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1.
Cytokine ; 137: 155341, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33128919

RESUMO

The adipokine, leptin exerts inhibitory effect on both spontaneous and oxytocin-induced contractions in myometrium. However, the mechanisms involved in leptin-induced effect are not clear. In the present study, we studied the altered characteristics of uterine contractions in the presence of leptin and the possible mechanisms of its effect in late pregnant (18.5 day) mouse uterus. We conducted functional, biochemical and molecular biology studies to demonstrate the mechanism of leptin-induced response. Leptin exerted an inhibitory response (Emax 40.5 ± 3.99%) on basal uterine contractions. The extent of inhibition was less than that obtained with known uterine relaxants, salbutamol (Emax103 ± 8.66%) and BRL-37344 (Emax 84.79 ± 8.12%). Leptin-induced uterine response was inhibited by leptin receptor antagonist SHLA and JAK-STAT pathway inhibitor, AG-490. The relaxant response was also subdued by NO-cGMP-PK-G pathway blockers L-NAME, 1400W, ODQ and KT-5823. Further, leptin enhanced the levels of NO and cGMP in uterine tissues. Also, SHLA, AG-490 and a combination of 1400 W and L-NAME prevented leptin-induced increase in NO. Similar effect was observed on cGMP levels in presence of leptin and SHLA. However, leptin did not influence CaCl2-induced response in potassium-depolarized tissues. We also detected leptin receptor protein in late pregnant mouse uterus located in endometrial luminal epithelium and myometrial layers. Real-time PCR studies revealed significantly higher expression of short forms of the receptor (ObRa and ObRc) in comparison to the long form (ObRb). In conclusion, the results of the present study suggest that leptin inhibits mouse uterine contraction by stimulating short forms of the leptin receptors and activating NO pathway in a JAK-STAT-dependent manner.

2.
Theriogenology ; 159: 123-131, 2021 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-33137633

RESUMO

Environmental stress in the form of high temperature humidity index (THI) in tropical and sub-tropical region negatively affects semen quality and fertility of boar. Therefore, the present study was done to evaluate the effect of supplementing flaxseed oil (FLO) to boar's diet on its semen quality, antioxidant status, fatty acid composition of seminal plasma and fertility under sub-tropical climate. For this purpose, six Hampshire crossbreed (50% Hampshire and 50% Gunghroo) boars were divided into two groups i.e control (CON) and treatment (FLO). In FLO and CON group, flaxseed and vegetable oil, respectively, was top dressed at the rate of 3% in basal diets for each boar on daily basis for 16 weeks during monsoon season. A total of 60 ejaculates, comprising 30 ejaculates from each group (ten ejaculates from each boar) were collected. Semen samples were evaluated for sperm quality parameters (SQPs: motility, viability, abnormality, acrosomal integrity and Hypo-osmotic swelling test) and velocity attributes by computer assisted semen analysis (CASA) at fresh and after 72 h of preservation at 17 °C. Antioxidant (glutathione peroxidase; GPx, catalase; CAT, total antioxidant capacity; TAC and malondialdehyde; MDA) were analyzed in seminal plasma and serum. Fatty acid compositions of seminal plasma were analyzed by gas chromatography-mass spectrometry (GC-MS). In-vivo fertility study was also conducted. Reaction time and false mounts were significantly (p < 0.05) reduced in FLO group as compared to CON group. Semen quality parameters were significantly (p < 0.05) improved at fresh stage and after 72 h of liquid storage in FLO group as compared to CON group. Velocity attributes (VAP, VSL, VCL, ALH, BCF and LIN) were significantly (p < 0.05) higher in FLO group. Flaxseed oil supplementation significantly (p < 0.01) enhanced serum GPx and CAT concentration. Serum and seminal plasma MDA concentration decreased significantly (p < 0.01) in FLO group. Similarly, GPx, TAC and CAT were significantly (p < 0.01) elevated in seminal plasma of FLO group. The study revealed that feeding of flaxseed oil altered the fatty acid composition of seminal plasma and significantly (p < 0.05) improved the farrowing rate. In summary, flaxseed oil supplementation improved the semen quality parameters and fertility of boars in sub-tropical climate by improving the antioxidant capacity and altering the fatty acid composition of seminal plasma.

3.
Chemosphere ; 263: 128074, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33297076

RESUMO

Environmental exposure to pesticides increases the risk of neurotoxicity and neurodegenerative diseases. The mechanism of pesticide-induced toxicity is attributed to the increased reactive oxygen species, mitochondrial dysfunction, inhibition of key cellular enzymes and accelerated pathogenic protein aggregation. The structural basis of pesticide-protein interaction is limited to pathogenic proteins such as α-synuclein, Tau and amyloid-beta. However, the effect of pesticides on metabolic proteins is still unexplored. Here, we used rotenone and chlorpyrifos to understand the interaction of these pesticides with a metabolic protein, malate dehydrogenase (MDH) and the consequent pesticide-induced cytotoxicity. We found that rotenone and chlorpyrifos strongly bind to MDH, interferes with protein folding and triggers alteration in its secondary structure. Both pesticides showed high binding affinities for MDH as observed by NMR and LCMS. Rotenone and chlorpyrifos induced structural alterations during MDH refolding resulting in the formation of cytotoxic conformers that generated oxidative stress and reduced cell viability. Our findings suggest that pesticides, in general, interact with proteins resulting in the formation of cytotoxic conformers that may have implications in neurotoxicity and neurodegenerative diseases.


Assuntos
Clorpirifos , Praguicidas , Malato Desidrogenase , Praguicidas/toxicidade , Rotenona , alfa-Sinucleína
4.
J Ethnopharmacol ; 265: 113353, 2021 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-32891818

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Different plants are used for the treatment of various ailments and Acorus calamus L. is one such plant found in Western Himalaya. Rhizome of this plants has ethnomedicinal significance, as its rhizome is used for curing fever, pain and inflammation. An attempt has been made to alter the phytochemicals and increase its antioxidant property in a sustainable way with the help of mycorrhizal inoculation. AIM OF THE STUDY: Study of mycorrhizal (Funneliformis mosseae) impact on the biological activities and phytochemical profile of A. calamus L. rhizome and in silico studies of phytochemicals for their anti-inflammatory property. MATERIALS AND METHODS: F. mosseae was mass multiplied by single spore culture and then A. calamus rhizomes were inoculated with it. Antioxidant potential of rhizome extract was observed by DPPH and FRAP assays and the phytochemical profiling was done with GC-MS analysis. For observing antimicrobial activity disc diffusion method was employed. Dominant phytochemicals α-asarone and monolinolein TMS were chosen for molecular docking studies against four receptors (4COX, 2AZ5, 5I1B, 1ALU). RESULTS: There was increase in antioxidant activity of rhizome extract after mycorrhizal inoculation. However, no change in antimicrobial activity was observed in the plant after mycorrhizal inoculation. The comparison in phytochemicals was observed by GC-MS analysis which showed qualitative and quantitative variation in biochemical content in plants. The phytochemical, α-asarone and monolinolein TMS showed highest docking score and least binding energy against 1ALU and 4COX respectively for anti-inflammatory activity. CONCLUSION: Medicinal plants are potential source of antioxidants which can be increased by mycorrhizal inoculation without addition of chemical fertilizers and also results in altering the phytochemical composition.

5.
Artigo em Inglês | MEDLINE | ID: mdl-33273437

RESUMO

STUDY DESIGN: Retrospective review. OBJECTIVE: The aim of this study was to develop a surgical invasiveness index for metastatic spine tumor surgery (MSTS) that can serve as a standardized tool in predicting intraoperative blood loss and surgical duration; for the purpose of ascertaining resource requirements and aiding in patient education. SUMMARY OF BACKGROUND DATA: Magnitude of surgery is important in the metastatic spine disease (MSD) population since these patients have a continuing postoperative oncological process; a consideration that must be taken into account to maintain or improve quality of life. Surgical invasiveness indices have been established for general spine surgery, adult deformity, and cervical deformity, but not yet for spinal metastasis. METHODS: Demographic, oncological, and procedural data were collected from consecutive patients that underwent MSTS. Binary logistic regression, using median values for surgical duration and intraoperative estimated blood loss (EBL), was used to determine statistical significance of variables to be included in the "spinal metastasis invasiveness index" (SMII). The corresponding weightage of each of these variables was agreed upon by experienced spine surgeons. Multivariable regression analysis was used to predict operative time and EBL while controlling for demographical, procedural, and oncological characteristics. RESULTS: Two hundred and sixty-one MSD patients were included with a mean age of 59.7-years and near equal sex distribution. The SMII strongly predicted extended surgical duration (R = 0.28, P < 0.001) and high intraoperative blood loss (R = 0.18, P < 0.001). When compared to a previously established surgical invasiveness index, the SMII accounted for more variability in the outcomes. For every unit increase in score, there was a 42-mL increase in mean blood loss (P < 0.001) and 5-minute increase in mean operative time (P < 0.001). CONCLUSION: Long surgical duration and high blood loss were strongly predicted by the newly developed SMII. The use of the SMII may aid in preoperative risk assessment with the goal of improving patient outcomes and quality of life. LEVEL OF EVIDENCE: 4.

6.
Entropy (Basel) ; 22(4)2020 Apr 22.
Artigo em Inglês | MEDLINE | ID: mdl-33286255

RESUMO

The article studies the simulation-based mathematical modeling of bioheat transfer under the Dirichlet boundary condition. We used complex non-linear dual-phase-lag bioheat transfer (DPLBHT) for analyzing the temperature distribution in skin tissues during hyperthermia treatment of infected cells. The perfusion term, metabolic heat source, and external heat source were the three parts of the volumetric heat source that were used in the model. The non-linear DPLBHT model predicted a more accurate temperature within skin tissues. The finite element Runge-Kutta (4,5) (FERK (4,5)) method, which was based on two techniques, finite difference and Runge-Kutta (4,5), was applied for calculating the result in the case of our typical non-linear problem. The paper studies and presents the non-dimensional unit. Thermal damage of normal tissue was observed near zero during hyperthermia treatment. The effects of the non-dimensional time, non-dimensional space coordinate, location parameter, regional parameter, relaxation and thermalization time, metabolic heat source, associated metabolic heat source parameter, perfusion rate, associated perfusion heat source parameter, and external heat source coefficient on the dimensionless temperature profile were studied in detail during the hyperthermia treatment process.

7.
Asian Spine J ; 2020 Dec 02.
Artigo em Inglês | MEDLINE | ID: mdl-33260284

RESUMO

Study Design: Retrospective cohort study. Purpose: To identify the clinical significance of different patterns of intraoperative neuromonitoring (IONM) signal alerts. Overview of Literature: IONM is a long-established valuable adjunct to complex spine surgeries. IONM for cervical spine surgery is in the form of somatosensory evoked potential (SSEP) and motor evoked potential (MEP). The efficacy of both modalities (individually or in combination) to detect clinically significant neurological compromise is constantly being debated and requires conclusive suggestions. Methods: Clinical and neuromonitoring data of 207 consecutive adult patients who underwent cervical spine surgeries at multiple surgical centers using bimodal IONM were analyzed. Signal changes were divided into three groups. Group 0 had transient signal changes in either MEPs or SSEPs, group 1 had sustained unimodal changes, and group 2 had sustained changes in both MEPs and SSEPs. The incidences of true neurological deficits in each group were recorded. Results: A total of 25% (52/207) had IONM signal alerts. Out of these signal drops, 96% (50/52) were considered to be false positives. Groups 0 and 1 had no incidence of neurological deficits, while group 2 had a 29% (2/7) rate of true neurological deficits. The sensitivities of both MEP and SSEP were 100%. SSEP had a specificity of 96.6%, while MEP had a lower specificity at 76.6%. C5 palsy rate was 6%, and there was no correlation with IONM signal alerts (p=0.73). Conclusions: This study shows that we can better predict its clinical significance by dividing IONM signal drops into three groups. A sustained, bimodal (MEP and SSEP) signal drop had the highest risk of true neurological deficits and warrants a high level of caution. There were no clear risk factors for false-positive alerts but there was a trend toward patients with cervical myelopathy.

8.
Int J Mol Sci ; 21(23)2020 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-33261095

RESUMO

The use of metallic nanoparticles in engineering and biomedicine disciplines has gained considerable attention. Scientists are exploring new synthesis protocols of these substances considering their small size and lucrative antimicrobial potential. Among the most economical techniques of synthesis of metallic nanoparticles via chemical routes, which includes the use of chemicals as metal reducing agents, is considered to generate nanoparticles possessing toxicity and biological risk. This limitation of chemically synthesized nanoparticles has engendered the exploration for the ecofriendly synthesis process. Biological or green synthesis approaches have emerged as an effective solution to address the limitations of conventionally synthesized nanoparticles. Nanoparticles synthesized via biological entities obtained from plant extracts exhibit superior effect in comparison to chemical methods. Recently, conifer extracts have been found to be effective in synthesizing metallic nanoparticles through a highly regulated process. The current review highlights the importance of conifers and its extracts in synthesis of metallic nanoparticles. It also discusses the different applications of the conifer extract mediated metallic nanoparticles.

9.
Physiol Plant ; 2020 Dec 10.
Artigo em Inglês | MEDLINE | ID: mdl-33305409

RESUMO

Black pepper (Piper nigrum L.; 2n= 52; Piperaceae), the king of spices, is a perennial, trailing woody flowering vine and has global importance with widespread dietary, medicinal, and preservative uses. It is an economically-important germplasm cultivated for its fruit and the major cash crop in >30 tropical countries. Crop production is mainly affected by drought stress. The present study deals with the candidate gene identification from drought-affected black pepper leaf transcriptome generated by Illumina Hiseq2000. It also aims to mine putative molecular markers (namely SSRs, SNPs and InDels) and generate primers for them. The identification of transcription factors and pathways involved in drought tolerance is also reported here. De novo transcriptome assembly was performed with trinity assembler. In total, 4914 differential expressed genes, 2110 transcriptional factors, 786 domains and 1137 families, 20124 putative SSR markers and 259236 variants were identified. At2g30105 (unidentified gene containing leucine-rich repeats and ubiquitin-like domain), serine threonine protein kinase, Mitogen-activated protein kinase, NBS-LRR, Myeloblastosis related proteins, Basic helix-loop-helix are all found upregulated and are reported to be associated with plant tolerance against drought condition. All these information are catalogued in the Black Pepper Drought Transcriptome Database (BPDRTDb), freely accessible for academic use at http://webtom.cabgrid.res.in/bpdrtdb/. This database is a good foundation for the genetic improvement of pepper plants, breeding programmes and mapping population of this crop. Putative markers can also be a reliable genomic resource to develop drought-tolerant variety for better black pepper productivity. This article is protected by copyright. All rights reserved.

10.
Sci Rep ; 10(1): 21789, 2020 12 11.
Artigo em Inglês | MEDLINE | ID: mdl-33311512

RESUMO

Contemplating the exemplary benefits of pectin on human health, we precisely characterized and evaluated the antibacterial and anticancer activities from purified Mulberry Fruit Pectins (MFP). Here, we tested BR-2 and S-13 varieties of mulberry fruit pectins against six bacterial strains and two human cancer cell lines (HT-29 and Hep G-2), using MIC and an in vitro cell-based assay respectively. The BR-2 mulberry fruit pectin performs superior to S-13 by inhibiting strong bacterial growth (MIC = 500-1000 µg/mL) against tested bacterial strains and cytotoxic activities at the lowest concentration (10 µg/ml) against the Hep G-2 cell line. However, both tested drugs failed to exhibit cytotoxicity on the human colon cancer cell line (HT-29). Based on molecular interaction through docking, pectin binds effectively with the receptors (1e3g, 3t0c, 5czz, 6j7l, 6v40, 5ibs, 5zsy, and 6ggb) and proven to be a promising antimicrobial and anti-cancer agents. The pursuit of unexploited drugs from mulberry fruit pectin will potentially combat against bacterial and cancer diseases. Finally, future perspectives of MFP for the treatment of many chronic diseases will help immensely due to their therapeutic properties.

11.
Sci Rep ; 10(1): 21944, 2020 12 15.
Artigo em Inglês | MEDLINE | ID: mdl-33319787

RESUMO

Nutrient uptake by the rice-wheat cropping system (RWCS) is an important indicator of soil fertility and plant nutrient status. The hypothesis of this investigation was that the rate and sources of nutrient application can differentially influence nutrient removal and soil nutrient status in different crop establishment techniques (CETs). Cropping system yield was on par in all the CETs evaluated, however, there were significant changes in soil nutrient availability and microbiological aspects. The system nitrogen (N), phosphorus (P), potassium (K) and zinc (Zn) uptake in aerobic rice system followed by zero tillage wheat (ARS-ZTW) was 15.7-17.6 kg ha-1, 0.7-0.9 kg ha-1, 7-9.8 kg ha-1 and 13.5-23.1 g ha-1 and higher than other CETs. The formulations of Anabaena sp. (CR1) + Providencia sp. (PR3) consortium (MC1) and Anabaena-Pseudomonas biofilm (MC2) recorded significantly higher values of soil chlorophyll and microbial biomass carbon and positively affected cropping system nutrient uptake and soil nutrient balance, illustrating the beneficial effect of microbial inoculation through increased supply of biologically fixed N and solubilised P. Zinc fertilization (5 kg Zn ha-1 through ZnSO4·7H2O as soil application) increased soil DTPA-extractable Zn by 4.025-4.836 g ha-1, with enhancement to the tune of 20-24% after two cropping cycles of RWCS. Our investigation recommends the need for change in the present CETs to ARS-ZTW, along with the use of microbial inoculation as a means of significantly enhancing cropping system nutrient uptake and soil nutrient status improvement.

12.
Cochrane Database Syst Rev ; 12: CD012965, 2020 12 14.
Artigo em Inglês | MEDLINE | ID: mdl-33316083

RESUMO

BACKGROUND: Acute bronchiolitis is a significant burden on children, their families and healthcare facilities. It mostly affects children younger than two years of age. Treatment involves adequate hydration, humidified oxygen supplementation, and nebulisation of medications, such as salbutamol, epinephrine, and hypertonic saline. The effectiveness of magnesium sulphate for acute bronchiolitis is unclear. OBJECTIVES: To assess the effects of magnesium sulphate in acute bronchiolitis in children up to two years of age. SEARCH METHODS: We searched CENTRAL, MEDLINE, Embase, LILACS, CINAHL, and two trials registries to 30 April 2020. We contacted trial authors to identify additional studies. We searched conference proceedings and reference lists of retrieved articles. Unpublished and published studies were eligible for inclusion. SELECTION CRITERIA: Randomised controlled trials (RCTs) and quasi-RCTs, comparing magnesium sulphate, alone or with another treatment, with placebo or another treatment, in children up to two years old with acute bronchiolitis. Primary outcomes were time to recovery, mortality, and adverse events. Secondary outcomes were duration of hospital stay, clinical severity score at 0 to 24 hours and 25 to 48 hours after treatment, pulmonary function test, hospital readmission within 30 days, duration of mechanical ventilation, and duration of intensive care unit stay. DATA COLLECTION AND ANALYSIS: We used standard methodological procedures expected by Cochrane. We used GRADE methods to assess the certainty of the evidence. MAIN RESULTS: We included four RCTs (564 children). One study received funding from a hospital and one from a university; two studies did not report funding sources. Comparator interventions differed among all four trials. Studies were conducted in Qatar, Turkey, Iran, and India. We assessed two studies to be at an overall low risk of bias, and two to be at unclear risk of bias, overall. The certainty of the evidence for all outcomes and comparisons was very low except for one: hospital re-admission rate within 30 days of discharge for magnesium sulphate versus placebo. None of the studies measured time to recovery, duration of mechanical ventilation, duration of intensive care unit stay, or pulmonary function. There were no events of mortality or adverse effects for magnesium sulphate compared with placebo (1 RCT, 160 children). The effects of magnesium sulphate on clinical severity are uncertain (at 0 to 24 hours: mean difference (MD) on the Wang score 0.13, 95% confidence interval (CI) -0.28 to 0.54; and at 25 to 48 hours: MD on the Wang score -0.42, 95% CI -0.84 to -0.00). Magnesium sulphate may increase hospital re-admission rate within 30 days of discharge (risk ratio (RR) 3.16, 95% CI 1.20 to 8.27; 158 children; low-certainty evidence). None of our primary outcomes were measured for magnesium sulphate compared with hypertonic saline (1 RCT, 220 children). Effects were uncertain on the duration of hospital stay in days (MD 0.00, 95% CI -0.28 to 0.28), and on clinical severity on the Respiratory Distress Assessment Instrument (RDAI) score at 25 to 48 hours (MD 0.10, 95% CI -0.39 to 0.59). There were no events of mortality or adverse effects for magnesium sulphate, with or without salbutamol, compared with salbutamol (1 RCT, 57 children). Effects on the duration of hospital stay were uncertain (magnesium sulphate: 24 hours (95% CI 25.8 to 47.4), magnesium sulphate + salbutamol: 20 hours (95% CI 15.3 to 39.0), and salbutamol: 24 hours (95% CI 23.4 to 76.9)). None of our primary outcomes were measured for magnesium sulphate + epinephrine compared with no treatment or normal saline + epinephrine (1 RCT,120 children). Effects were uncertain for the duration of hospital stay in hours (MD -0.40, 95% CI -3.94 to 3.14), and for RDAI scores (0 to 24 hours: MD -0.20, 95% CI -1.06 to 0.66; and 25 to 48 hours: MD -0.90, 95% CI -1.75 to -0.05). AUTHORS' CONCLUSIONS: There is insufficient evidence to establish the efficacy and safety of magnesium sulphate for treating children up to two years of age with acute bronchiolitis. No evidence was available for time to recovery, duration of mechanical ventilation and intensive care unit stay, or pulmonary function. There was no information about adverse events for some comparisons. Well-designed RCTs to assess the effects of magnesium sulphate for children with acute bronchiolitis are needed. Important outcomes, such as time to recovery and adverse events should be measured.


Assuntos
Bronquiolite/tratamento farmacológico , Broncodilatadores/uso terapêutico , Sulfato de Magnésio/uso terapêutico , Doença Aguda , Albuterol/uso terapêutico , Viés , Broncodilatadores/administração & dosagem , Quimioterapia Combinada/métodos , Epinefrina/uso terapêutico , Humanos , Lactente , Recém-Nascido , Tempo de Internação , Sulfato de Magnésio/administração & dosagem , Readmissão do Paciente/estatística & dados numéricos , Placebos/uso terapêutico , Ensaios Clínicos Controlados Aleatórios como Assunto , Solução Salina/uso terapêutico , Índice de Gravidade de Doença
13.
Anal Bioanal Chem ; 2020 Nov 23.
Artigo em Inglês | MEDLINE | ID: mdl-33230700

RESUMO

Detection of hepatitis B Virus surface antigen (HBsAg) is an established method for diagnosing both acute and chronic hepatitis B virus (HBV) infection. In addition to enzyme immunoassays (EIAs), rapid diagnostic tests (RDTs) are available for the detection of HBsAg in resource-poor settings. However, the available RDTs have inadequate sensitivity and therefore are not suitable for diagnosis of patients with low levels of HBsAg and for blood screening. To provide a high-sensitivity RDT, we developed a lateral flow immunoassay (LFIA) for HBsAg utilizing upconverting nanoparticle (UCNP) reporter. The UCNP-LFIA can use whole blood, serum, or plasma and the results can be read in 30 min using a reader device. When compared with a commercial conventional visually read LFIA, the developed UCNP-LFIA had a Limit of Detection (LoD) of 0.1 IU HBsAg/ml in spiked serum, whereas the LoD of the conventional LFIA was 3.2 IU HBsAg/ml. The developed UCNP-LFIA fulfills the WHO criterion for blood screening (LoD ≤ 0.13 IU HBsAg/ml) in terms of LoD. The UCNP-LFIA and conventional LFIA were evaluated with well-characterized sample panels. The UCNP-LFIA detected 20/24 HBsAg-positive samples within the HBsAg Performance Panel and 8/10 samples within the Mixed Titer Performance Panel, whereas the conventional LFIA detected 8/24 and 4/10 samples in these panels, respectively. The performance of the assays was further evaluated with HBsAg-positive (n = 108) and HBsAg-negative (n = 315) patient samples. In comparison with a central laboratory test, UCNP-LFIA showed 95.4% (95% CI: 89.5-98.5%) sensitivity whereas sensitivity of the conventional LFIA was 87.7% (95%CI: 79.9-93.3%).

14.
Int J Mol Sci ; 21(22)2020 Nov 11.
Artigo em Inglês | MEDLINE | ID: mdl-33187086

RESUMO

Fruit extracts have natural bioactive molecules that are known to possess significant therapeutic potential. Traditionally, metallic nanoparticles were synthesized via chemical methods, in which the chemical act as the reducing agent. Later, these traditional metallic nanoparticles emerged as the biological risk, which prompted researchers to explore an eco-friendly approach. There are different eco-friendly methods employed for synthesizing these metallic nanoparticles via the usage of microbes and plants, primarily via fruit extract. These explorations have paved the way for using fruit extracts for developing nanoparticles, as they eliminate the usage of reducing and stabilizing agents. Metallic nanoparticles have gained significant attention, and are used for diverse biological applications. The present review discusses the potential activities of phytochemicals, and it intends to summarize the different metallic nanoparticles synthesized using fruit extracts and their associated pharmacological activities like anti-cancerous, antimicrobial, antioxidant and catalytic efficiency.

15.
Appl Radiat Isot ; : 109486, 2020 Oct 20.
Artigo em Inglês | MEDLINE | ID: mdl-33153893

RESUMO

Glucose is the renowned source of the energy for the cancer growth, that's the reason for [18F]FDG success and make it widely used radiotracer. Though [18F]FDG has its own inherent limitations therefore many tracers have been developed to target specific receptors, and other metabolic routes. We have used FX2C and FX2N Tracerlab modules for the synthesis of the [11C]methionine, [18F]choline and [18F]fluorodopa via nucleophilic pathway in FX2C/N module. [11C]methionine was standardized in FX2C module using two different precursors, and purified using C18 cartridge based technique. [18F]methylcholine was synthesized using dimethylaminoethanol precursor and purified using cartridge-based method. [18F]fluorodopa was synthesized using nucleophilic precursor and purified using in-built preparative HPLC on FX2N module. All radioactive intermediates and chemical impurities were evaluated by analytical HPLC. The radiochemical purity of D and L-[11C]methionine were 4.6 ± 3.2% and 95.4 ± 3.6% while other chemical impurities were less than prescribed limits with yield of 20 ± 5%. [18F]fluoromethylcholine was prepared with high radiochemical purity of 97.3 ± 2.6% with yield of 8 ± 3%. [18F]fluorodopa was synthesized with high radiochemical purity of 95.8 ± 1.4% with 15 ± 3% yield. The adaptation of [18F]fluorodopa synthesis to FX2N module via designing synthesis sequence and purified through on-line HPLC has provided high radiochemical purity. PET-MR imaging was done using these tracers which have validated the synthesis and their availability for future clinical applications.

16.
J Family Med Prim Care ; 9(9): 4507-4511, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-33209753

RESUMO

Background: Lockdown effectively can only result in relative freezing of populations that is expected to slow down the disease spread rather than zeroing it. Flattening of epidemic curve Current analysis was carried out to observe a pattern in the rise of CoVID-19 cases along with concurrent announcements of strategies to control the spread of disease. Material and Methods: Data in from of daily number of cases and issued notifications were studied from the official website of Government of India from 30/01/2020 to 03/05/2020. Qualitative assessment with thematic analysis was carried out for notifications issued by the government. The fit to data on cumulative cases was observed with R2 and checked for linearity, logarithmic, polynomial, and exponential growth. Daily growth fraction (Gt) was calculated based on the difference between current and previous number of cases, thereafter daily doubling time (Td(t)) was estimated. Results: Daily reported cases were entered and cumulative growth of cases observed with a polynomial increasing pattern (third-order) with better fit (R2: 0.999). Total 108 notifications were issued, and as compared to phase-0 and 1 (87.0%), few (12.9%) notifications were issued in phase-2 of study period. As compared to phase-0 and 1, rising trend of cumulative cases and Td(t) was high in phase-2. Conclusion: Across phases of lockdown along with a rising trend of COVID-19 cases, the country has managed to increase the doubling time of cases with an effort to flatten the epidemic curve.

17.
Pharmacol Res Perspect ; 8(6): e00678, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33135390

RESUMO

Lemborexant is a dual orexin receptor antagonist approved for treating insomnia. As the solubility of lemborexant is pH-sensitive, the impact of the gastric acid-reducing agent (ARA), famotidine, on lemborexant pharmacokinetics was evaluated in a Phase 1 study. Additionally, post hoc analysis of data from Phase 3 studies examined the potential effect of concomitant ARAs on patient-reported/subjective sleep onset latency (sSOL) in subjects with insomnia. Coadministration of lemborexant 10 mg with famotidine decreased the maximum observed concentration by 27% and delayed time of maximum observed concentration by 0.5 hours. Famotidine did not affect overall lemborexant exposure based on comparison of area under the concentration curves. Concomitant ARA use in the Phase 3 studies did not impact the effect of lemborexant on sSOL; the change from baseline during the last 7 nights of 1 month of treatment with lemborexant 10 mg was -17.1 minutes with vs -17.9 minutes without ARAs. Collectively, these results indicate that lemborexant can be coadministered with ARAs.

18.
Int J Mol Sci ; 21(21)2020 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-33142948

RESUMO

Although feed cost is the greatest concern in aquaculture, the inclusion of carbohydrates in the fish diet, and their assimilation, are still not well understood in aquaculture species. We identified molecular events that occur due to the inclusion of high carbohydrate levels in the diets of genetically improved 'Jayanti rohu' Labeo rohita. To reveal transcriptional changes in the liver of rohu, a feeding experiment was conducted with three doses of gelatinized starch (20% (control), 40%, and 60%). Transcriptome sequencing revealed totals of 15,232 (4464 up- and 4343 down-regulated) and 15,360 (4478 up- and 4171 down-regulated) differentially expressed genes. Up-regulated transcripts associated with glucose metabolisms, such as hexokinase, PHK, glycogen synthase and PGK, were found in fish fed diets with high starch levels. Interestingly, a de novo lipogenesis mechanism was found to be enriched in the livers of treated fish due to up-regulated transcripts such as FAS, ACCα, and PPARγ. The insulin signaling pathways with enriched PPAR and mTOR were identified by Kyoto Encyclopedia of Genes and Genome (KEGG) as a result of high carbohydrates. This work revealed for the first time the atypical regulation transcripts associated with glucose metabolism and lipogenesis in the livers of Jayanti rohu due to the inclusion of high carbohydrate levels in the diet. This study also encourages the exploration of early nutritional programming for enhancing glucose efficiency in carp species, for sustainable and cost-effective aquaculture production.

19.
Eur J Med Chem ; : 112844, 2020 Sep 17.
Artigo em Inglês | MEDLINE | ID: mdl-33143937

RESUMO

'Epigenetic' regulation of genes via post-translational modulation of proteins is the current mainstay approach for the disease therapies, particularly explored in the Histone Deacetylase (HDAC) class of enzymes. Mainly sight saw in cancer chemotherapeutics, HDAC inhibitors have also found a promising role in other diseases (neurodegenerative disorders, cardiovascular diseases, and viral infections) and successfully entered in various combination therapies (pre-clinical/clinical stages). The prevalent flexibility in the structural design of HDAC inhibitors makes them easily tuneable to merge with other pharmacophore modules for generating multi-targeted single hybrids as a novel tactic to overcome drawbacks of polypharmacy. Herein, we reviewed the putative role of prevalent HDAC hybrids inhibitors in the current and prospective stage as a translational approach to overcome the limitations of the existing conventional drug candidates (parent molecule) when used either alone (drug resistance, solubility issues, adverse side effects, selectivity profile) or in combination (pharmacokinetic interactions, patient compliance) for treating various diseases.

20.
Antioxidants (Basel) ; 9(11)2020 Nov 13.
Artigo em Inglês | MEDLINE | ID: mdl-33202871

RESUMO

Aging is a complicated biological process in which functional and structural alterations in a living organism take place over time. Reactive oxygen species is one of the main factors responsible for aging and is associated with several chronic pathologies. The relationship between aging and diet is quite interesting and has attained worldwide attention. Healthy food, in addition to dietary antioxidants, are required to delay the process of aging and improve the quality of life. Many healthy foods such as fruits are a good source of dietary nutrients and natural bioactive compounds which have antioxidant properties and are involved in preventing aging and other age-related disorders. Health benefits linked with healthy consumption of fruit have drawn increased interest. A significant number of studies have documented the advantages of fruit intake, as it suppresses free-radical development that further reduces the oxidative stress created in the body and protects against several types of diseases such as cancer, type 2 diabetes, inflammatory disorders, and other cardiovascular diseases that ultimately prevent aging. In addition, fruits have numerous other properties like anti-inflammatory, anti-cancerous, anti-diabetic, neuroprotective, and have health-promoting effects. Mechanisms of various bioactive compounds that aids in preventing various diseases and increases longevity are also described. This manuscript provides a summary of various bioactive components present in fruits along with their health-promoting and antiaging properties.

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