Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 25
Filtrar
Más filtros













Base de datos
Intervalo de año de publicación
1.
Sci Rep ; 14(1): 11705, 2024 05 22.
Artículo en Inglés | MEDLINE | ID: mdl-38778064

RESUMEN

A serious environmental problem that threatens soil quality, agricultural productivity, and food safety is heavy metal pollution in water sources. Heavy metal pollution is the main problem in tehsil Pasrur, Sialkot, Pakistan. Present study was arranged to notice the heavy metals in water, soil, forages and buffalo milk. There are seven sites that were used for this experiment. Highest malondialdehyde (MDA) contents (3.00 ± 0.01) were noticed in barseem roots at site 7. Ascorbate Peroxidase (APX) was reached at its peak (1.93 ± 0.01) at site 7 in the fresh barseem. Maximum protein contents (0.36 ± 0.01) were observed in fresh plant samples at site 2. Site 3's buffalo milk samples had the highest Ni content (7.22 ± 0.33 ppm), while Site 3's soil samples had the lowest Cr content (8.89 ± 0.56 ppm), Site 1's plant shoots had the lowest Cr content (27.75 ± 1.98 ppm), and Site 3's water had the highest Cr content (40.07 ± 0.49 ppm). The maximum fat content (5.38 ± 2.32%) was found in the milk of the animals at site 7. The highest density (31.88 ± 6.501%), protein content (3.64 ± 0.33%), lactose content (5.54 ± 0.320%), salt content (0.66 ± 0.1673%), and freezing point (- 0.5814 ± 0.1827 °C) were also observed in the milk from animals at site 7, whereas site 5 displayed the highest water content (0.66 ± 0.1673%) and peak pH value (11.64 ± 0.09). In selected samples, the pollution load index for Ni (which ranged from 0.01 to 1.03 mg/kg) was greater than 1. Site 7 has the highest conductivity value (5.48 ± 0.48). Values for the health risk index varied from 0.000151 to 1.00010 mg/kg, suggesting that eating tainted animal feed may pose health concerns. Significant health concerns arise from metal deposition in the food chain from soil to feed, with nickel having the highest health risk index.


Asunto(s)
Metales Pesados , Leche , Contaminantes del Suelo , Suelo , Animales , Metales Pesados/análisis , Contaminantes del Suelo/análisis , Leche/química , Leche/metabolismo , Pakistán , Suelo/química , Contaminantes Químicos del Agua/análisis , Alimentación Animal/análisis , Búfalos , Monitoreo del Ambiente/métodos , Malondialdehído/metabolismo , Malondialdehído/análisis
2.
Sci Data ; 10(1): 884, 2023 Dec 08.
Artículo en Inglés | MEDLINE | ID: mdl-38065977

RESUMEN

Here, we performed RNA-seq based expression analysis of root and leaf tissues of a set of 24 historical spring wheat cultivars representing 110 years of temporal genetic variations. This huge 130 tissues RNAseq dataset was initially used to study expression pattern of 97 genes regulating root growth and development in wheat. Root system architecture (RSA) is an important target for breeding stress-resilient and high-yielding wheat cultivars under climatic fluctuations. However, root transcriptome analysis is usually obscured due to challenges in root research due to their below ground presence. We also validated the dataset by performing correlation analysis between expression of RSA related genes in roots and leaves with 25 root traits analyzed under varying moisture conditions and 10 yield-related traits. The Pearson's correlation coefficients between root phenotypes and expression of root-specific genes varied from -0.72 to 0.78, and strong correlations with genes such as DRO1, TaMOR, ARF4, PIN1 was observed. The presented datasets have multiple uses such as a) studying the change in expression pattern of genes during time, b) differential expression of genes in two very important tissues of wheat i.e., leaf and roots, and c) studying customized expression of genes associated with important phenotypes in diverse wheat cultivars. The initial findings presented here provided key insights into understanding the transcriptomic basis of phenotypic variability of RSA in wheat cultivars.


Asunto(s)
RNA-Seq , Triticum , Perfilación de la Expresión Génica , Fenotipo , Fitomejoramiento , Transcriptoma , Triticum/genética
3.
Heliyon ; 9(9): e19326, 2023 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-37681127

RESUMEN

Alpha arbutin is a skin-whitening agent in cosmetics. Structurally, it is 4-hydroxyphenyl-α-glucopyranoside. Ethosomes encourage the formation of lamellar-shaped vesicles with improved solubility and entrapment of whitening agents. The objective of this study was to fabricate an optimized nanostructured ethosomal gel loaded with alpha arbutin for the treatment of skin pigmentation. Different ethosomal suspensions of alpha arbutin were prepared by the cold method. Invitro evaluation included zeta potential, droplet size analysis, polydispersity index, entrapment efficiency (EE), scanning electron microscopy (SEM) and Fourier transform infrared (FTIR) spectroscopy. Stability studies of the optimized ethosomal and control gels were performed for three months under different temperature conditions. The optimized ethosomal gel loaded with alpha arbutin was further analyzed on human volunteers for skin benefits by measuring melanin level, moisture content and elasticity. It was concluded that the optimized formulation had a size, zeta potential, polydispersity index and entrapment efficiency of 196.87 nm, -45.140 mV, 0.217 and 93.458343%, respectively. Scanning electron microscopy (SEM) depicted spherical ethosomal vesicles. Stability data was obtained in terms of pH and conductivity. Rheological analysis revealed non-Newtonian flow. The cumulative drug permeated for ethosomal gel was 78.4%. Moreover, encapsulation of alpha arbutin causes significant improvement in skin melanin, moisture content and elasticity. The overall findings suggested that the arbutin-loaded ethosomal formulation was stable and could be a better approach than conventional formulation for cosmeceutical purposes such as for depigmentation and moisturizing effects.

4.
Cell Biochem Funct ; 41(5): 573-589, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-37222443

RESUMEN

Inflammation is an innate reaction of the body of an individual when subjected to the noxious factors repeatedly. Pharmacological approaches focused at disrupting cytokine signaling networks have become significant therapeutic alternatives for the treatment of inflammatory illnesses, cancer and autoimmune disorders. High levels of inflammatory mediators, particularly interleukin IL-1, IL-6, IL-18, IL-12, and tumor necrosis factor alpha leads to a cytokine storm in the body. Among all the released cytokines in a patient suffering from inflammatory disorder, IL-6 mediator has a pivotal role in this inflammatory cascade which progresses to a cytokine storm. Therefore, the blockage of the IL-6 inflammatory mediator could be a promising treatment option for the patients with hyper inflammatory conditions. The phytochemicals could provide the new lead compounds against the IL-6 mediator. Ficus carica has been the ideal plant of research and investigation due to its commercial, economic and medical importance. The anti-inflammatory properties of F. carica were further investigated by in silico and in vivo approaches. The docking scores of Cyanidin-3,5-diglucoside, Kaempferol-7-O-rutinoside, Cyanidin-3-rhamnoglucoside, and Rutin are -9.231, -8.921, -8.840, and -8.335 Kcal/mole respectively. The free energy of binding and stability of the docked complexes of these top four phytochemicals with the IL-6 were further analyzed by Molecular Mechanics-Generalized Born Surface Area and Molecular Dynamic simulations, respectively. The in vivo anti-inflammatory carrageenan-induced rat paw edema model was used for the validation of in silico results. The maximum percentage paw edema inhibition with petroleum ether and ethyl acetate was 70.32% and 45.05%, respectively. The in vivo anti-inflammatory activity confirms the anti-inflammatory potential of F. carica. Therefore, it is predicted that Cyanidin-3,5-diglucoside, Kaempferol-7-O-rutinoside, Cyanidin-3-rhamnoglucoside, and Rutin have the potential to inhibit the IL-6 mediator which will aid in mitigating the cytokine storm in patients with acute inflammations.


Asunto(s)
Ficus , Interleucina-6 , Ratas , Animales , Interleucina-6/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/química , Ficus/química , Ficus/metabolismo , Quempferoles , Síndrome de Liberación de Citoquinas , Carragenina/efectos adversos , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Antiinflamatorios/química , Citocinas/metabolismo , Fitoquímicos/efectos adversos , Edema/inducido químicamente
5.
Molecules ; 27(18)2022 Sep 14.
Artículo en Inglés | MEDLINE | ID: mdl-36144719

RESUMEN

Emulgel is a new innovatory technique for drug development permitting controlled release of active ingredients for topical administration. We report a stable emulgel of 4% Piper nigrum extract (PNE) prepared using 80% ethanol. The PNE-loaded formulation had an antioxidant activity of 84% and tyrosinase inhibition was 82%. Prepared formulation rendered spherical-shaped globules with high zeta potential (-45.5 mV) indicative of a stable system. Total phenolic contents were 58.01 mg GAE/g of dry extract whereas total flavonoid content was 52.63 mg QE/g of dry extract. Sun protection factor for PNE-loaded emulgel was 7.512 and formulation was stable without any evidence of physical and chemical changes following 90 days of storage. Gas chromatography-mass spectroscopy (GC-MS) revealed seventeen bioactive compounds in the PNE including monoterpenoids, triterpenoids, a tertiary alcohol, fatty acid esters, and phytosterols. In silico studies of GC-MS identified compounds show higher binding affinity in comparison to standard kojic acid indicating tyrosinase inhibition. It can be concluded that PNE-loaded emulgel had prominent antioxidant and tyrosinase inhibition and can be utilized as a promising topical system for anti-aging skin formulation.


Asunto(s)
Fitosteroles , Piper nigrum , Triterpenos , Alérgenos , Antioxidantes/química , Antioxidantes/farmacología , Preparaciones de Acción Retardada , Etanol , Alcoholes Grasos , Flavonoides , Simulación del Acoplamiento Molecular , Monofenol Monooxigenasa , Monoterpenos , Piper nigrum/química , Extractos Vegetales/química , Semillas
6.
Pharmaceutics ; 14(8)2022 Aug 09.
Artículo en Inglés | MEDLINE | ID: mdl-36015282

RESUMEN

Antioxidants from natural sources are extensively attaining consideration to avert the skin from damage and aging caused by free radicals. Flaxseed (Linum usitatissimum L.), a natural therapeutic agent, was meant to be explored cosmeceutical by quantifying its potential phytoconstituents and to be incorporated into a microemulgel for topical use. Hydroalcoholic fractions (both methanolic and ethanolic; 80%) flaxseed extracts were subjected to phytochemical screening by quantifying total phenolic content (TPC), total flavonoid content (TFC), and high-performance liquid chromatography-ultraviolet (HPLC-UV), and for biological activities through 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, tyrosinase inhibition assay, and sun protection factor (SPF). Ethanolic fraction was selected for further study by TPC (18.75 mg gallic acid equivalent/g) and TFC (1.34 mg quercetin equivalent/g). HPLC-UV analysis showed the existence of benzoic, quercetin, caffeic, vanillic, p-coumaric, gallic, cinnamic, syringic, and sinapic acids. Biological activities showed 87.00%, 72.00%, and 21.75 values for DPPH assay, tyrosinase inhibition, and SPF assays, respectively. An oil-in-water (OW) microemulsion containing the flaxseed extract, with 99.20 nm Zeta size, −19.3 Zeta potential and 0.434 polydispersity index was developed and incorporated in Carbopol-940 gel matrix to formulate an active microemulgel with 59.15% release in in vitro studies. The successfully formulated stable active microemulgel produced statistically significant effects (p < 0.05), in comparison to a placebo, on skin erythema, melanin, sebum, moisture, and elasticity, in a noninvasive in vivo study performed on 13 healthy human female volunteers. Other cosmeceutical products can also be formulated from flaxseed, making it a considerable candidate for further utilization in the pharmaceutical industry.

7.
AAPS PharmSciTech ; 23(5): 156, 2022 Jun 02.
Artículo en Inglés | MEDLINE | ID: mdl-35655105

RESUMEN

Sumatriptan succinate and prochlorperazine maleate are a clinically proven combination for treating migraine and associated nausea and vomiting. Classical oral dosage forms are not frequently workable in migraine because of the associated nausea/vomiting, and no effective fixed dose combination is available. Thus, the aim of the study was to optimize a combined sumatriptan-prochlorperazine orodispersible film for rapid release of drugs. Orodispersible films were prepared by solvent casting method using varied amounts of polyvinyl alcohol and glycerol as film former and plasticizer, respectively, along with fixed levels of other ingredients employing central composite design. The optimum film (VF) demonstrated disintegration and total dispersion times as 21 s and 2.3 min, respectively. Tensile strength and Young's modulus were 8.86 ± 0.37 MPa and 24.15 ± 0.07 MPa, respectively. The in vitro T80% of both drugs from the ODF was achieved within 4 min. The film was palatable and disintegrated in 2 min in buccal cavity of human volunteers. Permeation study through goat mucosa demonstrated 100% permeation of both drugs within 15 min. X-Ray diffraction and differential scanning calorimetry supported drugs being amorphous and Fourier transform infrared demonstrated drug-excipient compatibility in optimized film. A judicious combination of sumatriptan succinate and prochlorperazine maleate could be prepared in orodispersible films for the possible relief of migraine.


Asunto(s)
Trastornos Migrañosos , Sumatriptán , Excipientes/química , Humanos , Náusea , Proclorperazina , Vómitos
8.
Insect Mol Biol ; 31(5): 568-584, 2022 10.
Artículo en Inglés | MEDLINE | ID: mdl-35499809

RESUMEN

Insects are highly reliant on their active olfactory system in which odorant binding proteins play a role to selectivity and sensitivity during odour perception and processing. This study sets out to determine whether and to which extent the antennal loaded SaveOBP10 in English grain aphid Sitobion avenae, contributes in olfactory processing during host selection. To understand this possible relationship, we purified the SaveOBP10 recombinant protein and performed fluorescence ligand binding tests, molecular docking, RNA interference (RNAi) and behavioural trials. The results showed that SaveOBP10 had strong binding affinities (Ki ≤5 µM) with most of wheat plant volatiles at pH 5.0 as compared to pH 7.4. In Y-tube olfactometer bioassays, the S. avenae was attracted behaviourally towards pentadecane, butylated hydroxytoluene, tetradecane and ß-caryophyllene however repelled by naphthalene. After RNAi of SaveOBP10, the aphid showed nonattraction towards ß-caryophyllene and nonsignificant behavioural response to pentadecane, butylated hydroxytoluene and tetradecane. Furthermore, the three-dimensional structure modelling and molecular docking of SaveOBP10 were performed to the volatiles with high binding abilities. Together these findings indicate that SaveOBP10 can bind more strongly to the volatiles that involved in S. avenae behaviour regulation and possibly will contribute effectively in S. avenae integrated pest management.


Asunto(s)
Áfidos , Animales , Áfidos/genética , Hidroxitolueno Butilado , Simulación del Acoplamiento Molecular , Odorantes , Interferencia de ARN
9.
Plant Physiol Biochem ; 178: 20-30, 2022 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-35247694

RESUMEN

Drought is a big challenge for agricultural production. Root attributes are the important target traits for breeding high-yielding sustainable wheat varieties against ever changing climatic conditions. However, the transcriptomic of wheat concerning root architecture remained obscure. Here, we explored RNA-Seq based transcriptome to dissect putative genes involved in root system variations in naturally occurring six genotypes (drought-tolerant and sensitive) of wheat. Global RNA-Seq based root transcriptome analysis revealed single nucleotide polymorphisms (SNPs) variations and differentially expressed genes. Putative 56 SNPs were identified related to 15 genes involved in root architecture. Enrichment of these genes using GO terms demonstrated that differentially expressed genes (DEGs) are divided into sub-categories implicated in molecular functions, cellular components and biological processes. The KEGG analysis of DEGs in each comparison of genotype include metabolic, biosynthesis of secondary metabolites, microbial metabolism in diverse environments and biosynthesis of antibiotics. A deeper insight into DEGs unveiled various pathways involved in drought response and positive gravitropism. These genes belong to various transcription factor families such as DOF, C3H, MYB, and NAC involved in root developmental and stress-related pathways. Local White and UZ-11-CWA-8, which are drought-tolerant genotypes, harbor over-representation of most of DEGs or transcription factors. Notably, a microtubule-associated protein MAPRE1 belonging to RP/EB family recruited in positive gravitropism was enriched. Real-time PCR analysis revealed expression of MAPRE1 and PAL genes is consistent with RNA-seq data. The presented data and genetic resources seem valuable for providing genes involved in the root system architecture of drought-tolerant and susceptible genotypes.


Asunto(s)
Sequías , Transcriptoma , Perfilación de la Expresión Génica , Regulación de la Expresión Génica de las Plantas , Genotipo , Fitomejoramiento , Estrés Fisiológico/genética , Transcriptoma/genética , Triticum/genética , Triticum/metabolismo
10.
PLoS One ; 17(3): e0265270, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35275970

RESUMEN

Wheat is an important cereal and half of the world population consumed it. Wheat faces environmental stresses and different techniques (CRISPR, gene silencing, GWAS, etc.) were used to enhance its production but RNA editing (RESs) is not fully explored in wheat. RNA editing has a special role in controlling environmental stresses. The genome-wide identification and functional characterization of RESs in different types of wheat genotypes was done. We employed six wheat genotypes by RNA-seq analyses to achieve RESs. The findings revealed that RNA editing events occurred on all chromosomes equally. RNA editing sites were distributed randomly and 10-12 types of RESs were detected in wheat genotypes. Higher number of RESs were detected in drought-tolerant genotypes. A-to-I RNA editing (2952, 2977, 1916, 2576, 3422, and 3459) sites were also identified in six wheat genotypes. Most of the genes were found to be engaged in molecular processes after a Gene Ontology analysis. PPR (pentatricopeptide repeat), OZ1 (organelle zinc-finger), and MORF/RIP gene expression levels in wheat were also examined. Normal growth conditions diverge gene expression of these three different gene families, implying that normal growth conditions for various genotypes can modify RNA editing events and have an impact on gene expression levels. While the expression of PPR genes was not change. We used Variant Effect Predictor (VEP) to annotate RNA editing sites, and Local White had the highest RESs in the CDS region of the protein. These findings will be useful for prediction of RESs in other crops and will be helpful in drought tolerance development in wheat.


Asunto(s)
Edición de ARN , Triticum , Sequías , Genoma , Orgánulos , Edición de ARN/genética , Triticum/genética
11.
Curr Drug Deliv ; 19(5): 534-546, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-34288836

RESUMEN

INTRODUCTION: The pleiotropic effects of statins are recently explored for wound healing through angiogenesis and lymph-angiogenesis that could be of great importance in diabetic wounds. AIMS: The aim of the present study is to fabricate nanofilm embedded with simvastatin-loaded chitosan nanoparticles (CS-SIM-NPs) and to explore the efficacy of SIM in diabetic wound healing. METHODS: The NPs, prepared via ionic gelation, were 173 nm ± 2.645 in size with a zeta potential of -0.299 ± 0.009 and PDI 0.051 ± 0.088 with excellent encapsulation efficiency (99.97%). The optimized formulation (CS: TPP, 1:1) that exhibited the highest drug release (91.64%) was incorporated into the polymeric nanofilm (HPMC, Sodium alginate, PVA), followed by in vitro characterization. The optimized nanofilm was applied to the wound created on the back of diabetes-induced (with alloxan injection 120 mg/kg) albino rats. RESULTS: The results showed a significant (p < 0.05) improvement in the wound healing process compared to the diabetes-induced non-treated group. The results highlighted the importance of nanofilms loaded with SIM-NPs in diabetic wound healing through angiogenesis promotion at the wound site. CONCLUSION: Thus, CS-SIM-NPs loaded polymeric nanofilms could be an emerging diabetic wound healing agent in the industry of nanomedicines.


Asunto(s)
Quitosano , Diabetes Mellitus , Nanopartículas , Animales , Polímeros , Ratas , Simvastatina/farmacología , Cicatrización de Heridas
12.
Curr Issues Mol Biol ; 45(1): 12-32, 2022 Dec 20.
Artículo en Inglés | MEDLINE | ID: mdl-36661488

RESUMEN

COVID-19 disease has had a global impact on human health with increased levels of morbidity and mortality. There is an unmet need to design and produce effective antivirals to treat COVID-19. This study aimed to explore the potential ability of natural stilbenes to inhibit the Mpro protease, an acute respiratory syndrome coronavirus-2 (SARS-CoV-2) enzyme involved in viral replication. The binding affinities of stilbene compounds against Mpro were scrutinized using molecular docking, prime molecular mechanics-generalized Born surface area (MM-GBSA) energy calculations, and molecular dynamic simulations. Seven stilbene molecules were docked with Mpro and compared with GC376 and N3, antivirals with demonstrated efficacy against Mpro. Ligand binding efficiencies and polar and non-polar interactions between stilbene compounds and Mpro were analyzed. The binding affinities of astringin, isorhapontin, and piceatannol were -9.319, -8.166, and -6.291 kcal/mol, respectively, and higher than either GC376 or N3 at -6.976 and -6.345 kcal/mol, respectively. Prime MM-GBSA revealed that these stilbene compounds exhibited useful ligand efficacy and binding affinity to Mpro. Molecular dynamic simulation studies of astringin, isorhapontin, and piceatannol showed their stability at 300 K throughout the simulation time. Collectively, these results suggest that stilbenes such as astringin, isorhapontin, and piceatannol could provide useful natural inhibitors of Mpro and thereby act as novel treatments to limit SARS-CoV-2 replication.

13.
Drug Des Devel Ther ; 15: 2193-2210, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34079222

RESUMEN

PURPOSE: A differential release fixed dose matrix tablet of amlodipine besylate (AML-B) and simvastatin (SIM) was formulated to enhance patient compliance. MATERIAL AND METHOD: In the first phase, release controlling parameters of AML-B and SIM granules were identified and in the second phase a fixed dose AML-B and SIM tablet formulation was prepared and optimized for a differential release of the drugs using a quality by design (QbD) and risk assessment approach. A validated HPLC method was employed for simultaneous determination of AML-B and SIM for FDC formulation. A pharmacokinetics of the above drugs was studied in healthy dogs in the third phase. RESULTS: In QbD-based optimized formulation, Eudragit® RSPO-dicalcium phosphate (DCP) blend controlled the release of AML-B over 8 h, though this diffusion-controlled release assumed first order kinetics. DCP and Eudragit® RS 100 also retarded release of SIM causing SIM release over 8 h after AML-B release from the optimized FDC tablet formulation. The HPLC retention times of AML-B and SIM were 2.10 and 15.52 min, respectively. Linearity for AML-B was 5.0-50 ng/mL and 0.01-2.0 µg/mL for SIM with percent recoveries of 92.85-101.53% and 94.51-117.75% for AML-B and SIM. AUC0-∞ of AML-B was increased 3 fold, while AUC0-∞ of SIM was decreased 2 fold. The tmax values for AML-B and SIM were 12 and 6 h, respectively. AML-B was absorbed without any lag time (tlag) while tlag was 6.33 ± 0.81 h for SIM, thus met the study objective. CONCLUSION: The pharmacokinetic study showed an immediate absorption of AML-B while that of SIM was withheld for 6 h, close to the desired delay time of 8 h.


Asunto(s)
Amlodipino/farmacocinética , Simvastatina/farmacocinética , Amlodipino/síntesis química , Amlodipino/química , Relación Dosis-Respuesta a Droga , Composición de Medicamentos , Diseño de Fármacos , Liberación de Fármacos , Humanos , Medición de Riesgo , Simvastatina/síntesis química , Simvastatina/química , Comprimidos
14.
Drug Dev Ind Pharm ; 46(12): 2070-2080, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-33112681

RESUMEN

Patients suffering from dysphagia have trouble in swallowing conventional oral dosage forms and there is also risk of choking, which may cause patient noncompliance. This study aimed to develop an orodispersible film (ODF) containing cefixime trihydrate (CFX) to cope with the above-mentioned problems as well as to enhance water solubility and masking the bitter taste of the drug. The freeze-drying and kneading methods were used for the formation of inclusion complexes. The physicochemical evaluation revealed that T7 was the best film for the incorporation of pure drug and inclusion complexes. Films were further characterized for physical and mechanical properties. Drug content, dissolving time of the film and drug release tests were performed. In vivo taste and disintegration time studies were also conducted in healthy human volunteers. FTIR spectra of the individual ingredients and prepared formulations have confirmed the chemical compatibilities of the ingredients. The solubility of CFX was increased by complexation with ß-CD and optimized freeze-dried inclusion complex (FD1) was selected for the formation of ODF. C4 was selected as an optimized film for the delivery of CFX as this film has released 95.52% drug at the end of 10 min. Dissolution kinetics of FD1 showed that it followed zero-order kinetics while drug release from films, exhibits first-order kinetics; however, both showed non-Fickian transport. In vivo taste evaluation revealed that taste was masked by inclusion complexation with ß-CD. However, selected ingredients and employed methodology enabled to formulate film, capable of delivering taste-masked CFX with improved solubility and better patient compliance.


Asunto(s)
Cefixima/química , Gusto , Administración Oral , Composición de Medicamentos , Liberación de Fármacos , Humanos , Solubilidad
15.
Drug Des Devel Ther ; 14: 2435-2448, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32606610

RESUMEN

BACKGROUND: Severe bleeding and perforation of the colon and rectum are complications of ulcerative colitis which can be treated by a targeted drug delivery system. PURPOSE: Development of colon-targeted delivery usually involves a complex formulation process and coating steps of pH-sensitive methacrylic acid based Eudragit®. The current work was purposefully designed to develop dicalcium phosphate (DCP) facilitated with Eudragit-S100-based pH-dependent, uncoated mesalamine matrix tablets. MATERIALS AND METHODS: Mesalamine formulations were compressed using wet granulation technique with varying compositions of dicalcium phosphate (DCP) and Eudragit-S100. The developed formulations were characterized for physicochemical and drug release profiles. Infrared studies were carried out to ensure that there was no interaction between active ingredients and excipients. Artificial neural network (ANN) was used for the optimization of final DCP-Eudragit-S100 complex and the experimental data were employed to train a multi-layer perception (MLP) using quick propagation (QP) training algorithm until a satisfactory root mean square error (RMSE) was reached. The ANN-aided optimized formulation was compared with commercially available Masacol®. RESULTS: Compressed tablets met the desirability criteria in terms of thickness, hardness, weight variation, friability, and content uniformity, ie, 5.34 mm, 7.7 kg/cm2, 585±5 mg (%), 0.44%, and 103%, respectively. In-vitro dissolution study of commercially available mesalamine and optimized formulation was carried out and the former showed 100% release at 6 h while the latter released only 12.09% after 2 h and 72.96% after 12 h which was fitted to Weibull release model with b value of 1.3, indicating a complex release mechanism. CONCLUSION: DCP-Eudragit-S100 blend was found explicative for mesalamine release without coating in gastric and colonic regions. This combination may provide a better control of ulcerative colitis.


Asunto(s)
Redes Neurales de la Computación , Ácidos Polimetacrílicos/química , Comprimidos/química , Fosfatos de Calcio/síntesis química , Fosfatos de Calcio/química , Composición de Medicamentos , Concentración de Iones de Hidrógeno , Ácidos Polimetacrílicos/síntesis química , Comprimidos/síntesis química
16.
J Chem Ecol ; 46(4): 363-377, 2020 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-32125582

RESUMEN

Insects have evolved highly sensitive olfactory sensory systems to detect plant hosts and mates, with plant volatiles playing an important role in informing insect behavior. Chemosensory proteins (CSPs) are thought to play a key role in this process, but in this respect, there is limited information on brown planthopper Nilaparvata lugens, one of the most destructive pests of rice. To expand our understanding of CSP function in N. lugens we explored expression profiles and binding characteristics of NlugCSP3. The ligands with higher binding affinity were also validated by molecular docking and behavioral assays. NlugCSP3 mRNA was expressed at relatively higher levels in antennae and abdomen of 3-day-old unmated macropterous males as well as in antennae of 3-day mated macropterous and brachypterous females. Fluorescence competitive binding assays revealed that 5 out of 25 candidate volatiles are strong binders (Ki < 10 µM). Behavioral assays revealed that nonadecane and 2-tridecanone, which have high binding affinities in fluorescence competition-binding assays, displayed strong attractiveness to N. lugens. Pursuing this further, molecular docking analysis identified key amino acid residues involved in binding volatile compounds. Overall, our data provide a base for further investigation of the potential physiological functions of CSP3 in Nilaparvata lugens, and extend the function of NlugCSP3 in chemoreception of N. lugens.


Asunto(s)
Expresión Génica , Hemípteros/genética , Proteínas de Insectos/genética , Compuestos Orgánicos Volátiles/metabolismo , Factores de Edad , Aminoácidos/metabolismo , Animales , Antenas de Artrópodos/metabolismo , Femenino , Perfilación de la Expresión Génica , Hemípteros/química , Hemípteros/metabolismo , Proteínas de Insectos/metabolismo , Ligandos , Masculino , Simulación del Acoplamiento Molecular , Reproducción , Factores Sexuales , Alas de Animales/anatomía & histología
17.
PLoS One ; 14(4): e0214145, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-30947257

RESUMEN

Root growth angle (RGA) in response to gravity controlled by auxin is a pertinent target trait for obtainment of higher yield in cereals. But molecular basis of this root architecture trait remain obscure in wheat and barley. We selected four cultivars two each for wheat and barley to unveil the molecular genetic mechanism of Deeper Rooting 1-like gene which controls RGA in rice leading to higher yield under drought imposition. Morphological analyses revealed a deeper and vertically oriented root growth in "NARC 2009" variety of wheat than "Galaxy" and two other barley cultivars "Scarlet" and "ISR42-8". Three new homoeologs designated as TaANDRO1-like, TaBNDRO1-like and TaDNDRO1-like corresponding to A, B and D genomes of wheat could be isolated from "NARC 2009". Due to frameshift and intronization/exonization events the gene structures of these paralogs exhibit variations in size. DRO1-like genes with five distinct domains prevail in diverse plant phyla from mosses to angiosperms but in lower plants their differentiation from LAZY, NGR and TAC1 (root and shoot angle genes) is enigmatic. Instead of IGT as denominator motif of this family, a new C-terminus motif WxxTD in the V-domain is proposed as family specific motif. The EAR-like motif IVLEM at the C-terminus of the TaADRO1-like and TaDDRO1-like that diverged to KLHTLIPNK in TaBDRO1-like and HvDRO1-like is the hallmark of these proteins. Split-YFP and yeast two hybrid assays complemented the interaction of TaDRO1-like with TOPLESS-a repressor of auxin regulated root promoting genes in plants-through IVLEM/KLHTLIPNK motif. Quantitative RT-PCR revealed abundance of DRO1-like RNA in root tips and spikelets while transcript signals were barely detectable in shoot and leaf tissues. Interestingly, wheat exhibited stronger expression of TaBDRO1-like than barley (HvDRO1-like), but TaBDRO1-like was the least expressing among three paralogs. The underlying cause of this expression divergence seems to be the presence of AuxRE motif TGTCTC and core TGTC with a coupling AuxRE-like motif ATTTTCTT proximal to the transcriptional start site in TaBDRO1-like and HvDRO1-like promoters. This is evident from binding of ARF1 to TGTCTC and TGTC motifs of TaBDRO1-like as revealed by yeast one-hybrid assay. Thus, evolution of DRO1-like wheat homoeologs might incorporate the C-terminus mutations as well as gain and loss of AuxREs and other cis-regulatory elements during expression divergence. Since root architecture is an important target trait for wheat crop improvement, therefore DRO1-like genes have potential applications in plant breeding for enhancement of plant productivity by the use of modern genome editing approaches.


Asunto(s)
Evolución Molecular , Ácidos Indolacéticos/farmacología , Mutación/genética , Proteínas de Plantas/química , Proteínas de Plantas/genética , Elementos de Respuesta/genética , Homología de Secuencia de Aminoácido , Triticum/genética , Secuencias de Aminoácidos , Secuencia de Aminoácidos , Secuencia de Bases , Regulación de la Expresión Génica de las Plantas/efectos de los fármacos , Hordeum/anatomía & histología , Hordeum/efectos de los fármacos , Intrones/genética , Proteínas de Plantas/metabolismo , Raíces de Plantas/anatomía & histología , Raíces de Plantas/efectos de los fármacos , Raíces de Plantas/genética , Regiones Promotoras Genéticas , ARN Mensajero/genética , ARN Mensajero/metabolismo , Triticum/anatomía & histología , Triticum/efectos de los fármacos
18.
Pak J Pharm Sci ; 32(5(Supplementary)): 2299-2304, 2019 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-31894058

RESUMEN

Chitosan nanoparticles (CSNPs) have proven their excellent drug delivery potential through various routes of administration and therefore, the need for large scale production of CSNPs for the commercialization is paramount. Their particle size and surface charge, drug loading capacity, and morphology were characterized in this study. Finally, drug release studies of both continuous and scalable modes were undertaken to ascertain suitability of CSNPs as a carrier for HC. The particle size of the large and small scale of HC-CSNPs was 253.3±16.4 nm and 225.4 ±9.6 nm, respectively. Besides, the surface charge of the large and small scale of HC-CSNPs was +35.3±0.3 mV and +32.6±2.5 mV, respectively. The size and surface charge of both HC-CSNPs were not proven to be statistically different. Drug loading capacity of large and small scale production of HC-CSNPs was high with 89%, and 83% of HC was loaded into CSNPs, respectively. Moreover, the morphology of both large and small scale production of HC-CSNPs had a similar shape and particle size. The drug release profile of CSNPs prepared by both methods showed a significantly (p<0.05) higher percentage release as compared to the free form. It is expected that positively charged nano-sized HC-CSNPs with high drug loading capacity could enhance the efficiency of drug delivery system to carry and diffuse into the target cells. The results obtained also suggested that the modified method applied could be further developed for large scale production of HC-CSNPs.


Asunto(s)
Quitosano/química , Dermatitis Atópica/tratamiento farmacológico , Sistemas de Liberación de Medicamentos , Hidrocortisona/química , Nanopartículas/química , Análisis Costo-Beneficio , Liberación de Fármacos , Geles , Humanos , Hidrocortisona/administración & dosificación , Tamaño de la Partícula
19.
Biomed Pharmacother ; 107: 806-817, 2018 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-30142542

RESUMEN

Several plants found rich in flavonoid, polyphenols, and antioxidants reported antiaging, oppose inflammation and carcinogenic properties but have rarely been applied in dermatology. The present study was an active attempt to formulate a stable phytocosmetic emulsion system loaded with 2% pre-concentrated Prosopis cineraria bark extract, aiming to revive facial skin properties. In order to obtain potent therapeutic activities, we first prepared extracts of stem, leaves, and bark and screen them on basis of phenolic, flavonoids contents and antioxidant, antibacterial, lipoxygenase and tyrosinase inhibition activities. Furthermore, cytocompatibility of the extract was also determined prior starting in vivo investigations. Then the in vivo performance of 2% bark extract loaded emulsion formulation was determined by using non-invasive probe cutometer and elastometer with comparison to base formulation. The preliminary experiment showed that bark extract has a significant amount of phenolic and flavonoid compounds with eminent antioxidant potential. Furthermore, indicated an efficient antibacterial, lipoxygenase, and tyrosinase enzyme inhibition activities. Importantly, the bark extract did not induce any toxicity or apoptosis, when incubated with HaCat cells. Moreover, the in vivo results showed the formulation (size 3 µm) decreased the skin melanin, erythema and sebum contents up to 2.1-,2.7-and 79%, while increased the skin hydration and elasticity up to 2-folds and 22% as compared to the base, respectively. Owing to enhanced therapeutic effects the phytocosmetic formulation proved to be a potential skin whitening, moisturizer, anti-acne, anti-wrinkle, anti-aging therapy and could actively induce skin rejuvenation and resurfacing.


Asunto(s)
Cosméticos/farmacología , Composición de Medicamentos , Fitoquímicos/farmacología , Adulto , Antibacterianos/farmacología , Antioxidantes/análisis , Apoptosis/efectos de los fármacos , Línea Celular , Forma de la Célula/efectos de los fármacos , Elasticidad , Eritema/patología , Flavonoides/análisis , Humanos , Inhibidores de la Lipooxigenasa/farmacología , Masculino , Melaninas , Monofenol Monooxigenasa/antagonistas & inhibidores , Fenoles/análisis , Corteza de la Planta/química , Hojas de la Planta/química , Reología , Sebo/metabolismo , Piel/patología , Factor de Protección Solar
20.
Acta Pol Pharm ; 69(2): 285-90, 2012.
Artículo en Inglés | MEDLINE | ID: mdl-22568043

RESUMEN

Atenolol and simvastatin were granulated in combination by non-solvent addition coacervation method to treat hypertension orally. Dissolution test was performed in water containing 0.5% sodium dodecyl sulfate at 37 0.05 degrees C. FTIR spectrometry, X-ray diffractometry and thermal analysis confirmed the absence of any chemical interaction between polymer and the entrapped drugs. The granules size was about 280-619 µm. Scanning electron microscopy reported irregular morphology of granules. The entrapment efficiency was approximately 90% for atenolol and 70% for simvastatin. A controlled release behavior of both drugs but a burst release phenomenon of simvastatin from the formulations were observed. In conclusion, granules loaded with a hydrophilic and a lipophilic drug were successfully prepared.


Asunto(s)
Antihipertensivos/administración & dosificación , Atenolol/administración & dosificación , Simvastatina/administración & dosificación , Tecnología Farmacéutica , Atenolol/química , Combinación de Medicamentos , Simvastatina/química , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier , Difracción de Rayos X
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA