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Objective: The present research aims to synthesize some new polycyclic compounds including chromene moiety and study their antimicrobial activity. Methods: Several new polycyclic systems including chromene scaffold incorporated with pyridine, pyrimidine, imidazopyrimidine, and imidazodiazocine were achieved via condensation reaction of chromene derivative under the proper condition with various reagents namely; cyanothioacetamide, phenyl isothiocyanate, malononitrile, carbon disulfide, benzaldehyde, triethyl orthoformate, and 1,4-dichlorobutane. Moreover, a chlorodiazenyl chromene derivative was reacted with some substances possessing active–CH2-bridge such as ethyl cyanoacetate and malononitrile to end up with hydrazono compounds. Such compounds were eventually cyclized with hydrazine hydrate to form pyrazole and oxopyrazole derivatives. Moreover, compound 1 was treated with benzoyl acetone, and then followed by cyclization with malononitrile to provide the corresponding 2-amino14-(4-methoxyphenyl)-4-methy-5-phenyl-14H-benzo[5,6] chromeno [2,3H][1,6]naphthyridine-3-carbonitrile (20). Results: The results of the antimicrobial screening in vitro revealed that the inhibition zone (mm) of the synthesized compounds 1-3, 5 and 8 implied their optimum antibacterial activity, while the compounds 4, 6 and 9-13, 15 showed a moderate to weak antibacterial activity against multiple species of B. subtilis, S. aureus, E. coli and P. aeruginosa. In contrast, the compounds 1, 6, 11, 15 showed high antifungal activities against different species of A. flavinand C. albicans, while the other compounds exhibit a moderate to poor antifungal activity. Conclusion: It is remarkable that a series of chromene derivatives synthesized by a simple and available method leads to a molecule of promising antimicrobial activity. Further research is recommended to approve the importance of polycyclic systems for various applications.
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Objective To analyze the association between polycyclic aromatic hydrocarbons(PAHs)exposure and rheumatoid arthritis (RA)based on large sample data.Methods The RA patients(RA group)and non-RA patients(non-RA group)with complete data were selected from the National Health and Nutrition Survey Database in the United States(NHANES)(2005-2014).The logistic regression model was used to analyze the association between 8 monohydroxylated(OH-)PAH metabolites in the urine and RA.Results A total of 357 RA patients and 5,256 non-RA participants were included.After adjusting the confounding factors by logistic analysis,the level of OH-PAHs mixture at the highest quartile(Q4)was associated with increased risk of RA compared with that at the lowest quartile(Q1) (OR =1.60,95 ％ CI:1.16 2.23).For a single kind of OH-PAHs,the Q4 levels of 1-hydroxynaphthalene (OR =1.59,95 ％ CI.1.14-2.23),2-hydroxynaphthalene (OR =1.66,95 ％ CI:1.19-2.32),2-hydroxyfluorene(OR =1.61,95 ％ CI:1.17-2.22),3-hydroxyfluorene(OR =1.64,95％ CI:1.18-2.27) and 1-hydroxyphenanthrene (OR =1.38,95 ％ CI:1.00-1.94) were all associated with significantly increased risk of RA compared with the Q1 level(all P＜0.05).However,the Q2 level of 1-hydroxypyrene(OR =0.60,95％ CI:0.43-0.83) was related to a decreased incidence of RA (P＜0.01).Conclusions OH-PAHs mixed exposure is a risk factor for RA.The association between the level of individual OH-PAH and the rate of RA is bidirectional and is depended on the type and concentration of OH-PAHs.
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Objective@#To analyze the association between polycyclic aromatic hydrocarbons(PAHs)exposure and rheumatoid arthritis(RA)based on large sample data.@*Methods@#The RA patients(RA group)and non-RA patients(non-RA group)with complete data were selected from the National Health and Nutrition Survey Database in the United States(NHANES)(2005—2014). The logistic regression model was used to analyze the association between 8 monohydroxylated(OH-)PAH metabolites in the urine and RA.@*Results@#A total of 357 RA patients and 5, 256 non-RA participants were included.After adjusting the confounding factors by logistic analysis, the level of OH-PAHs mixture at the highest quartile(Q4)was associated with increased risk of RA compared with that at the lowest quartile(Q1)(OR=1.60, 95%CI: 1.16-2.23). For a single kind of OH-PAHs, the Q4 levels of 1-hydroxynaphthalene(OR=1.59, 95%CI: 1.14-2.23), 2-hydroxynaphthalene(OR=1.66, 95%CI: 1.19-2.32), 2-hydroxyfluorene(OR=1.61, 95%CI: 1.17-2.22), 3-hydroxyfluorene(OR=1.64, 95%CI: 1.18-2.27)and 1-hydroxyphenanthrene(OR=1.38, 95%CI: 1.00-1.94)were all associated with significantly increased risk of RA compared with the Q1 level(all P<0.05). However, the Q2 level of 1-hydroxypyrene(OR=0.60, 95%CI: 0.43-0.83)was related to a decreased incidence of RA(P<0.01).@*Conclusions@#OH-PAHs mixed exposure is a risk factor for RA.The association between the level of individual OH-PAH and the rate of RA is bidirectional and is depended on the type and concentration of OH-PAHs.
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Objective: The present research aims to synthesize some new polycyclic compounds including chromene moiety and study their antimicrobial activity. Methods: Several new polycyclic systems including chromene scaffold incorporated with pyridine, pyrimidine, imidazopyrimidine, and imidazodiazocine were achieved via condensation reaction of chromene derivative under the proper condition with various reagents namely; cyanothioacetamide, phenyl isothiocyanate, malononitrile, carbon disulfide, benzaldehyde, triethylorthoformate, and 1,4-dichlorobutane. Moreover, a chlorodiazenyl chromene derivative was reacted with some substances possessing active–CH2-bridge such as ethyl cyanoacetate and malononitrile to end up with hydrazono compounds. Such compounds were eventually cyclized with hydrazine hydrate to form pyrazole and oxopyrazole derivatives. Moreover, compound 1 was treated with benzoyl acetone, and then followed by cyclization with malononitrile to provide the corresponding 2-amino14-(4-methoxyphenyl)-4-methy-5-phenyl-14H-benzo[5,6] chromeno[2,3H][1,6]naphthyridine-3-carbonitrile (20). Results: The results of the antimicrobial screening in vitro revealed that the inhibition zone (mm) of the synthesized compounds 1-3, 5 and 8 implied their optimum antibacterial activity, while the compounds 4, 6 and 9-13, 15 showed a moderate to weak antibacterial activity against multiple species of B. subtilis, S. aureus, E. coli and P. aeruginosa. In contrast, the compounds 1, 6, 11, 15 showed high antifungal activities against different species of A. flavinand C. albicans, while the other compounds exhibit a moderate to poor antifungal activity. Conclusion: It is remarkable that a series of chromene derivatives synthesized by a simple and available method leads to a molecule of promising antimicrobial activity. Further research is recommended to approve the importance of polycyclic systems for various applications.
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Objetivo: Evaluar el efecto genotóxico de las mezclas complejas de hidrocarburos en los trabajadores de estaciones de servicio de gasolina en Barranquilla (Atlántico, Colombia) a través de la prueba Cometa(CA) alcalina. Materiales y métodos: Se realizó un estudio transversal, prospectivo inferencial de casos y controles. El grupo control estuvo conformado por 15 personas no expuestas laboralmente a hidrocarburos y el expuesto por 38 personas que trabajaron al menos 1 año como despachador de combustible. Se realizó un ensayo cometa alcalino en sangre venosa. Se determinó el efecto genotóxico utilizando el porcentaje de ADN n la cola y por Unidades Arbitrarias de daño. La comparación entre grupos se realizó por la prueba t-student o W-Wilcoxon. Los datos fueron modelados con una regresión simple ajustada. Los análisis de datos fueron realizados con el paquete estadístico R. Resultados: Las edades de los grupos control y experimental fueron de 33±9 y 38±10 años, respectivamente; no hubo diferencia estadísticamente significativa para esta variable (t = -1.82; p-valor > 0,05; a = 95%). Hubo asociación entre Edad y Tiempo de Exposición (x² = 24.9; p-valor < 0,05; a = 95%). El %ADN en la cola para el grupo control fue de 20,67±25,79, mientras que para el grupo expuesto fue 53,35±40,28. El modelo de degradación de ADN es «y=√l(512,687+733,899√1(t))¼. Conclusiones: Las mezclas complejas de heterocíclicos son potencialmente genotóxicas. El daño progresivo se encuentra al 80 % después de 6 años de exposición, siendo igual a los 9 años de exposición que a los 15.
Objective: To evaluate the genotoxic effects of complex mixtures of hydrocarbons in gasoline stations's workers in Barranquilla (Atlántico, Colombia) using the alkaline Comet Assay (CA). Materials and methods: Study was transversal, prospective inferential of case and control. The controls were 15 persons without occupationally exposed to hydrocarbons and the exposed were 38 persons that were working at least one year as fuel dispenser. The alkaline Comet Assay was performed on venous blood. Genotoxic effects was determined throug DNA percentage in tail and damage Arbitrary Units. The comparison between groups was performed by t-student or W-Wilcoxon test. The data were modeled with a simple regression adjusted. The data analyses were performed with the statistical package R. Results: Age of control and experimental groups were 33±9 and 38±10 years respectively, there was no statistically significant difference for this variable (t = -1.82; p-value > 0.05; a = 95 %). There was an association between Age and Exposure Time (x² = 24.9; p-value < 0.05, a = 95%). The %DNA tail for the control group was 20.67 ± 25.79, while for the exposed group was 53.35± 40.28. The DNA degradation model is «y=√ (512.687+733,899√ (t))¼. Conclusions: The complex mixtures of heterocyclic are potentially genotoxic. As the progressive damage is 80 % after 6 years of exposure, being equal damage to the 9 to 15 years of exposure.
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O estuário de Santos abriga o maior porto da América Latina e um dos maiores complexos industriais do Brasil. Na década de 1970 foi considerado um dos maiores exemplos de degradação ambiental em ambientes costeiros, e apesar da melhora na qualidade ambiental observada nos últimos anos algumas áreas deste estuário apresentam sedimentos ainda altamente contaminados com compostos tóxicos e genotóxicos, especialmente os Hidrocarbonetos Policíclicos Aromáticos (HPA). Operações de dragagem para manutenção das atividades portuárias são necessárias e consequentemente durante este processo pode ocorrer a ressuspensão de contaminantes presentes nesses sedimentos, tornando-os disponíveis novamente na coluna d'água. Desta forma é interessante ter uma estratégia eficiente e aplicável no monitoramento da qualidade dessas águas...
Santos estuary is the major Latin American harbor and one of the largest industrial complex of Brazil. In the 1970s, it was considered one of the major examples of coastal degradation. Due to enforcement actions the quality of the environment has improved in the last years in relation to the chemical parameters and toxicity but unfortunately the sediment is still contaminated with toxic and genotoxic compounds especially Polycyclic Aromatic Hydrocarbons (PAHs). For the maintenance of the port activities sediment dredging is needed and during this process contaminants resuspension can occur, leading to the contamination of the water column. Therefore it is interesting to have an efficient strategy that can be used for the water quality monitoring of this area. The Blue rayon is a selective adsorbent to polycyclic compounds containing three or more fused rings and has been successfully used in the monitoring of PAHs and mutagenic activity in aquatic environments. The objective of this work was to evaluate a modified blue rayon hanging technique, denominated in this work "Blue rayon anchored technique", where the fibers are placed at a fixed distance from the sediment, associated with the Salmonella/microsome microsuspension assay in order to monitor the water quality of Santos estuary. Three sites with different sources and sediment contamination levels were selected in this study. Two initial samplings were performed in order to evaluate the efficiency of the BR modified technique and find the most sensitive strain of Salmonella typhimurium to the mutagens possibly present in the those waters as well as verify the presence of PAHs. Five subsequent samplings were performed to verify the performance and efficiency of the defined strategy in the estuary water quality monitoring using dose response experiments. In the two initial samplings, the water from the site containing the most contaminated sediment and under influence of COSIPA (site 1) presented higher mutagenic activity and higher levels of PAHs. It was also possible to verify the highest sensitivity of the YG1041 strain in the detection of the mutagenic activity in both sites analyzed. In the subsequent five samplings, higher mutagenic potencies were again observed for site 1, reaching 5,100 and 36,000 revertants per gram of BR for the YG1 041 strain in the absence and presence of S9 respectively. Sites 2 and: presented similar potencies, around 1000 revertants per gram of BR. Based on the obtained results we can conclude that the Blue rayon anchored technique associated with the Salmonella/microsome microsuspension assay with the YG1041 strain in the presence and absence of S9 is an suitable tool to monito Santos estuarine waters.