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Our review focused on nanomaterials-based toxicity evaluation and its exposure to the human and aquatic animals when it was leached and contaminated in the environment. Ecotoxicological assessment and its mechanism mainly affect the skin covering layers and its preventive barriers that protect the foreign particles' skin. Nanoscale materials are essential in the medical field, especially in biomedical and commercial applications such as nanomedicine and drug delivery, mainly in therapeutic treatments. However, various commercial formulations of pharmaceutical drugs are manufactured through a series of clinical trials. The role of such drugs and their metabolites has not met the requirement of an individual's need at the early stage of the treatments except few drugs and medicines with minimal or no side effects. Therefore, biology and medicines are taken up the advantages of nano scaled drugs and formulations for the treatment of various diseases. The present study identifies and analyses the different nanoparticles and their chemical components on the skin and their effects due to penetration. There are advantageous factors available to facilitate positive and negative contact between dermal layers. It creates a new agenda for an established application that is mainly based on skin diseases.
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DNA helicases are motor proteins that play an essential role in nucleic acid metabolism, by providing a duplex-unwinding function. To improve the drought and salinity tolerance of sugarcane, a DEAD-box helicase gene isolated from pea with a constitutive promoter, Port Ubi 2.3 was transformed into the commercial sugarcane variety Co 86032 through Agrobacterium-mediated transformation, and the transgenics were screened for tolerance to soil moisture stress and salinity. The transgene integration was confirmed through polymerase chain reaction, and the V 0 transgenic events showed significantly higher cell membrane thermostability under normal irrigated conditions. The V 1 transgenic events were screened for tolerance to soil moisture stress and exhibited significantly higher cell membrane thermostability, transgene expression, relative water content, gas exchange parameters, chlorophyll content, and photosynthetic efficiency under soil moisture stress compared to wild-type (WT). The overexpression of PDH45 transgenic sugarcane also led to the upregulation of DREB2-induced downstream stress-related genes. The transgenic events demonstrated higher germination ability and better chlorophyll retention than WT under salinity stress. Our results suggest the possibility for development of increased abiotic stress tolerant sugarcane cultivars through overexpression of PDH45 gene. Perhaps this is the first report, which provides evidence for increased drought and salinity tolerance in sugarcane through overexpression of PDH45.
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ADN Helicasas/metabolismo , Pisum sativum/enzimología , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Saccharum/fisiología , Membrana Celular/química , ADN Helicasas/genética , Sequías , Regulación de la Expresión Génica de las Plantas , Pisum sativum/genética , Plantas Modificadas Genéticamente/metabolismo , Saccharum/genética , Salinidad , Estrés Fisiológico , TemperaturaRESUMEN
Heat shock proteins (HSPs) have a major role in stress tolerance mechanisms in plants. Our studies have shown that the expression of HSP70 is enhanced under water stress in Erianthus arundinaceus. In this paper, we evaluate the effects of overexpression of EaHSP70 driven by Port Ubi 2.3 promoter in sugarcane. The transgenic events exhibit significantly higher gene expression, cell membrane thermostability, relative water content, gas exchange parameters, chlorophyll content and photosynthetic efficiency. The overexpression of EaHSP70 transgenic sugarcane led to the upregulation of stress-related genes. The transformed sugarcane plants had better chlorophyll retention and higher germination ability than control plants under salinity stress. Our results suggest that EaHSP70 plays an important role in sugarcane acclimation to drought and salinity stresses and its potential for genetic engineering of sugarcane for drought and salt tolerance.
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Proteínas HSP70 de Choque Térmico/fisiología , Saccharum/genética , Tolerancia a la Sal/genética , Agua/metabolismo , Sequías , Proteínas HSP70 de Choque Térmico/genética , Proteínas HSP70 de Choque Térmico/metabolismo , Plantas Modificadas Genéticamente/metabolismo , Plantas Modificadas Genéticamente/fisiología , Saccharum/metabolismo , Saccharum/fisiologíaRESUMEN
KEY MESSAGE: EaDREB2 overexpressed in sugarcane enhanced tolerance to drought and salinity. When co-transformed with plant DNA helicase gene, DREB2 showed greater level of salinity tolerance than in single-gene transgenics. Drought is one of the most challenging agricultural issues limiting sustainable sugarcane production and can potentially cause up to 50 % yield loss. DREB proteins play a vital regulatory role in abiotic stress tolerance in plants. We previously reported that expression of EaDREB2 is enhanced by drought stress in Erianthus arundinaceus. In this study, we have isolated the DREB2 gene from E. arundinaceus, transformed one of the most popular sugarcane variety Co 86032 in tropical India with EaDREB2 through Agrobacterium-mediated transformation, pyramided the EaDREB2 gene with the gene coding for PDH45 driven by Port Ubi 2.3 promoter through particle bombardment and evaluated the V1 transgenics for soil deficit moisture and salinity stresses. Soil moisture stress was imposed at the tillering phase by withholding irrigation. Physiological, molecular and morphological parameters were used to assess drought tolerance. Salinity tolerance was assessed through leaf disc senescence and bud sprout assays under salinity stress. Our results indicate that overexpression of EaDREB2 in sugarcane enhances drought and salinity tolerance to a greater extent than the untransformed control plants. This is the first report of the co-transformation of EaDREB2 and PDH45 which shows higher salinity tolerance but lower drought tolerance than EaDREB2 alone. The present study seems to suggest that, for combining drought and salinity tolerance together, co-transformation is a better approach.
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ADN Helicasas/genética , Pisum sativum/enzimología , Saccharum/fisiología , Factores de Transcripción/genética , Secuencia de Bases , Clorofila/metabolismo , ADN Helicasas/metabolismo , Expresión Génica , Regulación de la Expresión Génica de las Plantas , Datos de Secuencia Molecular , Pisum sativum/genética , Hojas de la Planta/efectos de los fármacos , Hojas de la Planta/genética , Hojas de la Planta/fisiología , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Transpiración de Plantas/fisiología , Plantas Modificadas Genéticamente , Regiones Promotoras Genéticas/genética , Saccharum/efectos de los fármacos , Saccharum/genética , Salinidad , Tolerancia a la Sal , Análisis de Secuencia de ADN , Cloruro de Sodio/farmacología , Estrés Fisiológico , Factores de Transcripción/metabolismoRESUMEN
Let f(z) = z + ∑(n=2)(∞) (a)n(z) (n) be analytic in the unit disk with the second coefficient a2 satisfying |a2| = 2b, 0 ≤ b ≤ 1. Sharp radius of Janowski starlikeness is obtained for functions f whose nth coefficient satisfies |a(n)| ≤ cn + d (c, d ≥ 0) or |a(n)| ≤ c/n (c > 0 and n ≥ 3). Other radius constants are also obtained for these functions, and connections with earlier results are made.
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Inhibition of human immunodeficiency virus 1 (HIV-1) protease is an important strategy for the treatment of HIV and acquired immune deficiency syndrome (AIDS). Therefore, HIV-1 protease inhibitory activity of dihydropyranone derivatives has been analyzed with different physico-chemical parameters. In the present work, QSAR studies were performed on a series of 4-hydroxy-5,6-dihydropyran-2-ones to explore the physico-chemical parameters responsible for their HIV-1 protease inhibitory activity. Physico-chemical parameters were calculated using WIN CAChe 6.1. Stepwise multiple linear regression analysis was performed to derive QSAR models which were further evaluated for statistical significance and predictive power by internal and external validation. The selected best QSAR model was having correlation coefficient (R) = 0.875 and cross-validated squared correlation coefficient (Q²) = 0.707. The developed significant QSAR model indicates that hydrophobicity of whole molecule and the substituent present at sixth position of dihydropyranones play an important role in the HIV-1 protease inhibitory activities of 4-hydroxy-5,6-dihydropyran-2-ones.
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Activación Enzimática/efectos de los fármacos , Proteasa del VIH/metabolismo , VIH-1 , Inhibidores de Proteasas/farmacología , Pironas/farmacología , Humanos , Concentración 50 Inhibidora , Estructura Molecular , Inhibidores de Proteasas/síntesis química , Inhibidores de Proteasas/química , Pironas/síntesis química , Pironas/química , Relación Estructura-Actividad CuantitativaRESUMEN
The stability of embedded Indium (In) nanoclusters (NCs) in silica under thermal annealing and ion irradiation was investigated. The In NCs were prepared by implantation of 890 keV indium ions in silica matrix at room temperature. Post implantation annealing resulted in the shifting of the size distribution to higher side. On the other hand 140 keV Nitrogen ion irradiation at elevated temperature resulted in the reduction of NCs size, with significant narrowing of the size distribution. The paper discusses the results of the study in the light of the models pertaining to the stability of NCs under ion irradiation conditions.
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HIV-1 (human immunodeficiency virus type-1) is the pathogenic retrovirus and causative agent of AIDS. HIV-1 RT is one of the key enzymes in the duplication of HIV-1. Inhibitors of HIV-1 RT are classified as NNRTIs and NRTIs. NNRTIs bind to a region that is not associated with the active site of the enzyme. Within the NNRTIs category, there is a set of inhibitors commonly referred to as thiazolidinone derivatives. The present 3D-QSAR study attempts to explore the structural requirements of thiazolidinone derivatives for anti-HIV activity. Based on the structures and biodata of previous thiazolidinone analogs, 3D-QSAR studies have been performed with a training set consisting of 96 molecules, which resulted in two reliable computational models, CoMFA and CoMSIA with r(2) values of 0.931 and 0.972, standard error of estimation (SEE) of 0.173 and 0.089, and q(2) values of 0.663 and 0.784, respectively, with the number of partial least-squares (PLS) components being six. It is shown that the steric and electrostatic properties predicted by CoMFA contours and the hydrogen bond acceptor, hydrogen bond donor, and hydrophobic properties predicted by CoMSIA contours are related to anti-HIV activity. The predictive ability of the resultant model was evaluated using a test set comprising of 17 molecules and the predicted r(2) values of CoMFA and CoMSIA models were 0.861 and 0.958, respectively. These models are more significant guide to trace the features that really matter especially with respect to the design of novel compounds.
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Fármacos Anti-VIH/farmacología , Inhibidores de la Transcriptasa Inversa/farmacología , Tiazolidinas/farmacología , Fármacos Anti-VIH/química , Modelos Moleculares , Estructura Molecular , Relación Estructura-Actividad Cuantitativa , Análisis de Regresión , Inhibidores de la Transcriptasa Inversa/química , Tiazolidinas/químicaRESUMEN
Neurodegenerative disorders are consequences of progressive and irreversible loss of neurons due to unwanted apoptosis which involves caspases, a group of cysteine proteases that cleave other proteins and inactivate them. Among several different groups of caspase enzymes, caspases-3 plays a key role in apoptosis and are a therapeutic target for their inhibition. In pursuit of better caspase-3 inhibitors, a quantitative structure-activity relationship (QSAR) analysis was performed on a series of 1,3-dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c] quinolines as caspase-3 inhibitors using WIN CAChe 6.1 and Medicinal Chemistry Regression Machine. The best QSAR model was selected and validated by internal and external validation method. The values of statistical data are r = 0.955, F = 72.95, SEE = 0.397, q(2) = 0.885, S(PRESS) = 0.44. The present study reveals that when the conformational minimum energy is increased, and lowest unoccupied molecular orbital energy and highest occupied molecular orbital energy are decreased the biological activity can be increased. On the basis of a selected QSAR model, we designed a new series of 1,3-dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines compounds, calculated their caspases inhibitory activity and found that the designed compounds were more potent than the existing compounds.
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Inhibidores de Caspasas , Relación Estructura-Actividad Cuantitativa , Quinolinas/farmacología , Diseño de Fármacos , Humanos , Quinolinas/químicaRESUMEN
Nanocrystals (approximately 5 nm) of the semiconducting wide band gap material beta-In2S3 obtained by chemical synthesis through a hydrothermal route were characterized for phase and compositional purity. These nanoparticles exhibited quantum confinement characteristics as revealed by a blue-shifted optical absorption. These quantum dots of beta-In2S3 were electrically driven from a monodisperse colloidal suspension on to conducting glass substrates by Electophoretic Deposition (EPD) technique and nanostructural thin films were obtained. The crystalline and morphological structures of these deposits were investigated by X-ray diffraction and nanoscopic techniques. We report here that certain interesting nanostructural morphologies were observed in the two-dimensional quantum dot assemblies of beta-In2S3. The effect of the controlling parameters on the cluster growth and deposit integrity was also systematically studied through a series of experiments and the results are reported here.
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Indio/química , Nanoestructuras/química , Puntos Cuánticos , Cristalización , Difracción de Rayos X/métodosRESUMEN
A new, simple, sensitive, precise and robust high-performance thin layer chromatographic (HPTLC) method was developed for the estimation of conessine in herbal extracts and pharmaceutical dosage forms. Analysis of conessine was performed on TLC aluminium plates pre-coated with silica gel 60F-254 as stationary phase. Linear ascending development was carried out in twin trough glass chamber saturated with mobile phase consisting of toluene-ethylacetate-diethyl amine (6.5:2.5:1, v/v/v) at room temperature (25+/-2 degrees C). After derivatized the plate with modified Dragendroff's reagent, Camag TLC scanner III was used for spectrodensitometric scanning and analysis of the plate in absorbance mode at 520 nm. The system was found to give compact spots for conessine (Rf value of 0.82). The data for calibration plots showed good linear relationship with r2=0.9998 in the concentration range of 1-10 microg with respect to peak area. The present method was validated for precision and recovery. The limits of detection and quantification were determined. Statistical analysis of the data showed that the method is reproducible and selective for estimation of conessine.
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Alcaloides/análisis , Cromatografía en Capa Delgada/métodos , Medicina de Hierbas , Preparaciones Farmacéuticas/química , Calibración , Formas de Dosificación , Reproducibilidad de los Resultados , Sensibilidad y EspecificidadRESUMEN
The present study was aimed to replace the alum type adjuvant for hepatitis B vaccine. The hepatitis B vaccine was encapsulated in poly (DL-lactide-co-glycolide) microspheres by solvent evaporation technique. The formulated microspheres were characterized in terms of morphology, particle size analysis, in vitro release study and in vivo immune response in male Wistar rats. The FT IR spectrum illustrates the characteristics bands of poly (DL-lactide-co-glycolide) microspheres and hepatitis B vaccine at 1750 cm(-1) and 1650 cm(-1), respectively. The hepatitis B vaccine loaded poly (DL-lactide-co-glycolide) microspheres were able to release antigens till day 42. Significant enhancement of specific antibodies to HBsAg was produced till day 90 after a single administration of HBsAg encapsulated poly (DL-lactide-co-glycolide) microspheres. However, the conventional alum adsorbed hepatitis B vaccine was not found to produce any significant specific antibody levels till day 90 after a single dose. The results showed that poly (DL-lactide-co-glycolide) microspheres show potential as an adjuvant for hepatitis B vaccine.
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Purpose: To evaluate Plumeria alba leaves for antitumor activity against Ehrlich ascites carcinoma (EAC) and Dalton lymphoma ascites (DLA) bearing Swiss albino mice. Method: The antitumour activity of the methanolic extract of Plumeria alba leaves (MPA) was evaluated against EAC and DLA using in-vitro cytotoxic and mean survival time; a decrease in the tumour volume and viable cell count in the DLA tumour hosts. The animal was observed for improvement in the haematological parameters (e.g.; heamoglobin content; red and white blood cells count; and differential cell count) following MPA treatment of the tumour bearing mice. Results: MPA was found to be cytotoxic in the in-vitro model. Intraperitoneal administration of MPA increased the survival time; dead cell count haematological parameters and solid tumour mass was also significantly reduced. Conclusion: MPA possesses significant antitumour activity
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Antineoplásicos , Apocynaceae , Ascitis , Metanol , RatonesRESUMEN
Semiconductor nanoparticles of Indium Sulphide were synthesized by a hydrothermal method using InCl3 and Na2S. Powder X-ray Diffraction analysis confirmed that the product obtained was nanocrystals of single-phase beta-In2S3. The crystallite size distribution was obtained from the diffraction profile and the average size was approximately 5 nm. The compositional analyses performed on the as-prepared powder showed that the material was devoid of any impurity with an In:S ratio very close to 2:3. A colloid of very fine In2S3 particles was obtained from the as-prepared powder by suspending them in acetonitrile. The optical absorption of this colloid showed evidence of strong quantum confinement of excitons and as a result the particles yielded intense photoluminescence in the violet-blue region. These colloidal particles were then electrophoretically driven on to a transparent conducting substrate to assemble into a nanostructure. A Grazing Incidence X-ray Diffraction analysis of the deposited layer revealed that the preferred orientation noticed in the native powder was removed in the deposit. The surface morphology of the deposit studied using SEM and AFM displayed an inherent ordering behaviour in the clusters organized into a two-dimensional film. The locus of the cluster lines tend to form closed circles, at the nanoscopic as well as microscopic scales, indicative of certain strong neighborhood correlations. Such structures may be expected to exhibit novel correlated properties also.
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The practice of traditional medicine for the control of fertility in Nilgris is based on the use of plant medicine for many years. The aim of the present study is to evaluate the effect of hydroalcoholic extract of stem bark of Ailanthus excelsa Roxb (Simaroubaceae) (HEA) has been studied in rats to explore its antifertility activity. A strong antiimplantation (72%) and abortifacient activity (56%) was observed at the tested dose levels (200 and 400mg/kg, p.o.). The extract shows further more, significant (P<0.05) increase in uterine weight in immature ovariectomised rats. Simultaneous administration of extract with ethinyl estradiol cause significant antiestrogenic activity. All these observations suggest that hydroalcoholic extract of Ailanthus excelsa has antifertility effect.
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Abortivos/farmacología , Ailanthus , Anticonceptivos/farmacología , Fertilidad/efectos de los fármacos , Animales , Relación Dosis-Respuesta a Droga , Implantación del Embrión/efectos de los fármacos , Moduladores de los Receptores de Estrógeno/farmacología , Estrógenos/farmacología , Etinilestradiol/farmacología , Femenino , India , Masculino , Medicina Tradicional de Asia Oriental , Tamaño de los Órganos/efectos de los fármacos , Ovariectomía , Corteza de la Planta , Extractos Vegetales , Ratas , Ratas Wistar , Útero/efectos de los fármacosRESUMEN
HIV-1 (Human Immunodeficiency Virus Type-1) is the pathogenic retrovirus and causative agent of AIDS. HIV-1 RT is one of the key enzymes in the duplication of HIV-1. Inhibitors of HIV-1 RT are classified as NNRTIs and NRTIs. NNRTIs bind in a region not associated with the active site of the enzyme. Within the NNRTIs category, there is a set of inhibitors commonly referred to as phenyl ethyl thiazolyl thiourea (PETT) derivatives. The present 3D QSAR study attempts to explore the structural requirements of phenyl ethyl thiazolyl thiourea (PETT) derivatives for anti-HIV activity. Based on the structures and biodata of previous PETT analogs, 3D-QSAR (CoMFA) study has been performed with a training set consisting of 60 molecules, which resulted in a reliable computational model with q(2)=0.657, S(PRESS)=0.957, r(2)=0.938, and standard error of estimation (SEE)=0.270 with the number of partial least square (PLS) components being 5. It is shown that the steric and electrostatic properties predicted by CoMFA contours can be related to the anti-HIV activity. The predictive ability of the resultant model was evaluated using a test set comprised of 11 molecules and the predicted r(2)=0.893. This model is a more significant guide to trace the features that really matter especially with respect to the design of novel compounds.
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Fármacos Anti-VIH/química , Diseño de Fármacos , Relación Estructura-Actividad Cuantitativa , Tiazoles/química , Triazoles/química , Fármacos Anti-VIH/farmacología , Biología Computacional , Humanos , Modelos Moleculares , Inhibidores de la Transcriptasa Inversa/química , Inhibidores de la Transcriptasa Inversa/farmacología , Electricidad Estática , Tiazoles/farmacología , Tiourea/análogos & derivados , Triazoles/farmacologíaRESUMEN
Two simple and sensitive spectrophotometric methods (A and B) for the determination of raloxifene hydrochloride in bulk samples and pharmaceutical formulations are described. Method A is based on the oxidation of the drug with ferric chloride and coupling with potassium ferric cyanide. Method B is based on reduction of the drug with Fehling's reagent. Bluish green color formed in method A absorbs at 735 nm and brown color produced in method B absorbs at 430 nm.
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Clorhidrato de Raloxifeno/análisis , Moduladores Selectivos de los Receptores de Estrógeno/análisis , Química Farmacéutica , Cloruros , Compuestos Férricos , Indicadores y Reactivos , Oxidación-Reducción , Estándares de Referencia , Soluciones , Espectrofotometría Ultravioleta , ComprimidosRESUMEN
The cytoskeletal changes that alter cellular morphogenesis and motility depend upon a complex interplay among molecules that regulate actin, myosin, and other cytoskeletal components. The Rho family of GTP binding proteins are important upstream mediators of cytoskeletal organization. Gem and Rad are members of another family of small GTP binding proteins (the Rad, Gem, and Kir family) for which biochemical functions have been mostly unknown. Here we show that Gem and Rad interface with the Rho pathway through association with the Rho effectors, Rho kinase (ROK) alpha and beta. Gem binds ROKbeta independently of RhoA in the ROKbeta coiled-coil region adjacent to the Rho binding domain. Expression of Gem inhibited ROKbeta-mediated phosphorylation of myosin light chain and myosin phosphatase, but not LIM kinase, suggesting that Gem acts by modifying the substrate specificity of ROKbeta. Gem or Rad expression led to cell flattening and neurite extension in N1E-115 neuroblastoma cells. In interference assays, Gem opposed ROKbeta- and Rad opposed ROKalpha-mediated cell rounding and neurite retraction. Gem did not oppose cell rounding initiated by ROKbeta containing a deletion of the Gem binding region, demonstrating that Gem binding to ROKbeta is required for the effects observed. In epithelial or fibroblastic cells, Gem or Rad expression resulted in stress fiber and focal adhesion disassembly. In addition, Gem reverted the anchorage-independent growth and invasiveness of Dbl-transformed fibroblasts. These results identify physiological roles for Gem and Rad in cytoskeletal regulation mediated by ROK.
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Proteínas Inmediatas-Precoces/metabolismo , Proteínas de Unión al GTP Monoméricas/metabolismo , Proteínas Serina-Treonina Quinasas/metabolismo , Transducción de Señal , Proteínas ras/metabolismo , Proteína de Unión al GTP rhoA/metabolismo , Células 3T3 , Actinas/metabolismo , Animales , Western Blotting , Células COS , Transformación Celular Neoplásica , Citoesqueleto/metabolismo , Retroalimentación Fisiológica , Humanos , Péptidos y Proteínas de Señalización Intracelular , Ratones , Cadenas Ligeras de Miosina/metabolismo , Invasividad Neoplásica , Neuritas/enzimología , Neuritas/metabolismo , Neuroblastoma/enzimología , Neuroblastoma/metabolismo , Neuroblastoma/patología , Fosforilación , Proteínas Serina-Treonina Quinasas/antagonistas & inhibidores , Saccharomyces cerevisiae , Células Tumorales Cultivadas , Técnicas del Sistema de Dos Híbridos , Quinasas Asociadas a rho , Proteína de Unión al GTP rhoA/antagonistas & inhibidoresAsunto(s)
Ampicilina/química , Profármacos/química , Amidas/química , Aminoácidos/química , Ampicilina/administración & dosificación , Ampicilina/farmacología , Bacterias/efectos de los fármacos , Fenómenos Químicos , Química Física , Pruebas de Sensibilidad Microbiana , Profármacos/administración & dosificación , Profármacos/farmacología , SolubilidadRESUMEN
The Protein Data Bank (PDB; http://www.rcsb.org/pdb/) is the single worldwide archive of structural data of biological macromolecules. This paper describes the data uniformity project that is underway to address the inconsistency in PDB data.