Mono-metallic, Bi-metallic and Tri-metallic Biogenic Nanoparticles Derived from Garlic and Ginger with their Applications

Biogenic metallic nanoparticles (NPs) produced from garlic and ginger have a wide range of applications in the pharmaceuticals, biotechnology and electronics industries. Despite many commercial NPs reported, NPs made from natural extracts are more affordable, straightforward and environmentally friendly than synthetic ap-proaches. Biogenic metallic NPs derived from garlic and ginger have superior biocompatibility, better dispersion, higher stability, and stronger biological activities. This is due to the fact that garlic and ginger possess significant activities against multi-drug resisted pathogens and are in high demand, especially for the prevention of microbial diseases. This review placed a substantial emphasis on comparative investigations of the synthesis of mono-, bi-, and tri-metallic NPs with a variety of sizes and forms, as well as applications using materials like ginger and garlic. The benefits and drawbacks of mono-metallic, bi-metallic, and tri-metallic biogenic NPs produced from garlic and ginger are also comprehensively highlighted. Recent improvements have opened the way to site-specific targeting and drug delivery by these metallic NPs

Biological Activity and Characterization of Bioactive Compounds under Lead Induced Stress in Maize

Background: Lead is most commonly released environmental contaminant making its way to air, soils and water. It causes hormonal imbalance and over production of reactive oxygen in plants when absorbed through leaves and roots. It contaminates the ground water depending on the type of soils and characteristics of lead. Plants ability to tolerate lead is linked with cell wall potential, activation of antioxidants defense mechanism and synthesis of osmolytes.Methods: The study was designed to evaluate the effects of Pb(NO3)2 induced stress on biological activity and bioactive compounds in maize. The plants were subjected under two different lead concentrations (T1- 0.35mg/ml and T2- 0.45mg/ml). Phytochemical screening revealed the presence of alkaloids, coumarins, saponins, tannins and terpenoids in maize. Total Phenolic Content (TPC) was increased (T1- 45%, T2- 58.42%) under lead stress when compared with control (36.29%). The cytotoxicity was checked using hemolytic activity against human red blood cells.Results: The scavenging rate was highest (T1- 33.5%, T2- 52%) when compared with control (18.6%). Zone of inhibition of Aspergillus niger was highest amongst other fungal strains. The HPLC results showed that maize has some phyto-ingredients which may be accountable for cell reinforcement and anti-microbial activity. The extracts were further analyzed for the biochemical profile like superoxide dismutase, peroxidase, catalase, amylase and protease. Escherichia colishowed maximum activity with control (25±3.46mm) and maximum under stress (T1- 17±1.633 mm, T2- 20±4.08 mm).Conclusion: Lead stress altered all the activities when compared to control plants. In conclusion, Maize can be used as a potential indicator for lead and other compounds to play a vital role in phytoremediation. The results would further lead to find the new compounds and plant mechanism to cope with stress.

Experimentally Validated Pharmacoinformatics Approach to Predict hERG Inhibition Potential of New Chemical Entities

The hERG (human ether-a-go-go-related gene) encoded potassium ion (K+) channel plays a major role in cardiac repolarization. Drug-induced blockade of hERG has been a major cause of potentially lethal ventricular tachycardia termed Torsades de Pointes (TdPs). Therefore, we presented a pharmacoinformatics strategy using combined ligand and structure based models for the prediction of hERG inhibition potential (IC50) of new chemical entities (NCEs) during early stages of drug design and development. Integrated GRid-INdependent Descriptor (GRIND) models, and lipophilic efficiency (LipE), ligand efficiency (LE) guided template selection for the structure based pharmacophore models have been used for virtual screening and subsequent hERG activity (pIC50) prediction of identified hits. Finally selected two hits were experimentally evaluated for hERG inhibition potential (pIC50) using whole cell patch clamp assay. Overall, our results demonstrate a difference of less than ±1.6 log unit between experimentally determined and predicted hERG inhibition potential (IC50) of the selected hits. This revealed predictive ability and robustness of our models and could help in correctly rank the potency order (lower μM to higher nM range) against hERG

Experimentally Validated Pharmacoinformatics Approach to Predict hERG Inhibition Potential of New Chemical Entities

The hERG (human ether-a-go-go-related gene) encoded potassium ion (K+) channel plays a major role in cardiac repolarization. Drug-induced blockade of hERG has been a major cause of potentially lethal ventricular tachycardia termed Torsades de Pointes (TdPs). Therefore, we presented a pharmacoinformatics strategy using combined ligand and structure based models for the prediction of hERG inhibition potential (IC50) of new chemical entities (NCEs) during early stages of drug design and development. Integrated GRid-INdependent Descriptor (GRIND) models, and lipophilic efficiency (LipE), ligand efficiency (LE) guided template selection for the structure based pharmacophore models have been used for virtual screening and subsequent hERG activity (pIC50) prediction of identified hits. Finally selected two hits were experimentally evaluated for hERG inhibition potential (pIC50) using whole cell patch clamp assay. Overall, our results demonstrate a difference of less than ±1.6 log unit between experimentally determined and predicted hERG inhibition potential (IC50) of the selected hits. This revealed predictive ability and robustness of our models and could help in correctly rank the potency order (lower μM to higher nM range) against hERG

Preparation, Characterization and Application of Vitamin-E fortified Nanocoatings on Fresh-cut Apples

Fresh-cut apples have a very low shelf life due to high vulnerability to oxidation in open air. The aim of the present work was to prepare enriched nanocoatings to increase not only the shelf life of the fruit, but to add to it nutritive values as well. Hence, four different edible coatings were prepared containing vitamin-E nanoemulsion. Vitamin-E nanoemulsion was successfully prepared by EPI (Emulsion Phase Inversion) method and the particles size distribution was checked by DLS (Dynamic Light Scattering) method. Potassium Sorbate and Calcium Chloride were added, respectively, as antimicrobial and antioxidant agents. In one coating, fresh lemon juice was used in place of ascorbic acid for comparison. To reduce respiration and water vapor permeability, methyl cellulose and stearic acid were added in different ratios to all the four coatings. Prepared coatings were then applied on freshly-cut apple pieces using dip method. Various characterization parameters were performed to analyze the quality of vitamin-E fortified edible nanocoatings such as weight loss, titrateable acidity, total soluble solids, and total phenolics for two weeks. In addition, antimicrobial activity of the prepared edible coatings was done using LBA (Luria Bertani Agar) culture media. All the coatings showed good results but the coating containing fresh lemon juice gave comparatively better results

Breast cancer detection using forward scattering radar technique

This paper presents an initial investigation for breast cancer detection using a special mode of bistatic radar system known as forward scattering radar (FSR). The proposed method analyzes the Doppler frequency in the received signal scattered from the tumor for cancer detection and localization. Three systems of architectures were analyzed which determined by the mechanical movement of transmitter or receiver or both. This paper also discusses an initial simulated result by using CST Microwave Studio as a feasibility study of utilizing FSR for breast cancer detection. It is shown that by investigating the unique character of Radar Cross Section (RCS) for breast tissue and tumor of FSR a cancer can be predicted. Electromagnetic model including fatty tissue and a tumor were simulated to obtain RCS parameter and analyzed as well as compared with whose fatty tissue without cancerous lesion to pinpoint the presence of tumor from its FSR signature. The result shows a significant different between these two models in FS RCS

Effect of biochar modified with magnetite nanoparticles and HNO\u3csub\u3e3\u3c/sub\u3e for efficient removal of Cr(VI) from contaminated water: A batch and column scale study

© 2020 Elsevier Ltd Chromium (Cr) poses serious consequences on human and animal health due to its potential carcinogenicity. The present study aims at preparing a novel biochar derived from Chenopodium quinoa crop residues (QBC), its activation with magnetite nanoparticles (QBC/MNPs) and strong acid HNO3 (QBC/Acid) to evaluate their batch and column scale potential to remove Cr (VI) from polluted water. The QBC, QBC/MNPs and QBC/Acid were characterized with SEM, FTIR, EDX, XRD as well as point of zero charge (PZC) to get an insight into their adsorption mechanism. The impact of different process parameters including dose of the adsorbent (1–4 g/L), contact time (0–180 min), initial concentration of Cr (25–200 mg/L) as well as solution pH (2–8) was evaluated on the Cr (VI) removal from contaminated water. The results revealed that QBC/MNPs proved more effective (73.35–93.62-%) for the Cr (VI) removal with 77.35 mg/g adsorption capacity as compared with QBC/Acid (55.85–79.8%) and QBC (48.85–75.28-%) when Cr concentration was changed from 200 to 25 mg/L. The isothermal experimental results follow the Freundlich adsorption model rather than Langmuir, Temkin and Dubinin-Radushkevich adsorption isotherm models. While kinetic adsorption results were well demonstrated by pseudo second order kinetic model. Column scale experiments conducted at steady state exhibited excellent retention of Cr (VI) by QBC, QBC/MNPs and QBC/Acid at 50 and 100 mg Cr/L. The results showed that this novel biochar (QBC) and its modified forms (QBC/Acid and QBC/MNPs) are applicable with excellent reusability and stability under acidic conditions for the practical treatment of Cr (VI) contaminated water

Effect of early tranexamic acid administration on mortality, hysterectomy, and other morbidities in women with post-partum haemorrhage (WOMAN): an international, randomised, double-blind, placebo-controlled trial

Background Post-partum haemorrhage is the leading cause of maternal death worldwide. Early administration of tranexamic acid reduces deaths due to bleeding in trauma patients. We aimed to assess the effects of early administration of tranexamic acid on death, hysterectomy, and other relevant outcomes in women with post-partum haemorrhage. Methods In this randomised, double-blind, placebo-controlled trial, we recruited women aged 16 years and older with a clinical diagnosis of post-partum haemorrhage after a vaginal birth or caesarean section from 193 hospitals in 21 countries. We randomly assigned women to receive either 1 g intravenous tranexamic acid or matching placebo in addition to usual care. If bleeding continued after 30 min, or stopped and restarted within 24 h of the first dose, a second dose of 1 g of tranexamic acid or placebo could be given. Patients were assigned by selection of a numbered treatment pack from a box containing eight numbered packs that were identical apart from the pack number. Participants, care givers, and those assessing outcomes were masked to allocation. We originally planned to enrol 15 000 women with a composite primary endpoint of death from all-causes or hysterectomy within 42 days of giving birth. However, during the trial it became apparent that the decision to conduct a hysterectomy was often made at the same time as randomisation. Although tranexamic acid could influence the risk of death in these cases, it could not affect the risk of hysterectomy. We therefore increased the sample size from 15 000 to 20 000 women in order to estimate the effect of tranexamic acid on the risk of death from post-partum haemorrhage. All analyses were done on an intention-to-treat basis. This trial is registered with ISRCTN76912190 (Dec 8, 2008); ClinicalTrials.gov, number NCT00872469; and PACTR201007000192283. Findings Between March, 2010, and April, 2016, 20 060 women were enrolled and randomly assigned to receive tranexamic acid (n=10 051) or placebo (n=10 009), of whom 10 036 and 9985, respectively, were included in the analysis. Death due to bleeding was significantly reduced in women given tranexamic acid (155 [1·5%] of 10 036 patients vs 191 [1·9%] of 9985 in the placebo group, risk ratio [RR] 0·81, 95% CI 0·65–1·00; p=0·045), especially in women given treatment within 3 h of giving birth (89 [1·2%] in the tranexamic acid group vs 127 [1·7%] in the placebo group, RR 0·69, 95% CI 0·52–0·91; p=0·008). All other causes of death did not differ significantly by group. Hysterectomy was not reduced with tranexamic acid (358 [3·6%] patients in the tranexamic acid group vs 351 [3·5%] in the placebo group, RR 1·02, 95% CI 0·88–1·07; p=0·84). The composite primary endpoint of death from all causes or hysterectomy was not reduced with tranexamic acid (534 [5·3%] deaths or hysterectomies in the tranexamic acid group vs 546 [5·5%] in the placebo group, RR 0·97, 95% CI 0·87-1·09; p=0·65). Adverse events (including thromboembolic events) did not differ significantly in the tranexamic acid versus placebo group. Interpretation Tranexamic acid reduces death due to bleeding in women with post-partum haemorrhage with no adverse effects. When used as a treatment for postpartum haemorrhage, tranexamic acid should be given as soon as possible after bleeding onset. Funding London School of Hygiene & Tropical Medicine, Pfizer, UK Department of Health, Wellcome Trust, and Bill & Melinda Gates Foundation

Molecular Docking Guided Grid-Independent Descriptor Analysis to Probe the Impact of Water Molecules on Conformational Changes of hERG Inhibitors in Drug Trapping Phenomenon

Human ether a-go-go related gene (hERG) or KV11.1 potassium channels mediate the rapid delayed rectifier current (IKr) in cardiac myocytes. Drug-induced inhibition of hERG channels has been implicated in the development of acquired long QT syndrome type (aLQTS) and fatal arrhythmias. Several marketed drugs have been withdrawn for this reason. Therefore, there is considerable interest in developing better tests for predicting drugs which can block the hERG channel. The drug-binding pocket in hERG channels, which lies below the selectivity filter, normally contains K+ ions and water molecules. In this study, we test the hypothesis that these water molecules impact drug binding to hERG. We developed 3D QSAR models based on alignment independent descriptors (GRIND) using docked ligands in open and closed conformations of hERG in the presence (solvated) and absence (non-solvated) of water molecules. The ligand–protein interaction fingerprints (PLIF) scheme was used to summarize and compare the interactions. All models delineated similar 3D hERG binding features, however, small deviations of about ~0.4 Å were observed between important hotspots of molecular interaction fields (MIFs) between solvated and non-solvated hERG models. These small changes in conformations do not affect the performance and predictive power of the model to any significant extent. The model that exhibits the best statistical values was attained with a cryo_EM structure of the hERG channel in open state without water. This model also showed the best R2 of 0.58 and 0.51 for the internal and external validation test sets respectively. Our results suggest that the inclusion of water molecules during the docking process has little effect on conformations and this conformational change does not impact the predictive ability of the 3D QSAR models

Two Pot and One Pot Synthetic Methodologies of Hantzsch Pyridines

Hantzsch pyridines are conspicuous nitrogen-holding heterocyclic compounds and different procedures have been worked out for their synthesis. Hantzsch pyridines have a variety of methods for their synthesis but according to the literature survey, two pot synthetic route is more developed than one pot due to a vast variety of catalysts becoming cheap, economical, eco-friendly and recyclable. However, researchers synthesized Hantzsch pyridines under different methodologies due to the molecule’s reactivity and requirement of the chemist. An up-to-date first review related to the two pot and one pot synthetic methodologies of Hantzsch pyridines gives the most valuable basic skeleton to derive the biologically active compounds, which are frequently used in the pharmacological field. The main objective of this review is to explore all the synthetic modifications in its methodologies, which are fruitful, especially for the synthetic chemists and therapeutical industry