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Purpose: Smoking has a negative effect on health and ocular tear film. The purpose of the current study is to investigate the correlation between the TearLab and I-Pen osmolarity scores in smokers and compare them with those of non-smoking healthy males. Methods: Thirty male smokers (25.3 ± 2.2 years) participated in the study. An age-matched (22.9 ± 2.0 years) control group of non-smoking healthy males (N = 30) was also recruited for comparison purposes. The ocular surface disease index (OSDI) was completed first, followed by the TearLab and I-Pen osmolarity measurements. Results: The median TearLab osmolarity score was lower (P < 0.001) than that obtained using the I-Pen in both the study and the control groups. The OSDI scores and osmolality measurements were higher (P < 0.001) in smokers than in the control subjects. In the smoker group, there were moderate correlations between the OSDI scores and the measurements obtained using the TearLab (Spearman's correlation coefficient, r = 0.463; P = 0.010) and I-Pen (r = 0.449; P = 0.013) systems. In addition, there was a strong correlation between the osmolarity scores obtained from the TearLab and I-Pen systems in smokers (r = 0.911; P < 0.001). Conclusion: The I-Pen scores in smokers were significantly higher than those obtained using TearLab. The TearLab scores showed small variations compared with those obtained using I-Pen. A strong correlation was found between the TearLab and I-Pen scores in smokers. The osmolarity TearLab and I-Pen scores were significantly higher in smokers compared with normal eye subjects.
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Piperazine-based dithiocarbamates serve as important scaffolds for numerous pharmacologically active drugs. The current study investigates the design and synthesis of a series of dithiocarbamates with a piperazine unit as well as their biological activities. Under ultrasound conditions, the corresponding piperazine-1-carbodithioates 5a-5j were synthesized from monosubstituted piperazine 2 and N-phenylacetamides 4a-4j in the presence of sodium acetate and carbon disulfide in methanol. The structures of the newly synthesized piperazines were confirmed, and their anti-lung carcinoma effects were evaluated. A cytotoxic assay was performed to assess the hemolytic and thrombolytic potential of the synthesized piperazines 5a-5j. The types of substituents on the aryl ring were found to affect the anticancer activity of piperazines 5a-5j. Piperazines containing 2-chlorophenyl (5b; cell viability = 25.11 ± 2.49) and 2,4-dimethylphenyl (5i; cell viability = 25.31 ± 3.62) moieties demonstrated the most potent antiproliferative activity. On the other hand, piperazines containing 3,4-dichlorophenyl (5d; 0.1%) and 3,4-dimethylphenyl (5j; 0.1%) rings demonstrated the least cytotoxicity. The piperazine with the 2,5-dimethoxyphenyl moiety (5h; 60.2%) showed the best thrombolytic effect. To determine the mode of binding, in silico modeling of the most potent piperazine (i.e., 5b) was performed, and the results were in accordance with those of antiproliferation. It exhibits a similar binding affinity to PQ10 and an efficient conformational alignment with the lipophilic site of PDE10A conserved for PQ10A.
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Antineoplásicos , Piperazinas , Antineoplásicos/química , Sobrevivência Celular , Simulação por Computador , Piperazina/farmacologia , Piperazinas/química , Relação Estrutura-AtividadeRESUMO
SIGNIFICANCE: The current study compares the ocular tear film parameters in three different groups using a single noninvasive, practical, and easy-to-use tool. PURPOSE: This study aimed to assess the tear film in smokers, those with a high body mass index (BMI), and healthy subjects using the EASYTEAR view+. METHODS: Thirty men with a high BMI (>25 kg/m2; 24.4 ± 6.4 years), 30 smokers (25.1 ± 6.1 years), and 30 healthy subjects (22.2 ± 3.5 years) were recruited. Each subject completed the Ocular Surface Disease Index, followed by the assessment of noninvasive tear breakup time, tear meniscus height (TMH), and lipid layer patterns (LLPs). RESULTS: Significant differences were found in the median TMH scores between smokers and healthy subjects (P = .03) and between subjects with a high BMI and the healthy ones (P = .04). The median LLP score was significantly (P < .001) higher in normal subjects (4.0 [1.0]) than in smokers (2.4 [1.0]) and subjects with high BMI (2.0 [1.3]). For subjects with a high BMI, the noninvasive tear breakup time score was strongly correlated (Spearman rank correlation coefficient; r) with TMH (r = 0.552, P = .002) and LLP (r = 0.555, P = .001). The LLP showed that grade B (lipid layer thickness, 30 to 50 nm; more compact) was common in subjects with a high BMI, grade C (50 to 80 nm, gray waves) was predominant in smokers, and grade D (~80 nm, dense white-blue layer) represented the majority of normal eye subjects. CONCLUSIONS: Smokers and individuals with a high BMI showed significantly lower lipid layer grades and tear meniscus height scores compared with the control group. The assessment of tear film parameters using the EASYTEAR view+ supports the findings of previous studies that implicate smoking and high BMI as risk factors for dry eye.
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Síndromes do Olho Seco , Fumantes , Índice de Massa Corporal , Síndromes do Olho Seco/diagnóstico , Síndromes do Olho Seco/etiologia , Humanos , Masculino , Fumar/efeitos adversos , LágrimasRESUMO
The photooxidative degradation process of plastics caused by ultraviolet irradiation leads to bond breaking, crosslinking, the elimination of volatiles, formation of free radicals, and decreases in weight and molecular weight. Photodegradation deteriorates both the mechanical and physical properties of plastics and affects their predicted life use, in particular for applications in harsh environments. Plastics have many benefits, while on the other hand, they have numerous disadvantages, such as photodegradation and photooxidation in harsh environments and the release of toxic substances due to the leaching of some components, which have a negative effect on living organisms. Therefore, attention is paid to the design and use of safe, plastic, ultraviolet stabilizers that do not pose a danger to the environment if released. Plastic ultraviolet photostabilizers act as efficient light screeners (absorbers or pigments), excited-state deactivators (quenchers), hydroperoxide decomposers, and radical scavengers. Ultraviolet absorbers are cheap to produce, can be used in low concentrations, mix well with polymers to produce a homogenous matrix, and do not alter the color of polymers. Recently, polyphosphates, Schiff bases, and organometallic complexes were synthesized and used as potential ultraviolet absorbers for polymeric materials. They reduced the damage caused by accelerated and natural ultraviolet aging, which was confirmed by inspecting the surface morphology of irradiated polymeric films. For example, atomic force microscopy revealed that the roughness factor of polymers' irradiated surfaces was improved significantly in the presence of ultraviolet absorbers. In addition, the investigation of the surface of irradiated polymers using scanning electron microscopy showed a high degree of homogeneity and the appearance of pores that were different in size and shape. The current work surveys for the first time the use of newly synthesized, ultraviolet absorbers as additives to enhance the photostability of polymeric materials and, in particular, polyvinyl chloride and polystyrene, based mainly on our own recent work in the field.
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Three new polyphosphates were synthesized in good yields by reacting diethylenetriamine with the appropriate phosphate ester in ethanol under acidic conditions. The polyphosphate structures were determined using FT-IR and 1H-NMR spectroscopies, and their elemental compositions were confirmed by EDX spectroscopy. Polyphosphates were added to poly(vinyl chloride) (PVC) at low concentrations to fabricate thin films. The PVC films were irradiated with ultraviolet light for long periods, and the effect of polyphosphates as the photostabilizer was investigated by determining changes in the infrared spectra (intensity of specific functional group peaks), reduction in molecular weight, weight loss, and surface morphology. Minimal changes were seen for PVC films containing polyphosphate compared to that for the blank film. In addition, optical, scanning electron, and atomic force microscopies were used to inspect the surface morphology of films. Undesirable changes due to photodegradation were negligible in PVC films containing additives compared to films containing no additives. In addition, the surfaces were smoother and more homogeneous. Polyphosphates, and in particular ones that contain an ortho-geometry, act as efficient photostabilizers to reduce the rate of photodegradation. Polyphosphates absorb ultraviolet light, chelate with polymeric chains, scavenge radical moieties, and decompose peroxide residues.
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PURPOSE: To evaluate and compare the tear ferning patterns of non-stimulated and stimulated tears in normal eye male subjects using the tear ferning test. METHODS: Thirty-five male subjects aged 20-38 years with normal eyes were enrolled in the study. Subjects with dry eye or with a risk factor for eye dryness (eg, recent ocular surgery, contact-lens wearers, smokers, anemic, diabetes, and thyroid gland problems) were excluded from the study. Dry eye subjects were excluded based on the ocular surface diseases index scores, non-invasive tear break-up time, and tear meniscus height measurements from the right and left eyes. A tear sample was collected from both eyes in each subject to perform the tear ferning test for non-stimulated tears. After 10 mins, the tears were stimulated using a Schirmer strip, a tear sample was collected from both eyes in each participant, the tear ferning test was performed, and the ferns were graded based on the five-point tear ferning grading scale. RESULTS: The average tear ferning grade [median (interquartile range)] for non-stimulated tears from the right and left eyes was 0.60 (1.25) and 0.50 (1.31), respectively. For stimulated tears, the average tear ferning grade from the right and left eyes was 0.50 (1.05) and 0.75 (1.25), respectively. There was no significant difference in the tear ferning grades obtained from non-stimulated and stimulated tears (Wilcoxon test, P>0.05). CONCLUSION: This study found no significant difference in the tear ferning patterns obtained from non-stimulated and stimulated tears, or between the tear ferning patterns in the tears collected from the right and left eyes before and after stimulating tears. It seems that there were no changes in the chemical composition of tears before and after stimulation, possibly due to the steady concentration of electrolytes and lipids within the tear film for both non-stimulated and stimulated tears.
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Objective: To test the effect of a single dose of hot peppermint consumption on the tear film in normal eye subjects. Methods: Thirty healthy male subjects aged 18-39 years (23.20±2.17 years) were enrolled. Also, an age-matched control group of 30 male subjects (19-39 years, 23.50±0.70 years) was enrolled to test the effect of the hot water. Tear meniscus height (TMH), noninvasive tear breakup time (NITBUT), and tear ferning (TF) tests were performed for each patient 30 mins before and 60 mins after they drank hot peppermint. Results: Mean TMH measurements were higher postintervention (0.32±0.07) than preintervention (0.27±0.04 mm). Similarly, mean TF grades were significantly higher (2.07±1.20) postintervention than preintervention (0.84±0.71). By contrast, mean NITBUT was lower postintervention than preintervention (11.57±3.17 and 15.84±3.36, respectively). TMH measurements increased in 90% of the subjects. Conversely, NITBUT decreased in 96.7% of the subjects. For the control group that tests the effect of drinking hot water, the scores did not differ significantly in the three tests pre- and postintervention (PË0.05). TF grades increased in 93.3% of the subjects, postintervention. Conclusion: Tear film quality decreases significantly after peppermint beverage consumption. A similar observation has been made on the consumption of hot green tea drink.
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OBJECTIVE: The study aimed to investigate the acute effect of a single dose of green tea on the quality and quantity of tears in normal eye subjects. METHODS: Forty normal eye subjects (22 men and 18 women) aged 19-39 years were enrolled in the study. Also, an age matching control group (20 males and 20 females) was enrolled for comparison. McMonnies dry eye symptoms questionnaire and slit lamp were used for the exclusion criteria determination. Phenol red thread (PRT) test was performed on both eyes of each subject. A tear sample was collected from the lower tear meniscus of the right eye of each subject for the tear ferning (TF) test, which was performed before (30 minutes) and after (60 minutes) drinking green tea. RESULTS: The median PRT measurement after green tea consumption was lower (median [IQR]=23.50 [8.00] mm) compared to that before consumption (median [IQR]=27.00 [8.75] mm). In contrast, the median TF grade was significantly higher following green tea consumption than that before consumption (median [IQR]=2.65 [1.23] vs 1.50 [0.88] mm, respectively). The results show that TF grades increased in 97.5%, and the red phenol thread scores decreased in 80% of the subjects after green tea consumption compared to those before consumption. The PRT readings and TF grades were significantly different (P<0.05) before and after green tea consumption. CONCLUSION: Drinking green tea could have a significant effect on the eye tear film quality. Tear quality appeared to decrease after green tea consumption.
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A modified poly(vinyl chloride) honeycomb thin film containing a low concentration of a thiadiazole Schiff base and nickel(II) chloride was successfully fabricated using the casting process. The surface morphology of the synthesized thin film was investigated using the scanning electronic microscopy. The synthesized poly(vinyl chloride) thin film was found to have a homogeneous surface morphology with a high crystalline nature. The addition of nickel(II) chloride was discovered to be vital for the formation of the honeycomb like structure.
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The fabrication of tunable poly(vinyl chloride) porous films containing polyphosphate as an additive was successful. Irradiation of poly(vinyl chloride) films containing polyphosphate at a low concentration (0.5% by weight) with an ultraviolet light (λmax = 313 nm) for 300 h leads to the formation of a honeycomb like structure. The scanning electron microscopy images, at different magnification power, confirmed the production of the PVC honeycomb-like structure. The morphological images of the polymeric film showed a rough surface and a large number of regularly distributed hexagonal pores. The number of pores increased upon irradiation time and it was maximum after 300 h. The honeycomb structure formation could be due to the regular aggregation of polyphosphate among the polymeric chains, the increase in solution intrinsic viscosity and evaluation of hydrogen chloride gas through dehydrochlorination process.
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Three polyphosphates were used as inhibitors for poly(vinyl chloride) (PVC) photodegradation. The polyphosphates were added to PVC at a concentration of 0.5% by weight. The PVC films (40 µm thickness) were irradiated at room temperature with ultraviolet (UV) light for up to 300 h. The changes in PVC films after irradiation were monitored by Fourier transform infrared spectroscopy, weight loss, viscosity-average molecular weight determination, and atomic force microscopy. These changes were very noticeable in the blank PVC films compared to the ones obtained when additives were used. The polyphosphates can inhibit the PVC photodegradation through direct absorption of UV light, interactions with PVC chains, and acting as radical scavengers.
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Fotólise/efeitos dos fármacos , Polifosfatos/farmacologia , Cloreto de Polivinila/química , Microscopia de Força Atômica , Estrutura Molecular , Peso Molecular , Espectroscopia de Infravermelho com Transformada de Fourier , ViscosidadeRESUMO
OBJECTIVES: To investigate the cytotoxic effect of anastrozole on breast (MCF7), liver hepatocellular (HepG2), and prostate (PC3) cancer cells. Methods: This is a prospective study. Anastrozole's mechanism of apoptosis in living cells was also determined by high content screening (HCS) assay. Methylthiazol tetrazolium (MTT) assay was carried out at the Centre of Biotechnology Research's, Al-Nahrain University, Baghdad, Iraq between July 2015 and October 2015. The HCS assay was performed at the Centre for Natural Product Research and Drug Discovery, Department of Pharmacology, Faculty of Medicine, University of Malaya, Kuala Lumpur, Malaysia between November 2015 and February 2016. Results: The most significant cytotoxic effect of anastrozole towards 3 cancer cell lines was obtained when its concentration was 400 µg/mL. The MCF7 cells were more sensitive to anastrozole compared with the HepG2 and PC-3 cells. There was a significant increase in membrane permeability, cytochrome c and nuclear intensity when anastrozole (200 µg/mL) was used compared with doxorubicin (20 µg/mL) as a standard. Also, there was a significant decrease in cell viability and mitochondrial membrane permeability when anastrozole (200 µg/mL) was used compared with positive control. Conclusion: Anastrozole showed cytotoxic effects against the MCF7, HepG2, and PC3 cell lines as determined in-vitro by the MTT assay. The HCS technique also showed toxic effect towards MCF7. It is evident that anastrozole inhibits the aromatase enzyme preventing the aromatization mechanism; however, it has a toxic effect.
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Antineoplásicos Hormonais/farmacologia , Inibidores da Aromatase/farmacologia , Nitrilas/farmacologia , Triazóis/farmacologia , Anastrozol , Apoptose/efeitos dos fármacos , Aromatase/metabolismo , Permeabilidade da Membrana Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Citocromos c/metabolismo , Doxorrubicina/farmacologia , Células Hep G2 , Humanos , Células MCF-7 , Membranas Mitocondriais/efeitos dos fármacosRESUMO
Three phosphate esters 1â»3 were successfully synthesized from the reaction of 2-, 3- and 4-hydroxybenzaldehyde with phosphoryl chloride. Reactions of 1â»3 with benzidine in the presence of glacial acetic acid gave the corresponding novel phosphorus organic polymers 4â»6 containing the azomethane linkage. The structures of the synthesized compounds were confirmed by Fourier transform infrared spectroscopy, nuclear magnetic resonance and elemental analysis. Interesting physiochemical properties for the polymeric materials 4â»6 were observed using a combination of several techniques such as gel permeation chromatography, scanning electron microscopy, Brunauerâ»Emmettâ»Teller and nitrogen adsorptionâ»desorption isotherm, Barrettâ»Joynerâ»Halenda and H-sorb 2600 analyzer. The mesoporous polymers 4â»6 exhibit tunable porosity with Brunauerâ»Emmettâ»Teller surface area (SABET = 24.8â»30 m²·gâ»1), pore volume (0.03â»0.05 cm³·gâ»1) and narrow pore size distribution, in which the average pore size was 2.4â»2.8 nm. Polymers 4â»6 were found to have high gas storage capacity and physico-chemical stability, particularly at a high pressure. At 323 K and 50 bars, polymers 4â»6 have remarkable carbon dioxide uptake (up to 82.1 cm³·gâ»1) and a low hydrogen uptake (up to 7.4 cm³·gâ»1). The adsorption capacity of gasses for polymer 5 was found to be higher than those for polymers 4 and 6.
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Techniques that quantify molecular endpoints sufficiently sensitive to identify and classify potentially toxic compounds have wide potential for high-throughput in vitro screening. Expression of three genes, RAD51C, TP53 and cystatin A (CSTA), in HEPG2 cells was measured by Q-PCR amplification. In parallel, we developed alternative assays for the same 3 gene signature based on an acridinium-ester chemiluminescent reporter molecule. HEPG2 cells were challenged with eighteen different compounds (n=18) chosen to represent compounds that are genotoxic (n=8), non-genotoxic non-carcinogenic (n=2) or have a less well defined mechanism of action with respect to genotoxicity (n=8). At least one of the three genes displayed dysregulated expression in the majority of compounds tested by Q-PCR and ten compounds changed the CSTA expression significantly. Acridinium-ester labelled probes for the three genes were synthesised and tested. Analytical sensitivity was characterised and suggested a limit of detection generally better than 0.1fmol but often 10-50 attomol. A linear amplification step was optimised and this quantitative method detected statistically significant increases in RAD51C and CSTA expression in agreement with the Q-PCR results, demonstrating the potential of this technology. The broad agreement of the amplified chemiluminescent method and Q-PCR in measuring gene expression suggests wider potential application for this chemiluminescent technology.
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Cistatina A/genética , Proteínas de Ligação a DNA/genética , Expressão Gênica/efeitos dos fármacos , Mutagênicos/toxicidade , Proteína Supressora de Tumor p53/genética , Células Hep G2 , Humanos , Medições Luminescentes , Reação em Cadeia da Polimerase/métodosRESUMO
Purpose. To investigate the effect of cigarette smoking on the ocular tear film. Methods. Thirty healthy young male cigarette smokers (20-38 years old) and 30 healthy age matched nonsmokers were enrolled in the study. McMonnies questionnaire, slit lamp, and PRT test were used to screen the subjects. Tear samples were collected from the right eyes and tear ferning patterns were observed and graded. Results. The mean MacMonnies scores and TF grades were significantly higher in the smoker subjects (mean ± SD = 9.83 ± 5.22 and 0.96 ± 0.54, resp.) compared to nonsmokers (mean ± SD = 5.96 ± 3.06 and 0.41 ± 0.38, resp.). The mean values obtained from PRT and TBUT tests were 22.23 ± 6.35 mm and 12.17 ± 3.81 s for smokers and 22.16 ± 5.63 mm and 14.13 ± 2.62 s for nonsmokers, respectively. Strong correlations were found between MacMonnies scores and both PRT (r = 0.596) and TF (r = 0.516). There was statistically significant difference in TF grades (p = 0.00), TBUT (p = 0.036) and McMonnies (p = 0.02) between smokers and nonsmokers. Conclusion. Cigarette smoking could have a significant effect on the tear film quality of the eye.
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A novel series of diphenyl 1-(arylamino)-1-(pyridin-3-yl)ethylphosphonates 1-5 was obtained in high yields from reactions of 3-acetyl pyridine with aromatic amines and triphenylphosphite in the presence of lithium perchlorate as a catalyst. The structures of the synthesized compounds were confirmed by IR, (1)H NMR spectral data and microanalyses. Compounds 1-5 showed high antimicrobial activities against Escherichia coli (NCIM2065) as a Gram-negative bacterium, Bacillus subtilis (PC1219) and Staphylococcus aureus (ATCC25292) as Gram-positive bacteria and Candidaalbicans and Saccharomyces cerevisiae as fungi, at low concentrations (10-100 µg/mL). Also, the synthesized compounds showed significant cytotoxicity anticancer activities against liver carcinoma cell line (HepG2) and human breast adenocarcinoma cell line (MCF7). The lethal dose of the synthesized compounds was also determined and indicated that most compounds are safe to use.