclear and nucleolar spectra, were compared to non-exposed control spectra. Results show that Raman micro spectroscopy is not only able to detect doxorubicin inside cells and profile its specific subcellular localisation, but, it is also capable of elucidating the local biomolecular changes elicited by the drug, differentiating the responses in different sub cellular regions. Further analysis clearly demonstrates the early apoptotic effect in the nuclear regions and the initial responses of cells to this death process, demonstrating the potential of the technique to monitor the mechanisms of action and response on a molecular level, with subcellular resolution. [ABSTRACT FROM AUTHOR]

Nonylphenol polyethoxylates (NPEOs) are a major group of nonionic surfactants widely used in various detergents, cleaners, plastics, papers, and agro-chemical products. Nonylphenol (NP), which is a final degraded metabolite derived from NPEOs, has been reported as an endocrine disrupter, known to mimic or disturb reproductive hormone functions. Concern about the hazards of NP and NPEOs has generated legal restrictions and action plans worldwide. Considering the fact that NP and NPEOs are majorly used in the production of products such as detergents, shampoos, and cosmetics which frequently come into contact with the skin, we investigated the effects of NP and NPEOs on a human keratinocyte cell line (HaCaT). In this study, the toxicity of NP and NPEOs was screened in HaCaT cells using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide thiazolyl blue assay and Western blotting. The potential cytotoxicity of substitutes was assessed by dose-response assays, relative cell viability, and genotoxicity caused by specific alterations in DNA damage response proteins (including ataxia-telangiectasia mutated, p53, Chk1, Chk2, and Histone H2A.X). We demonstrated that NP and NPEOs are toxic to HaCaT cells, as revealed by the decreased cell viability after 24 h treatment. NPs and NPEOs also induced apoptosis and DNA damage as shown by the activation of Poly(ADP-ribose) polymerase, Caspase-3, and Histone H2A.X. [ABSTRACT FROM AUTHOR]

Photodynamic treatment is often thought to produce reactive oxygen species (ROS) that directly induce killing; the nomenclature and phrases revolve around such notions of light‐dependency. Few studies reference the possible existence of oxidation products formed in secondary reactions, which bear cytotoxicity competitive to their ROS precursors. Here, we highlight the paper by Girotti and Korytowski in this issue of Photochemistry and Photobiology, which does just that. In this paper, they report on cholesterol hydroperoxides, which are formed after photosensitized oxidation and yield cytotoxic mixtures in dark reactions after the light's turned off. Some of the hydroperoxides are transported by protein carriers and damage tissue outside their site of origin. A similar dark cytotoxicity may be anticipated for biological peroxides from in vivo photodynamic therapy. Deciphering downstream reactions following photodynamic treatment can be problematic. The reactions may be viewed as like a one two punch, that is, light‐dependent/light‐independent processes that occur one after another. Deducing such initial light and subsequent dark processes can account for deeper understanding of and improve our control of photodynamic effects. [ABSTRACT FROM AUTHOR]

In this paper we report the synthesis and full characterisation of a range of Ti(IV)-catecholato systems complexed to piperazine or homopiperazine salan ligands. The steric/electronic environment of the catecholate moiety has been varied and the effect this has on cytotoxicity discussed. It was observed that the 7-membered homopiperazine complexes are more stable to hydrolysis than their piperazine cousins in biological media. In general the homopiperazine complexes show higher cytotoxicity than the piperazine complexes, with the most cytotoxic complex exhibiting IC50 (μM) values of 3 ± 0.5 μM (HT-29) and 4 ± 1 μM (OVCAR). [ABSTRACT FROM AUTHOR]

In this paper we propose and analyze a pathogen dynamics model with antibody and Cytotoxic T Lymphocyte (CTL) immune responses. We incorporate latently infected cells and three distributed time delays into the model. We show that the solutions of the proposed model are nonnegative and ultimately bounded. We derive four threshold parameters which fully determine the existence and stability of the five steady states of the model. Using Lyapunov functionals, we established the global stability of the steady states of the model. The theoretical results are confirmed by numerical simulations. [ABSTRACT FROM AUTHOR]

Abstract: E‐cigarettes are used by millions of people despite the fact that the harmful effect of aerosol emitted from these products to the human organism is still not clear. In this paper, toxicity of vapor generated using different solutions and battery output voltage on A549 cells viability is presented. The obtained EC50 values for commercially available propylene glycol/glycerol solution 1:1 e‐liquids based on 3.2 V (0.127%), 4.0 V (0.112%) and 4.8 V (0.038%) were about 1.5–4.5 times higher than in tobacco smoke (0.0086%). Furthermore, it was shown that the increase of battery output voltage decreased A549 cell viability. In addition, commercially available extracts were more cytotoxic than laboratory made extracts. Owing to the expansiveness of e‐cigarettes, it is very important to estimate their impact on public health. Our results not only confirm less cytotoxicity of e‐liquid aerosol than cigarette smoke, but also demonstrate that solutions used in e‐liquids and, for the first time, battery output voltage have a significant impact on cytotoxicity of e‐cigarette vapor. Thus, the results of this study are very important for the current and future legal regulations on e‐cigarettes. [ABSTRACT FROM AUTHOR]

Objective: The genus Ferula L. includes perennial flowering plants belonging to the Apiaceae family. This genus is a rich source of biologically active phytochemicals such as sulfur-containing derivatives, coumarins, sesquiterpenes, sesquiterpene lactones, sesquiterpene coumarins, glucuronic acid, galactose, arabinose, rhamnose, and daucane esters. Over the last decade, considerable attention has been paid to biological activities of these compounds; it is assumed that the most prominent biological features of the genus Ferula are their cytotoxic effects. This article discusses cytotoxic activity of the genus Ferula and their important compounds. Materials and Methods: In this mini-review article, papers published from 1990 to April 2016 were included and the following information was discussed; cytotoxic activity of the genus Ferula and their important compounds, the type of cell line used in vitro, concentrations of the extracts/active compound that were used, and the underlying mechanisms of action through which Ferula-related chemicals induced cytotoxicity. In addition, we explained different mechanisms of action through which the active constituents isolated from Ferula, could decrease cellular growth. Conclusion: It is highly recommended that potent and effective compounds that were isolated from Ferula plants and found to be appropriate as adjuvant therapy for certain diseases, should be identified. Also, the versatile biological activities of sesquiterpene coumarins suggest them as promising agents with a broad range of biological applications to be used in the future. [ABSTRACT FROM AUTHOR]

To explore the potential biomedical applications of nanogels, it is a key factor to improve their thermosensitivity. In this paper, triple-responsive nanogels poly(N-isopropylacrylamide–N,N′-dimethylaminoethyl methacrylate–acrylic acid) (PNDA) were synthesizedvia in situincorporating both cationic components and anionic components into a normal thermosensitive polymer matrix. The triple-monomer constructed PNDA nanogels displayed an enhanced thermosensitivity as compared with dual-monomer constructed PND nanogels. The PNDA nanogels presented higher encapsulation efficiency (∼89%) and exhibited better pH/redox/thermo-responsivenesses in an anticancer drug delivery.In vitrobiological study indicated that the PNDA nanogels have excellent biocompatibility and improved anticancer cytotoxicity to A549 cells after loading drug DOX. [ABSTRACT FROM AUTHOR]

This paper reports an evaluation of the structure, the flexural and viscoelastic properties, and the cytotoxicity of scaffolds produced from PLDLA and bioglass (BG) by selective laser sintering. The process conditions used in the scaffold preparation resulted in microstructures with a high sintering degree. The range of porosity values obtained for the scaffolds was 26–30%, which is appropriate for scaffold applications, and the average pore size in the PLDLA/BG scaffolds was 200 μm. The flexural modulus, ultimate strength, and elongation values for the PLDLA/BG scaffold specimens decreased for scaffolds with 20 and 30% of BG, probably due to the low chemical affinity between the polymeric and the ceramic phase. The PLDLA/BG scaffolds exhibited flexural modulus values between 10 and 79 MPa, depending on the scaffold composition, which lie within the range reported for human bone. In the direct cytotoxicity tests, cells seeded on PLDLA/BG scaffolds showed a high viability, indicating that the PLDLA/BG scaffolds prepared by selective laser sintering can be applied in bone repair. [ABSTRACT FROM AUTHOR]

This paper reports our original technique for visualizing cell-attached nanointerfaces with extremely high axial resolution using homogeneously excited localized surface plasmon resonance (LSPR) on self-assembled silver nanoparticle sheets. The LSPR sheet can confine and enhance the fluorescence at the nanointerface, which provides high signal-to-noise ratio images of focal adhesion at the cell-attached interface. The advantage of this LSPR-assisted technique is its usability, which provides comparable or higher-quality nanointerfacial images than TIRF microscopy, even under epifluorescence microscopy. We also report the cytotoxicity of silver nanoparticles, as determined via morphological analysis of adherent cells on the sheet. [ABSTRACT FROM AUTHOR]

Prebiotics are known as the 'food' for beneficial gut microbiota that are capable of promoting host health. Their effects depend on the product of gut fermentation or metabolites. This paper discusses the role of prebiotics on cytotoxicity, genotoxicity, and cell integrity. Metabolites produced from the fermentation of prebiotics can be used to understand gut diseases such as colorectal cancer. Fecal water from in vivo or in vitro studies can be used to understand the relationship between prebiotics and gut diseases because of its close contact with colon epithelium. Besides, fecal water has compounds that are capable of modifying colonocytes. [ABSTRACT FROM AUTHOR]

Lead (Pb) is one of the most important heavy metals that possess many applications in different kinds of industrial procedures and consumer products. The adverse effects of Pb on different parts of the immune system have been reported in various studies. Although it has been shown that high concentrations of Pb have low cytotoxicity on human lymphocytes, the effects of non-cytotoxic concentrations of Pb (detected in human blood) on cellular organelles and oxidative stress factors of human lymphocytes have yet to be determined. In this study, human lymphocytes were obtained from the blood of healthy male volunteers through the use of the Ficoll standard method. The intention of this paper was to determine the effects of non-cytotoxic concentrations of Pb on human lymphocytes using the accelerated cytotoxicity mechanism screening technique. For determination of cell viability, lymphocytes were treated with 0-1 mm Pb for 12 h. Subsequently, we assayed the effects of non-cytotoxic concentrations of Pb which are detected in human blood on human lymphocytes and investigated if Pb can affect oxidative stress and cellular organelles at these concentrations. So, in concentrations which have no cytotoxic effects, Pb is shown to induce oxidative stress in addition to inflicting damage on mitochondria and lysosomes in human blood lymphocytes. [ABSTRACT FROM AUTHOR]

Any microorganisms killing molecules have some cytotoxicity more or less. The effective way of reducing cytotoxicity mainly included two approaches: One was reducing the concentration of antiseptic, while this would lead to the decreased antimicrobial efficiency; the other way was choosing suitable antiseptics and then combining of them, which can balance the disinfection and cytotoxicity. In this paper, hydroxypropyltrimethyl ammonium chloride chitosan (HACC), a cationic natural macromolecular, as the first antiseptic, incorporated with polyhexamethylene biguanide (PHMB), a smaller molecular weight cationic antiseptic polymer, as the second antiseptic, their disinfection effect and cell cytotoxicity in borate buffer solution were investigated at fairly low contents. When HACC/PHMB weight ratios were 100/1 and 150/1, the disinfection solutions produced >1-log reductions against C. albicans and >3-log reductions against S. aureus and P. aeruginosa. HACC/PHMB disinfection solution at weight ratio of 150/1 even showed a highest antimicrobial efficiency and the cell proliferation rates were approximately 100% in MTT assays. Meanwhile, the research of micromorphology and fluorescence spectra indicated that bigger aggregation state of HACC-PHMB were helpful to improve antimicrobial ability. These results showed that the HACC-PHMB combination might be a promising candidate for novel antimicrobial group for biomedical applications. [ABSTRACT FROM AUTHOR]

This paper describes the synthesis of several new 4-arylaminoquinoline-3-carbonitriles derivatives. These were evaluated on the activity reverse transcriptase (RT) of HIV-1. Most of the synthesized compounds showed significant in vitro inhibition of RT enzyme, especially derivative 3h (IC50 = <8 μM). The derivatives showed low-level cytotoxicity. [ABSTRACT FROM AUTHOR]