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1.
Bull Environ Contam Toxicol ; 110(2): 44, 2023 Jan 21.
Artigo em Inglês | MEDLINE | ID: mdl-36680693

RESUMO

Long- term application of marginal quality water accumulated significant amount of pollutant into the soil. It reduces soil health parameters, and crop yield and their quality. In this regards, graded application of pressmud (PM), i.e. 0, 2.5, 5 and 10 g/kg was applied on lead (Pb) contamination level (0, 100, 150, 300 mg/kg) and evaluated interaction effect on plant nutrients uptake by spinach. Analytical data showed that increasing the PM levels enhanced the macro (phosphorus, potassium, sulphur) and micro-nutrient (zinc, copper, manganese, iron) concentration into the soil. Whereas, increasing the level of Pb significantly (p ≤ 0.05) reduced the P, K and S nutrient concentration and uptake pattern by spinach crop. Increasing PM levels (control to 10 g/kg soil) improved P, K and S by 46.99, 98.96 and 76.79%, respectively in soil. This study is useful to formulate management strategies for minimizing Pb contamination in the food chain by the application of PM mostly in peri-urban areas.


Assuntos
Chumbo , Poluentes do Solo , Manganês , Zinco/análise , Nutrientes , Solo , Poluentes do Solo/análise
2.
Environ Monit Assess ; 195(1): 31, 2022 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-36282356

RESUMO

Industrialization results in production of large volume of wastewaters, and disposing of them become a serious problem. The wastewaters may have range of heavy metals, which have an impact on soil and plant health. The objective was to evaluate the influence of farm yard manure (FYM) and pressmud (PM) applications on Indian mustard growth and chromium (Cr) uptake in tannery effluent irrigated Cr-contaminated soil. Soil was collected from the tannery effluent irrigated fields (chromium contaminated) of Shekhpura village of Kanpur, India. A pot culture experiment was carried out by growing Indian mustard (Brassica juncea) var. RH 749 on the Cr-contaminated soil with application of different levels and combinations of FYM and PM (at 0, 2.5, and 5 g kg-1 each). Biomass yield, Cr uptake, bioconcentration factor (BCF), transfer factor (TF), transfer efficiency (TE), and Cr removal indices were examined. Higher doses of FYM and PM resulted in reduction of Cr concentrations in shoot (6.60 to 2.50 µg g-1) and root (27.27 to 9.43 µg g-1); and absorption in plant tissues and had improved total dry matter yield (14.56 to 30.94 g pot-1). The use of FYM and PM had a substantial (p ≤ 0.05) impact on phytoremediation parameters like BCF (0.128 to 0.045), TE (59.61 to 64.51%), and Cr removal (0.65 to 0.51%). Combined application of FYM (5 g kg-1) and PM (5 g kg-1) had enhanced the dry matter yield of shoot (12.51 to 26.40 g pot-1) and root (2.05 to 4.54 g pot-1) and reduced the Cr uptake (138.54 to 108.79 mg pot-1) than the individual amendment addition of FYM (138.52 to 135.89 mg pot-1) and PM (126.02 to 130.52 mg pot-1). Combined application of FYM (5 g kg-1) and PM (5 g kg-1) could be beneficial for remediation of Cr-contaminated areas for cultivation of crops.


Assuntos
Metais Pesados , Poluentes do Solo , Mostardeira , Cromo , Poluentes do Solo/análise , Disponibilidade Biológica , Esterco , Águas Residuárias , Fator de Transferência , Monitoramento Ambiental , Solo , Biodegradação Ambiental , Metais Pesados/análise
3.
Environ Monit Assess ; 195(1): 107, 2022 Nov 14.
Artigo em Inglês | MEDLINE | ID: mdl-36376496

RESUMO

Lead (Pb) pollution is a severe problem that primarily affects food chain in developing countries. Continuous use of Pb containing effluent for growing food crops builds up measurable concentration of Pb in soils; and adversely affects the soil properties and crop produce quality. To reduce the Pb metal toxicity in contaminated soil, a pot experiment was conducted with graded doses of pressmud (PM) (0, 2.5, 5.0, and 10.0 g/kg) and Pb (0, 100, 150, and 300 mg/kg soil). Various metal dynamics parameters were computed after spinach crop was harvested. Result showed that higher doses of Pb (300 mg/kg) diminished the spinach root and shoot biomass during the study; whereas, application of PM improved the spinach biomass. However, increasing the pressmud reduced the Pb concentration in shoot from 6.16, 5.99, 4.94, and 3.39 µg/g. Maximum reduction was measured in highest PM applied treatment in shoot (44.92%) and root (57.33%). In this experiment, increasing level of Pb significantly uptake was recorded with higher application rate of Pb (150 and 300 mg/kg). However, elevated doses of PM from control initially enhanced the small chunk of Pb and drastically reduced the shoot Pb uptake (0.060 to 0.049 mg/pot) in maximum level of PM applied treatment. This study is very useful to improve the soil health by immobilizing the labile fraction of Pb by addition of PM in Pb-contaminated soils.


Assuntos
Chumbo , Poluentes do Solo , Chumbo/toxicidade , Chumbo/análise , Spinacia oleracea , Poluentes do Solo/toxicidade , Poluentes do Solo/análise , Biomassa , Monitoramento Ambiental , Solo , Biodegradação Ambiental
4.
Environ Dev Sustain ; : 1-32, 2022 May 24.
Artigo em Inglês | MEDLINE | ID: mdl-35645606

RESUMO

The availability of freshwater is limited for agriculture systems across the globe. A fast-growing population demands need to enhance the food grain production from a limited natural resources. Therefore, researchers and policymakers have been emphasized on the production potential of agricultural crops in a sustainable manner. On the challenging side, freshwater bodies are shrinking with the pace of time further limiting crop production. Poor-quality water may be a good alternative for fresh water in water scarce areas. It should not contain toxic pollutants beyond certain critical levels. Unfortunately, such critical limits for different pollutants as well as permissible quality parameters for different wastewater types are lacking or poorly addressed. Marginal quality water and industrial effluent used in crop production should be treated prior to application in crop field. Hence, safe reuse of wastewater for cultivation of food material is necessary to fulfil the demands of growing population across the globe in the changing scenario of climate.

5.
Environ Monit Assess ; 191(12): 754, 2019 Nov 16.
Artigo em Inglês | MEDLINE | ID: mdl-31734742

RESUMO

In peri-urban areas, the use of wastewater for crop production is a common practice due to water scarcity. Moreover, in the recent years, large quantity of wastewater generation and discharge as industrial effluent in water resources is another issue for reduction of water quality. The leather industries are significantly contributing chromium (Cr) in effluent, whereas, other industries may have salt and cationic load in their discharges are mixed up. Therefore, it is mandatory to study the interactive effect of different effluent constituents on crop plants. In this connection, a pot culture experiment was conducted at the ICAR-Indian Institute of Soil Science, Bhopal to compute the effect of application of calcium (Ca) and sodium (Na) ions on Cr uptake by spinach crop in Vertisol of central India. Three levels of Cr (0, 50, 100 mg kg-1), calcium (0, 2, 4 mM), and sodium (0, 40, 80 mM) were applied in combinations. The spinach variety All Green was used as a test crop and harvested at full maturity. Results showed that application of Ca and Na reduced the Cr uptake in spinach crop. The reduction of Cr uptake was more in the root than shoot. Applied calcium acted as an essential plant nutrient and enhanced the crop biomass. Sole applications of Na adversely affected the crop biomass and Cr uptake in both root and shoot of spinach. In conclusion, application of Ca fertilizers reduced the Cr toxicity in spinach and could be used as a strategy for the safe utilization of tannery industrial effluents for crop production.


Assuntos
Cálcio/química , Cromo/metabolismo , Produção Agrícola/métodos , Sódio/química , Poluentes do Solo/análise , Spinacia oleracea/química , Biomassa , Monitoramento Ambiental , Fertilizantes/análise , Índia , Raízes de Plantas/química , Águas Residuárias/química
6.
Environ Monit Assess ; 191(7): 429, 2019 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-31190097

RESUMO

Chromium (Cr) is one of the toxic metals adversely affecting organisms including humans in the ecosystems, and it is present in considerable concentration in the tannery industrial effluent. Toxicity expression of Cr is suspected to be influenced considerably by other accompanying ions present in the effluent used for irrigation. In a screen house experiment, interactive effects of chloride and sulfate ions in a Vertisol on uptake of Cr by spinach crop were investigated and treatments imposed were three levels each of Cr (0, 50, 100 mg kg-1), chloride (Cl-) (0, 25, 50 mM kg-1), and sulfur (S) (0, 4, 8 mM kg-1) in possible combinations. Plant growth parameters and leaf Cr concentrations were recorded to find out the effect of anions on Cr dynamics in the plant. Increasing the concentration of Cl- ions in soil reduced the Cr concentration in both root and shoot. Similarly, increasing the concentration of S from 4 to 8 mM kg-1 also reduced the concentration and uptake of Cr. Application of sulfate ions augmented the plant growth and counters the negative effect of Cl- ions and Cr. Thus, the study revealed that the addition of S fertilizers could minimize the Cr toxicity in high Cr contaminated soils.


Assuntos
Cloretos/química , Cromo/toxicidade , Poluentes do Solo/toxicidade , Solo/química , Spinacia oleracea/efeitos dos fármacos , Sulfatos/química , Cromo/análise , Monitoramento Ambiental/métodos , Índia , Folhas de Planta/química , Folhas de Planta/efeitos dos fármacos , Folhas de Planta/crescimento & desenvolvimento , Poluentes do Solo/análise , Spinacia oleracea/química , Spinacia oleracea/crescimento & desenvolvimento
7.
Bull Environ Contam Toxicol ; 101(6): 779-786, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30283993

RESUMO

Shortfall of rain and the decreased groundwater level force farmers to use poor quality water for crop production in developing countries. In this study, the quality of agricultural produce and soil health affected by sewage water (Patranala) irrigation was evaluated. Sewage sediment, soil and crop samples were analyzed for physico-chemical properties. Sewage water found to contain trace concentration of heavy metals. However, long-term application of this water for crop production could build up a significant amount of trace metals in both soil and sediments. The DTPA extractable heavy metals ranged Cu 2.7-7.59, Cd 0.04-0.06, Pb 1.29-2.05, Cr 0.01-0.04, Ni 0.24-1.03 and Zn 0.63-2.59 mg kg-1 soil. The heavy metal risk assessment (hazard quotient, HQ) was calculated and found that HQ for these metals in the crops under study was in safe limits. From the study, it is concluded that growing vegetables using sewage water of Patranala is safe, but periodic monitoring to be carried out to avoid food chain contamination.


Assuntos
Produtos Agrícolas/química , Monitoramento Ambiental/métodos , Esgotos/química , Solo/química , Agricultura , Água Subterrânea/química , Índia , Metais Pesados/análise , Medição de Risco , Poluentes do Solo/análise , Verduras/química , Qualidade da Água
8.
Bull Environ Contam Toxicol ; 98(5): 706-711, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-27878320

RESUMO

Soil and groundwater from long-term (>50 years) tannery effluent irrigated areas of Kanpur were analyzed and significant buildup of heavy metals such as Cr, Ni, Cd, Pb, Zn, and As in the range of 252-972, 23-30, 2.3-14.1, 23.7-58.8, 138-338 and 6.8-11 mg kg-1, respectively in soil was found. Few groundwater samples in the effluent irrigated areas also exhibited high Cr concentration above the permissible limit of United States Environmental Protection Agency. The tannery effluents contained 1.53-57.3 ppm Cr, 0-0.12 ppm Ni, 0-0.02 ppm Cd, 0-0.07 ppm Pb, 0-0.48 ppm Zn and 0-0.03 ppm As. The Geo-accumulation index (Igeo) revealed that soil samples were unpolluted to moderately polluted with Cu, Ni, Zn, Pb and As; moderately polluted in case of Cd; and heavily to extremely polluted by Cr.


Assuntos
Água Subterrânea/química , Resíduos Industriais/análise , Metais Pesados/análise , Poluentes do Solo/análise , Poluentes Químicos da Água/análise , Monitoramento Ambiental , Concentração de Íons de Hidrogênio , Índia , Solo/química , Curtume
9.
Environ Monit Assess ; 188(1): 31, 2016 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-26670040

RESUMO

Introduction of heavy metals in the environment by various anthropogenic activities has become a potential treat to life. Among the heavy metals, cadmium (Cd) shows relatively high soil mobility and has high phyto-mammalian toxicity. Integration of soil remediation and ecosystem services, such as carbon sequestration in soils through organic amendments, may provide an attractive land management option for contaminated sites. The application of biochar in agriculture has recently received much attention globally due to its associated multiple benefits, particularly, long-term carbon storage in soil. However, the application of biochar from softwood crop residue for heavy metal immobilization, as an alternative to direct field application, has not received much attention. Hence, a pot experiment was conducted to study the effect of pigeon pea biochar on cadmium mobility in a soil-plant system in cadmium-spiked sandy loam soil. The biochar was prepared from pigeon pea stalk through a slow pyrolysis method at 300 °C. The experiment was designed with three levels of Cd (0, 5, and 10 mg Cd kg(-1) soil) and three levels of biochar (0, 2.5, and 5 g kg(-1) soil) using spinach as a test crop. The results indicate that with increasing levels of applied cadmium at 5 and 10 mg kg(-1) soil, the dry matter yield (DMY) of spinach leaf decreased by 9.84 and 18.29 %, respectively. However, application of biochar (at 2.5 and 5 g kg(-1) soil) significantly increased the dry matter yield of spinach leaf by 5.07 and 15.02 %, respectively, and root by 14.0 and 24.0 %, respectively, over the control. Organic carbon content in the post-harvest soil increased to 34.9 and 60.5 % due to the application of biochar 2.5 and 5 g kg(-1) soil, respectively. Further, there was a reduction in the diethylene triamine pentaacetic acid (DTPA)-extractable cadmium in the soil and in transfer coefficient values (soil to plant), as well as its concentrations in spinach leaf and root, indicating that cadmium mobility was decreased due to biochar application. This study shows that pigeon pea biochar has the potential to increase spinach yield and reduce cadmium mobility in contaminated sandy soil.


Assuntos
Cádmio/análise , Carvão Vegetal , Monitoramento Ambiental , Poluentes do Solo/análise , Solo/química , Spinacia oleracea/química , Agricultura , Animais , Carbono , Ecossistema , Pisum sativum/química , Folhas de Planta/química , Verduras/química
10.
Environ Monit Assess ; 186(4): 2349-56, 2014 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-24271649

RESUMO

This study was carried out in three different cities of western Madhya Pradesh (India) to investigate the effects of long-term irrigation with industrial waste water (IWW), contaminated groundwater (CGW), and untreated municipal sewage water (USW) on soil fertility as well as on wheat crop yield. Irrigation with these three types of polluted water increased organic matter content as well as contents of available P (with IWW and USW only), available K, available S, available Zn, available Cu (IWW only), and available Mn (IWW and CGW only). The magnitude of improvement in soil fertility status was the highest in the case of USW, followed by IWW and finally, by CGW. Concentrations of Na in wheat leaf tissue increased by 198 and 58% whereas concentrations of Ca decreased significantly by 16 and 13% due to the use of IWW and CGW, respectively, resulting in poor Ca nutrition to the crop. Although wheat grain yield increased considerably due to USW, the same recorded significant decreases with IWW and CGW. In spite of the enhancement in the available nutrient status, decrease in wheat grain yield with the use of IWW and CGW could be due to the build-up of salts in the soil and an imbalance in the Na/Ca ratio in wheat crops irrigated with IWW and CGW. The adverse effect on wheat productivity was more pronounced with IWW as compared to CGW.


Assuntos
Irrigação Agrícola/métodos , Monitoramento Ambiental , Poluentes do Solo/análise , Solo/química , Triticum/fisiologia , Eliminação de Resíduos Líquidos/métodos , Índia , Resíduos Industriais , Esgotos , Águas Residuárias/química , Águas Residuárias/estatística & dados numéricos , Poluição da Água/estatística & dados numéricos
11.
Phys Rev Lett ; 111(24): 243201, 2013 Dec 13.
Artigo em Inglês | MEDLINE | ID: mdl-24483657

RESUMO

We present an experimental determination of the 2p3d(1Po)→1s3d(1De) x-ray line emitted from He-like Si, S, and Cl projectile ions, excited in collisions with thin carbon foils, using a high-resolution bent-crystal spectrometer. A good agreement between the observation and state-of-the-art relativistic calculations using the multiconfiguration Dirac-Fock formalism including the Breit interaction and QED effects implies the dominance of fluorescent decay over the autoionization process for the 2p3d(^{1}P^{o}) state of He-like heavy ions. This is the first observation of the fluorescence-active doubly excited states in He-like Si, S, and Cl ions.

12.
Environ Monit Assess ; 185(11): 8815-21, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23604730

RESUMO

The present study compares the distribution and nature of heavy metals in composts from 12 cities of India, prepared from different types of processed urban solid wastes, namely mixed wastes (MWC), partially segregated wastes (PSWC), and segregated bio-wastes (BWC). Compost samples were physically fractionated by wet sieving, followed by extraction of heavy metals by dilute HCl and NaOH. Bigger particles (>0.5 mm) constituted the major fraction in all three types of composts and had a relatively lower concentration of organic matter and heavy metals, the effect being more pronounced in MWC and PSWC in which a significant portion of the heavy metals was distributed in finer size fractions. Cd, Ni, Pb, and Zn were extracted to a greater extent by acid than by alkali, the difference being greater in MWC, which contained a higher amount of mineral matter. In contrast, Cu and Cr were extracted to a greater extent by dilute alkali, particularly from BWC containing a higher amount of organic matter. Water-soluble heavy metals were generally related to the water-soluble C or total C content as well as to pH, rather than to their total contents. This study concludes that wet sieving with dilute acid can effectively reduce heavy metal load in MWC and PSWC.


Assuntos
Metais Pesados/análise , Poluentes do Solo/análise , Resíduos Sólidos/análise , Cidades , Monitoramento Ambiental , Índia , Eliminação de Resíduos/métodos , Resíduos Sólidos/estatística & dados numéricos
13.
PLoS One ; 18(5): e0286223, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37256859

RESUMO

Soil fertility management and crop productivity both are inter-related need extensive attention for sustainability. Industries are being built, which over time produces a lot of effluents containing heavy metal(s), which is then dumped on healthy soils and water bodies. Long-term discharge of lead (Pb)-containing wastewater resulted in significant Pb buildup as well as a decrease in soil biological activity. In this experiment, graded dose of Pb, i.e. 0, 100, 150 and 300 mg/kg and pressmud (PM) (0, 2.5, 5, 10 g/kg) were applied to monitor the Pb toxic effect on soil acid and alkaline phosphatase, dehydrogenase activity. Different treatment combinations were formulated and the experiment was conducted in a completely randomized design (CRD) with three replications. In this experiment, spinach crop was used as a test crop. According to the findings, increased Pb levels in the soil lowered dehydrogenase activity (DHA), acid and alkaline phosphatase. The addition of PM enhanced enzymatic activities by decreasing the labile fraction of Pb in the soil. Incorporation of PM improved the soil enzymatic activities as alkaline phosphatase activity > DHA > acid phosphatase activity in the study. This study suggested that the addition of 10 g/kg PM reduced Pb toxicity (contamination level 300 mg/kg) and improved the soil microbial properties in black soil. These findings are very useful for the remediation of Pb contaminated soil with the help of PM, particularly in peri-urban Pb effluent irrigated areas.


Assuntos
Metais Pesados , Saccharum , Poluentes do Solo , Fosfatase Alcalina , Saccharum/metabolismo , Resíduos Industriais , Chumbo/toxicidade , Poluentes do Solo/análise , Metais Pesados/análise , Solo , Oxirredutases
14.
Environ Monit Assess ; 161(1-4): 403-12, 2010 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-19219646

RESUMO

In the peri-urban areas of central India, sewage water is a valuable resource for agricultural production. In this study, impact of domestic sewage water irrigation for 5 years on Vertisol with no previous history of sewage irrigation was investigated in an ongoing field experiment at Bhopal (India) under subtropical monsoon type climate. The wheat (Triticum aestivum) crop was grown during post-rainy winter season with 30 cm of irrigation (groundwater or sewage water) and four nutrient treatments (T(1), 0; T(2), 100%; T(3), 50%; and T(4), 50% of general recommended doses of NPK + FYM at 10 Mg/ha). Results showed that sewage irrigation of about 150 cm over a period of 5 years resulted significant increases in salinity as well as available fractions of N, P, K, and micronutrients, viz., Zn, Fe, and Mn in soils. Carbon and phosphorus applied through sewage water were accumulated more in subsoil layer compared to topmost plough layer. Soil microbiological activity, as indicated by soil respiration, microbial biomass C, as well as dehydrogenase enzyme activity was higher in sewage water-irrigated soils. There was also significant increase in fungal and actinomycetes as well as total coliform population in such soils. Nutrients supplied through sewage water were not able to raise the productivity of wheat to the level that obtained through fertilizers at the recommended level which indicated that additional nutrients through fertilizers are required to obtain higher productivity of wheat under sewage farming. Protein and Zn content in wheat grains were more when the crop was grown with sewage irrigation. Overall results show that except for increase in coliform population, short duration (5 years) of municipal sewage water irrigation did not have any appreciable harmful effect on soil quality as well as crop productivity; rather, it proved beneficial in improving soil fertility, wheat productivity, and produce quality.


Assuntos
Esgotos , Microbiologia do Solo , Solo/análise , Triticum/crescimento & desenvolvimento , Actinobacteria/isolamento & purificação , Enterobacteriaceae/isolamento & purificação , Índia , Ferro/análise , Manganês/análise , Nitrogênio/análise , Fósforo/análise , Potássio/análise , Salinidade , Poluentes do Solo/análise , Zinco/análise
15.
J Med Chem ; 34(5): 1728-31, 1991 May.
Artigo em Inglês | MEDLINE | ID: mdl-2033595

RESUMO

The synthesis and pharmacological characterization of a series of N-substituted 3-(4-fluorophenyl)tropane derivatives is reported. The compounds displayed binding characteristics that paralleled those of cocaine, and several had substantially higher affinity at cocaine recognition sites. Conjugate addition of 4-fluorophenyl magnesium bromide to anhydroecgonine methyl ester gave 2 beta-(carbomethoxy)-3 beta-(4-fluorophenyl)tropane (4a, designated CFT, also known as WIN 35,428) after flash chromatography. N demethylation of 4a was effected by Zn/HOAc reduction of the corresponding 2,2,2-trichloroethyl carbamate to give 2 beta-carbomethoxy-3 beta-(4-fluorophenyl)nortropane (5), which was alkylated with allyl bromide to afford the N-allyl analogue, 6. The N-propyl analogue, 7, was prepared by catalytic reduction (Pd/C) of 6. The most potent analogue, 4a, was tritiated at a specific activity of 81.3 Ci/mmol. [3H]4a bound rapidly and reversibly to caudate putamen membranes; the two-component binding curve typical of cocaine analogues was observed. Equilibrium was achieved within 2 h and was stable for at least 4 h. High- and low-affinity Kd values observed for [3H]4a (4.7 and 60 nM, respectively) were more than 4 times lower than those for [3H]cocaine, and the density of binding sites (Bmax = 50 pmol/g, high, and 290 pmol/g, low) for the two drugs were comparable. Nonspecific binding of [3H]4a was 5-10% of total binding.


Assuntos
Proteínas de Transporte , Receptores de Droga/efeitos dos fármacos , Tropanos/síntese química , Animais , Sítios de Ligação , Fenômenos Químicos , Química , Cocaína/análogos & derivados , Cocaína/metabolismo , Feminino , Macaca fascicularis , Masculino , Receptores de Droga/metabolismo , Relação Estrutura-Atividade , Trítio , Tropanos/metabolismo , Tropanos/farmacologia
16.
J Med Chem ; 33(5): 1437-43, 1990 May.
Artigo em Inglês | MEDLINE | ID: mdl-2158563

RESUMO

The synthesis of a variety of novel 10-substituted cannabidiol (CBD) and 11- or 12-substituted delta 8-tetrahydrocannabinol (delta 8-THC) analogues containing amino, alkylamino, azido, or a N,N-bis(2-chloroethyl)amino functional group is described, as well as their pharmacological evaluation in mice. These analogues, which possess only a portion of the full pharmacological spectrum of activity of delta 9-THC, indicate that cannabinoid-mediated reduction of spontaneous locomotor activity, hypothermia, antinociception, and/or catalepsy need not be produced simultaneously, possibly suggesting the existence of more than one mechanism of action. The 10-substituted CBD analogues 3, 4, and 5 with an ethylamino, propylamino, or azido functional group, respectively, proved to be largely inactive, except for the production of central nervous system (CNS) depression concomitant with toxicity. Toxicity and CNS depression may be related phenomena in these nitrogenous compounds since 12-amino and 12-ethylamino analogues (8 and 11) of delta 8-THC also proved to be very toxic. Antinociceptive and hypothermic responses (without reduction of motor activity) were observed at a dose of 10 mg/kg of the 11-ethylamino analogue (9) of delta 8-THC, while a dose of 50 mg/kg of the nitrogen mustard 11-[N,N-bis(2-chloroethyl)amino]-delta 8-THC (12) was necessary to produce any observable pharmacological effect. When selected analogues were evaluated for antagonistic properties, they failed to attenuate the effects of delta 9-THC. Some nitrogen mustard analogues were capable of producing minimal pharmacological effects after either peripheral or direct CNS administration; however, these analogues also failed to attenuate the effects of delta 9-THC either immediately after administration or 24-48 h later.


Assuntos
Analgésicos/síntese química , Canabidiol/análogos & derivados , Dronabinol/análogos & derivados , Animais , Canabidiol/toxicidade , Canabinoides , Fenômenos Químicos , Química , Relação Dose-Resposta a Droga , Dronabinol/toxicidade , Dose Letal Mediana , Masculino , Camundongos , Camundongos Endogâmicos ICR , Atividade Motora/efeitos dos fármacos , Respiração/efeitos dos fármacos , Relação Estrutura-Atividade
17.
J Med Chem ; 43(21): 4005-16, 2000 Oct 19.
Artigo em Inglês | MEDLINE | ID: mdl-11052806

RESUMO

Despite its widespread use, diclofenac has gastrointestinal liabilities common to nonsteroidal antiinflammatory drugs (NSAIDs) that might be reduced by concomitant administration of a gastrointestinal cytoprotectant such as nitric oxide (NO). A series of novel diclofenac esters containing a nitrosothiol (-S-NO) moiety as a NO donor functionality has been synthesized and evaluated in vivo for bioavailability, pharmacological activity, and gastric irritation. All S-NO-diclofenac derivatives acted as orally bioavailable prodrugs, producing significant levels of diclofenac in plasma within 15 min after oral administration to mice. At equimolar oral doses, S-NO-diclofenac derivatives (20a-21b) displayed rat antiinflammatory and analgesic activities comparable to those of diclofenac in the carrageenan-induced paw edema test and the mouse phenylbenzoquinone-induced writhing test, respectively. All tested S-NO-diclofenac derivatives (20a-21b) were gastric-sparing in that they elicited markedly fewer stomach lesions as compared to the stomach lesions caused by a high equimolar dose of diclofenac in the rat. Nitrosothiol esters of diclofenac comprise a novel class of NO-donating compounds having therapeutic potential as nonsteroidal antiinflammatory agents with an enhanced gastric safety profile.


Assuntos
Anti-Inflamatórios não Esteroides/síntese química , Diclofenaco/síntese química , Compostos Nitrosos/síntese química , Pró-Fármacos/síntese química , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacocinética , Anti-Inflamatórios não Esteroides/farmacologia , Disponibilidade Biológica , Diclofenaco/química , Diclofenaco/farmacocinética , Diclofenaco/farmacologia , Masculino , Camundongos , Compostos Nitrosos/química , Compostos Nitrosos/farmacocinética , Compostos Nitrosos/farmacologia , Pró-Fármacos/química , Pró-Fármacos/farmacocinética , Pró-Fármacos/farmacologia , Ratos , Ratos Sprague-Dawley , Estômago/patologia , Relação Estrutura-Atividade
18.
Br J Pharmacol ; 83(2): 347-55, 1984 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-6487900

RESUMO

Nicotine and dimethyl-phenylpiperazinium (DMPP) increased intravesicular pressure and then transiently depressed the spontaneous activity of the urinary bladder in chloralose anaesthetized cats. Adrenaline (5-10 micrograms kg-1), noradrenaline (5-20 micrograms kg-1) and isoprenaline (40-50 micrograms kg-1) which depressed spontaneous urinary bladder activity, were antagonized by the beta-receptor blocking agent propranolol (1 mg kg-1). Phenylephrine (10-30 micrograms kg-1) was ineffective on the urinary bladder though it increased the systemic blood pressure. This latter effect was blocked by the alpha-receptor blocking agent phentolamine (2 mg kg-1). Acetylcholine (2-8 micrograms kg-1) caused a marked fall in systemic blood pressure, which was potentiated by physostigmine, but failed to produce any response on the intravesicular pressure even after physostigmine (50-100 micrograms kg-1) treatment. ATP (2 mg kg-1) produced an increase in intravesicular pressure accompanied by a fall in systemic blood pressure. The increased intravesicular pressure was antagonized by quinidine (20 mg kg-1); however, the fall in blood pressure remained unaltered. The increased intravesicular pressure induced by nicotine (20-40 micrograms kg-1) or DMPP (50-100 micrograms kg-1) was not affected by phentolamine (2 mg kg-1), propranolol (1 mg kg-1) or guanethidine (15-20 mg kg-1). Physostigmine (50-100 micrograms kg-1), hemicholinium 3 (2 mg kg-1) or atropine (1 mg kg-1) were also unable to affect the response to nicotine. Hexamethonium (1 mg kg-1), reduced the amplitude of spontaneous bladder contractions and quinidine (20 mg kg-1) abolished the effect of nicotine. 7 Bilateral sectioning of the cervical sympathetic or hypogastric nerves did not alter the effect of nicotine or DMPP. Higher spinal cord transection (Cl-C2) blocked the spontaneous, as well as the nicotine- and DMPP-induced, contractions of the bladder. 8 It is concluded that the increase in intravesicular pressure induced by nicotine is atropineresistant and is not mediated either through adrenergic or cholinergic mechanisms. It is probable that a purinergic mechanism is involved, via the activation of P2-receptors present in the urinary bladder.


Assuntos
Músculo Liso/efeitos dos fármacos , Nicotina/farmacologia , Bexiga Urinária/efeitos dos fármacos , Trifosfato de Adenosina/farmacologia , Adrenalectomia , Animais , Atropina/farmacologia , Sistema Nervoso Autônomo/efeitos dos fármacos , Pressão Sanguínea/efeitos dos fármacos , Gatos , Epinefrina/farmacologia , Guanetidina/farmacologia , Hemicolínio 3/farmacologia , Compostos de Hexametônio/farmacologia , Isoproterenol/farmacologia , Contração Muscular/efeitos dos fármacos , Denervação Muscular , Norepinefrina/farmacologia , Fentolamina/farmacologia , Fenilefrina/farmacologia , Fisostigmina/farmacologia , Propranolol/farmacologia , Quinidina/farmacologia , Medula Espinal/fisiologia
19.
Br J Pharmacol ; 97(4): 1279-91, 1989 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-2477106

RESUMO

1. Post-rest inotropy in canine ventricular myocardium has proved a useful indicator of sarcoplasmic reticular calcium release. This phenomenon is converted to rest depression by the calcium channel activator (agonist), Bay K 8644 as well as other chemically diverse agents such as caffeine and ryanodine. 2. Rapid cooling contractures and post-rest contraction amplitude were used as independent measures of sarcoplasmic reticular calcium content and release. Simultaneous recordings of transmembrane action potentials and their accompanying contractions were obtained to determine the association between electrophysiological and mechanical events. The present study was designed to elucidate the mechanism by which Bay K 8644, caffeine and ryanodine alter force production after variable periods of rest. 3. Bay K 8644 (1 microM) increased steady state contraction in response to a constant train of stimulation, caused rest-depression after 2 and 8 min rest, prolonged action potential duration and increased action potential plateau amplitude. Augmented steady state tension was not accompanied by any change in time to peak tension or rapid cooling contracture amplitude. However, the post-rest rapid cooling contracture was greatly diminished compared to that observed prior to Bay K 8644 treatment. 4. Caffeine (3 and 5 mM) caused rest-depression with an increase in steady state contraction amplitude. Along with this there was a slight decrease in action potential duration and plateau amplitude and an increase in time to peak tension. The rapid cooling contractures were virtually abolished at all conditioning intervals. The effect of caffeine on twitch tension and cooling contracture is consistent with the ability of this compound to inhibit calcium sequestration by the sarcoplasmic reticulum. 5. A combination of Bay K 8644 and caffeine caused significantly less rest-depression than that seen with Bay K 8644 alone. The augmented twitch tension was accompanied by a long time to peak tension and action potential duration. However, there was no increase in the amplitude of the rapid cooling contracture, either after a regular train of stimulation or after rest, compared to that seen after Bay K 8644. 6. Ryanodine (10 nM), produced rest-depression, reduced steady state twitch tension and augmented the rest-depression produced by Bay K 8644. The steady state rapid cooling contracture remained unchanged when both agents were present simultaneously, while the post-rest rapid cooling contracture was significantly depressed compared to that observed with Bay K 8644 alone. 7. Bay K 8644 and ryanodine appear to have similar actions with respect to promoting diastolic loss of calcium from the sarcoplasmic reticulum. Although caffeine also decreases post-rest potentiation, it antagonizes rest-depression caused by Bay K 8644. The data from these experiments suggest that this reversal is a result of depressed intracellular calcium buffering and enhanced myofilament sensitivity produced by caffeine in the presence of increased transmembrane calcium influx promoted by Bay K 8644.


Assuntos
Éster Metílico do Ácido 3-Piridinacarboxílico, 1,4-Di-Hidro-2,6-Dimetil-5-Nitro-4-(2-(Trifluormetil)fenil)/farmacologia , Alcaloides/farmacologia , Cafeína/farmacologia , Coração/efeitos dos fármacos , Contração Miocárdica/efeitos dos fármacos , Rianodina/farmacologia , Potenciais de Ação/efeitos dos fármacos , Animais , Cálcio/metabolismo , Temperatura Baixa , Cães , Interações Medicamentosas , Feminino , Técnicas In Vitro , Masculino , Potenciais da Membrana/efeitos dos fármacos
20.
Naunyn Schmiedebergs Arch Pharmacol ; 335(1): 86-90, 1987 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-2437461

RESUMO

The mechanism of the positive inotropic effect produced by nicotine (6.2 X 10(-5) mol/l to 4.9 X 10(-4) mol/l) on electrically driven toad ventricles was investigated. The response to nicotine was not affected by 6-hydroxydopamine pretreatment, bretylium (2.4 X 10(-4) mol/l) exposure or tyramine tachyphylaxis. Following desensitisation by isoprenaline (4.2 X 10(-6) mol/l) of the beta-adrenoceptor in the ventricles, the response to nicotine was no affected. However, the response was antagonised by ethylene diamine tetraethyl acetate (2.3 X 10(-4) mol/l), verapamil (0.4 X 10(-5) mol/l) or calcium-free Ringer. Nicotine prolonged the action potential duration and enhanced the force of contraction. Nicotine induced slow action potentials in partially depolarized (in high potassium solution) ventricles and this was antagonised by verapamil (0.4 X 10(-5) mol/l). These results suggest that the effects of nicotine are mediated by a direct interaction with the Ca2+ channels at the cell surface.


Assuntos
Canais Iônicos/fisiologia , Contração Miocárdica/efeitos dos fármacos , Nicotina/farmacologia , Potenciais de Ação/efeitos dos fármacos , Animais , Compostos de Bretílio/farmacologia , Bufonidae , Bloqueadores dos Canais de Cálcio/farmacologia , Hidroxidopaminas/farmacologia , Técnicas In Vitro , Isoproterenol/farmacologia , Oxidopamina , Tiramina/farmacologia
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