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Piperazine-substituted chalcones: a new class of MAO-B, AChE, and BACE-1 inhibitors for the treatment of neurological disorders Full text
2021
Mathew, Bijo | Oh, Jong Min | Baty, Roua S. | Batiha, Gaber El-Saber | Parambi, Della Grace Thomas | Gambacorta, Nicola | Nicolotti, Orazio | Kim, Hun
Eleven piperazine-containing 1,3-diphenylprop-2-en-1-one derivatives (PC1-PC11) were evaluated for their inhibitory activities against monoamine oxidases (MAOs), cholinesterases (ChEs), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1) with a view toward developing new treatments for neurological disorders. Compounds PC10 and PC11 remarkably inhibited MAO-B with IC₅₀ values of 0.65 and 0.71 μM, respectively. Ten of the eleven compounds weakly inhibited AChE and BChE with > 50% of residual activities at 10 μM, although PC4 inhibited AChE by 56.6% (IC₅₀ = 8.77 μM). Compound PC3 effectively inhibited BACE-1 (IC₅₀ = 6.72 μM), and PC10 and PC11 moderately inhibited BACE-1 (IC₅₀ =14.9 and 15.3 μM, respectively). Reversibility and kinetic studies showed that PC10 and PC11 were reversible and competitive inhibitors of MAO-B with Kᵢ values of 0.63 ± 0.13 and 0.53 ± 0.068 μM, respectively. ADME predictions for lead compounds revealed that PC10 and PC11 have central nervous system (CNS) drug-likeness. Molecular docking simulations showed that fluorine atom and trifluoromethyl group on PC10 and PC11, respectively, interacted with the substrate cavity of the MAO-B active site. Our results suggested that PC10 and PC11 can be considered potential candidates for the treatment of neurological disorders such as Alzheimer’s disease and Parkinson’s disease.
Show more [+] Less [-]Design of puncher for recycling of waste film fragments Full text
2021
Chen, Panpan | Li, Jing | Wang, Zhimin
Although the recycling of an entire piece of plastic film after farmland use has attracted significant attention, the film fragments generated by punching holes in such plastic films have never been studied. These film fragments can penetrate deeper into the soil more easily than whole pieces of plastic film, causing soil pollution. In this study, two new punchers with burrs were designed, and a group of comparative experiments were conducted on waste film fragment recycling. The results show that the average time required to complete the same task using punchers with two burrs (puncher 3) and one burr (puncher 2) can be reduced by 40.37% and 26.19%, respectively. The average success rates in recycling the film fragments are 91.67% and 68.17%, respectively. The performance of puncher 3 is better than that of puncher 2 for recycling the film fragments. Thus, the application of puncher 3 is beneficial for solving the problems in waste film recycling. Accordingly, the study is of great significance for protecting the soil environment, reducing “white pollution” and achieving China’s sustainable development goals.
Show more [+] Less [-]The correlation between single nucleotide polymorphisms of the thymic stromal lymphopoietin receptor and breast cancer in a cohort of female patients in Saudi Arabia Full text
2021
Semlali, Abdelhabib | Almutairi, Mikhlid H. | Alharbi, Sultan N. | Alamri, Abdullah M. | Alrefaei, Abdulwahed F. | Almutairi, Bader O. | Rouabhia, Mahmoud
The current study aimed to examine thymic stromal lymphopoietin receptor (TSLPR) genetic variation and breast cancer (BC) susceptibility in women in Saudi Arabia. Therefore, 127 blood samples from female patients diagnosed with BC and 116 blood samples from healthy female controls were studied using a genotyping assay to determine the association between three TSLPR single nucleotide polymorphisms (SNPs)—P196L, X201W, and A238V—and the risk of BC progression. In addition, gene expression was evaluated in 20 matching BC and normal tissues using immunohistochemistry. TSLPR protein levels were higher among BC patients than those with matching normal breast tissue. In addition, TSLPR SNP P196L was found to have a significant protective effect on BC progression (OR = 0.4427), although only the T allele for TSLPR P196L had this protective effect against BC progression in participants who were younger than 48 years old. In contrast, no association was found between the T allele and risk of BC in participants who were older than 48 years old, and the CT and TT genotypes were significantly associated with BC risk protection in the older group. The effects of the TT genotype and the T allele were closely associated with a decreased risk of BC in participants with estrogen receptors (ER+) and without them (ER−). Overall, the findings revealed a significant correlation between SNPs in the TSLPR genes and BC progression among women in Saudi Arabia.
Show more [+] Less [-]Stable isotopic characterization of nitrate wet deposition in the tropical urban atmosphere of Costa Rica Full text
2021
Villalobos-Forbes, Mario | Esquivel-Hernández, Germain | Sánchez-Murillo, Ricardo | Sánchez-Gutiérrez, Rolando | Matiatos, Ioannis
Increasing energy consumption and food production worldwide results in anthropogenic emissions of reactive nitrogen into the atmosphere. To date, however, little information is available on tropical urban environments where inorganic nitrogen is vastly transported and deposited through precipitation on terrestrial and aquatic ecosystems. To fill this gap, we present compositions of water stable isotopes in precipitation and atmospheric nitrate (δ¹⁸O-H₂O, δ²H-H₂O, δ¹⁵N-NO₃⁻, and δ¹⁸O-NO₃⁻) collected daily between August 2018 and November 2019 in a tropical urban atmosphere of central Costa Rica. Rainfall generation processes (convective and stratiform rainfall fractions) were identified using stable isotopes in precipitation coupled with air mass back trajectory analysis. A Bayesian isotope mixing model using δ¹⁵N-NO₃⁻ compositions and corrected for potential ¹⁵N fractionation effects revealed the contribution of lightning (25.9 ± 7.1%), biomass burning (21.8 ± 6.6%), gasoline (19.1 ± 6.4%), diesel (18.4 ± 6.0%), and soil biogenic emissions (15.0 ± 2.6%) to nitrate wet deposition. δ¹⁸O-NO₃⁻ values reflect the oxidation of NOₓ sources via the ·OH + RO₂ pathways. These findings provide necessary baseline information about the combination of water and nitrogen stable isotopes with atmospheric chemistry and hydrometeorological techniques to better understand wet deposition processes and to characterize the origin and magnitude of inorganic nitrogen loadings in tropical regions.
Show more [+] Less [-]Effects of diurnal temperature range on cardiovascular disease hospital admissions in farmers in China’s Western suburbs Full text
2021
Zha, Qunwu | Chai, Guorong | Zhang, Zhe George | Sha, Yongzhong | Su, Yana
Cardiovascular disease (CVD), reported to relate with climate change, is the leading cause of global mortality and morbidity. Since the relevant information is quite limited from suburbs and countryside in developing and underdeveloped countries, there are no studies that focused on morbidity through diurnal temperature range (DTR) for these regions. This is the first study to evaluate the short-term effect of DTR on CVD hospital admission in suburban farmers, as well as to identify vulnerable subpopulations. Daily time series data of CVD hospital admissions on suburban farmers of Qingyang, China, and meteorological data from 2011 to 2015 were collected, and a distributed lag non-linear model (DLNM) combined with a quasi-Poisson generalized additive regression model (GAM) was used to examine the exposure-response relationship and delayed effect between DTR and CVD hospital admissions. Stratified analyses by age and gender were performed and extreme DTR effects were examined. Non-linear relation between DTR and CVD hospital admissions was observed, and whether DTR lower or higher than the reference (13 °C, 50ᵗʰ percentile) had adverse effect while lower DTR have slightly higher impact. Also, both extreme low and extreme high DTR had adverse effect. Besides, adults (age < 65) and males were more vulnerable to the effects of DTR compared with the old (age ≥ 65) and females, respectively. This study provides evidence that not only high DTR but also low DTR had adverse effects on CVD which should be paid attention to. Adults and males were more vulnerable among suburban farmers. The results are inconsistent with the studies from urban and indicate differences between urban and suburban residents. Multiple factors such as occupations, risk awareness, and lifestyles could have a significant influence on CVD morbidity, and further study is needed to explore more evidence.
Show more [+] Less [-]Are aerosols on the leaves of apricot trees (Prunus armeniaca) signalizing the activity of a hidden paleo-supervolcano in a steppe? Full text
2021
Glinyanova, Irina | Fomichev, Valery | Asanova, Natali
Aerosols on plant leaves make it possible to assess the quality of air in settlements. The purpose of this work was to assess the acidity and specific electrical conductivity of aerosol suspensions (by washing off aerosol particles from the leaves of apricot trees (Prunus armeniaca)), which characterize the air pollution in the residential area of the Svetly Yar settlement (Volgograd region, Russia) during the spring-summer of 2019. The research hypothesis was as follows: Acidic mineralized aerosols with a mixed source are present in Svetly Yar. The differences were checked by the Student’s t-test and evaluated at the level of significance of p = 0.05. The results indicated the presence of acidic (pH = 4.56 + 0.02) and highly mineralized aerosols (EC = 130.41 + 0.17 μS/cm) in the ambient air of the Svetly Yar residential area during the spring-summer of 2019 and revealed environmental risks for the population in comparison with aerosol suspensions from a (relatively) clean location (pH = 6.46 + 0.02; EC = 37.61 + 0.19 μS/cm). The authors confirmed their hypothesis in favor of mixed source acidic mineralized aerosols in the residential area of the Svetly Yar village. The anthropogenic sources were the industrial zones of Svetly Yar, the southern part of the city of Volgograd and artificial sedimentation tanks in the southwestern part of Svetly Yar. A natural source of pollution in the vicinity of Svetly Yar may be hidden geologically active structures: faults in the Earth’s crust, a salt diapir, an underground ancient semiactive volcanic zone on a steppe, etc.
Show more [+] Less [-]Potential cytotoxicity of trace elements and polycyclic aromatic hydrocarbons bounded to particulate matter: a review on in vitro studies on human lung epithelial cells [Erratum: November 2021, v.28(43), p.61871] Full text
2021
Kermani, Majid | Rahmatinia, Tahere | Oskoei, Vahide | Norzaee, Samira | Shahsavani, Abbas | Farzadkia, Mahdi | Kazemi, Mohammad Hossein
A large number of studies have been conducted for clarifying toxicological mechanisms of particulate matter (PM) aimed to investigate the physicochemical properties of PM and providing biological endpoints such as inflammation, perturbation of cell cycle, oxidative stress, or DNA damage. However, although several studies have presented some effects, there is still no consensus on the determinants of biological responses. This review attempts to summarize all past research conducted in recent years on the physicochemical properties of environmental PM in different places and the relationship between different PM components and PM potential cytotoxicity on the human lung epithelial cells. Among 447 papers with our initial principles, a total of 50 articles were selected from 1986 to April 2020 based on the chosen criteria for review. According to the results of selected studies, it is obvious that cytotoxicity in human lung epithelial cells is created both directly or indirectly by transition metals (such as Cu, Cr, Fe, Zn), polycyclic aromatic hydrocarbons (PAH), and ions that formed on the surface of particles. In the selected studies, the findings of the correlation analysis indicate that there is a significant relationship between cell viability reduction and secretion of inflammatory mediators. As a result, it seems that the observed biological responses are related to the composition and the physicochemical properties of the PMs. Therefore, the physicochemical properties of PM should be considered when explaining PM cytotoxicity, and long-term research data will lead to improved strategies to reduce air pollution.
Show more [+] Less [-]Bioassays for the evaluation of reclaimed opencast coal mining areas Full text
2021
Honscha, Laiz Coutelle | Campos, Audrey Senandes | Tavella, Ronan Adler | Ramires, Paula Florencio | Volcão, Lisiane Martins | Halicki, Priscila Cristina Bartolomeu | Pech, Tatiani Maria | Bernardi, Eduardo | Ramos, Daniela Fernandes | Niemeyer, Júlia Carina | Baisch, Paulo Roberto Martins | Baisch, Ana Luíza Muccillo | da Silva Júnior, Flávio Manoel Rodrigues
This study aimed to use bioassays (single and multispecies) with organisms from different trophic levels to assess soil quality in reclaimed coal mining areas. Soil samples were collected from four sites: two sites with recent reclaim processes (one using topsoil and other using clayey soil), an natural attenuation site, and a control soil. The evaluated parameters were divided into (1) ecotoxicological tests (avoidance test with Eisenia andrei (earthworms) and Armadillidium vulgare (isopods); germination test with Sinapis alba seeds (mustard); reproduction tests with Folsomia candida (collembolans); bacterial toxicity test); (2) population and community assessments (a fungal count; microbial community analysis using Biolog EcoPlatesᵀᴹ); (3) microcosms scale evaluation (the MS-3 multispecies system); and (4) chemical analysis (soil parameters, soil metal, and cations and anions in soil leachate). Results pointed to toxicity in the natural attenuation site that compromised of habitat function, probably due to low pH and low nutrient levels. The most recent reclaim process, using topsoil and clay soil, improved soil quality and fertility, with a further increase in habitat quality and heterogeneity. This study shows that some techniques used to reclaim degraded mining areas are effective in rebuilding habitats, sustaining soil biota, and reestablishing ecosystem services.
Show more [+] Less [-]Monitoring and risk assessment of pesticide residue in plant-soil-groundwater systxem about medlar planting in Golmud Full text
2021
Jing, Xiuyan | Zhang, Wenyuan | Xie, Jinyan | Wang, Wenji | Lü, Tong | Dong, Qiangfei | Yang, Hongbin
Farm worker and consumers are vulnerable to the potentially toxic pesticides accumulated in the environment and food. Nonetheless, few studies have investigated the pesticide pollution and risk in the medlar planting site at a large scale. Hereupon, this study focused on the pesticide contamination distribution, their potential risk assessment of contaminated sites and dietary. The 11 pesticide pollution sources were collected from the five systems of fruit, leaf, soil, groundwater, and honey based on a systematic review in medlar planting site. Seventy-six samples were analyzed by chromatography technique. Residues of 4 (36.7%) compounds were found in the samples. The most distributed pesticides were imidacloprid for all samples, followed by avermectin for leaf, soil, groundwater, and honey, and carbendazim for leaf, glyphosate for soil, and those with the highest average concentrations were carbendazim (3.8–8.4 mg/kg of leaf) and glyphosate (0.21–1.3 mg/kg of soil). The vertical migration characteristic of imidacloprid was relatively stable, and the residual concentration gradually declined with the increase of burial depth. However, glyphosate tended to accumulate gradually or was close to the surface concentration with the increase of burial depth. The distribution of abamectin had no obvious regularity. Imidacloprid was lower than the MRL in fruit and honey. Imidacloprid, avermectin, and glyphosate no MRL in soil and groundwater are set. Using the monitoring data, potential health risk come from fruit, soil, and groundwater was evaluated. The HI and HQ could be considered safe for pesticide residues in fruit, soil, and groundwater. Even if these results are in general safe to eat, the effects of insecticide on human health, especially on genetic toxicity, have gradually aroused more attention. To minimize the increasing human health risk, this study suggests that authorities must regulate the usage of agrochemicals, to strengthen the controls for effective implementation of the pesticide bans.
Show more [+] Less [-]Fertilization with Poultry Litter Increases the Abundance of Antibiotic-Resistant Bacteria in Tropical Soil: a Microcosm Study Full text
2021
Chaves-Ulate, Carolina | Granados-Chinchilla, Fabio | Rodríguez, César
Various antimicrobial agents are used in the poultry industry to treat microbial infections and prevent disease or as growth promoters. As a result, poultry litter (PL) can contain antibiotic residues (AR), antibiotic-resistant bacteria (ARB), and antibiotic resistance genes. Still, PL is used in many countries as a fertilizer and feed supplement for cattle. To evaluate whether usage of PL in agriculture leads to the accumulation of AR and ARB accumulate in the soil, we (i) measured the concentration of monensin, tylosin, ciprofloxacin, oxytetracycline, and chlortetracycline and the abundance of culturable monensin-, tylosin-, and ciprofloxacin-resistant bacteria in 15 commercial PL samples and (ii) exposed soil microcosms to two PL regimes and followed the persistence of PL-associated ARB for 128 days through cultivation on media containing antibiotics. The PL samples analyzed contained high concentrations of monensin (27–95 mg kg⁻¹), tylosin (152–450 mg kg⁻¹), ciprofloxacin (29–101 mg kg⁻¹), and (oxy/chlor)tetracycline (13–87 mg kg⁻¹). Congruently, they included large absolute and relative numbers of bacteria capable of growing on agar plates supplemented with 5 to 50 μg mL⁻¹ monensin (medians, 10⁷–10⁹ CFU g⁻¹, 0.6–45%) or 25 to 50 μg mL⁻¹ tylosin (median, 10⁸ CFU g⁻¹, 14–26%). By contrast, the abundance of bacteria resistant to 25–250 μg mL⁻¹ CP in the PL samples was much lower (median values ranging from 10⁶ to less than 10² CFU g⁻¹, relative abundances, < 0.13%). We observed rapid increments of 1–3 logs in the amount of culturable tylosin- and CP-resistant bacteria in most microcosms upon fertilization (n = 3/4 and n = 5/8, respectively, p < 0.01). Half of these increments were sustained across the experiment (p < 0.05), demonstrating that the introduced ARB can thrive in soil. These results show that fertilization with PL can increase the basal amount of tylosin- and CP-resistant bacteria in the soil. The environmental and sanitary consequences of this finding justify changes in PL’s manufacturing process and a debate on its approved uses in agricultural systems.
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