Development of stable emulsified formulations of Terminalia arjuna for topical application: evaluation of antioxidant activity of final product and molecular docking study

Abstract

Objective: The aim of this work was to develop stable emulsified formulations containing Terminalia arjuna (T. arjuna) extract and to assess antioxidant potential of the final product with in silico molecular screening.

Methods: Terminalia arjuna emulsified formulations were prepared by application of ternary phase diagram design and were evaluated for phytochemical screening, solubility studies, ex vivo permeation study, DPPH free radical scavenging assay, anti-tyrosinase activity, skin irritation, stability studies, molecular docking study, and pharmacophore modeling.

Results: Phytochemical screening resulted in the presence of secondary metabolites. The result of the solubility study exhibited that olive oil, tween 80, and PEG 400 could be the most appropriate combination for preparation of the emulsified system. The ex vivo study showed adequate release from its emulsified formulation. Globule size determination and Zeta potential analysis indicate the stability of the emulsified system. The result of DPPH free radical scavenging activity and anti-tyrosinase activity of the final product were satisfactory. Skin irritation test on albino rats resulted in no allergic dermal effects. All the prepared formulations were found to be stable upon storage for 3?months. Molecular docking resulted in antioxidant potential via tyrosinase inhibitory mechanism mainly by hydrogen bonding interaction with His60B, Glu158B, His208B, Asn205B, Met215B, His42B, and Asn57B whereas ionic interactions by Arg209B and Val218B of tyrosinase. Pharmacophore modeling describes the similarity features with the standard.

Conclusions: The results suggest that developed emulsified formulations with T. arjuna extract for topical application demonstrate interesting attributes to be explored as potential pharmaceutical products.     

Tuning of PEM fuel cell model parameters for prediction of steady state and dynamic performance under various operating conditions

Many models are available with various degrees of complexity to study the behaviour of Proton Exchange Membrane Fuel Cells (PEMFC) under varying operating conditions. To our knowledge no model has been developed from single cells to multiple cells with increased electrode area for PEMFC stacks along with power conditioners, by considering the dynamic characteristics of the fuel cells under the influence of stoichiometry, humidity ratio and their response during their integration with power conditioners. We have developed a model using Matlab to study the transient response of the cell for 30 cm², which has been extended to a multicell stack of 1.2 kW capacity of electrode area 150 cm². The developed model has been validated using PEMFC single cells and stacks, by considering partial pressure of hydrogen, oxygen, and water as three states, anode fuel utilization and all three losses. This model is proposed to evaluate the transient response of all the stacks developed at Centre for Fuel Cell Technology (CFCT) ranging from a few watts to 10 kW that are integrated with various power conditioners depending on the applications.     

A New Stability–Indicating RP-HPLC Method to Determine Assay and Known Impurity of Celecoxib API

ABSTRACT

A simple, rapid and accurate Reverse Phase High-Performance Liquid Chromatography (RP-HPLC) method was developed to determine assay and known impurity of Celecoxib API. The chromatographic separation was performed on reversed-phase C-18 column. Eluents were monitored on photo-diode array detector at a wavelength of 254 nm using a mixture (40:60) of buffer and acetonitrile. Solution concentrations were measured on a weight basis to avoid the use of an internal standard. The method was statistically validated for forced-degradation study, linearity and range, accuracy, precision, stability of analytical solutions, and selectivity. Due to its simplicity, rapid, and accuracy, we believe that the method will be useful to determine assay and known impurity of Celecoxib.     

Chemical,biochemical, and biological significance of polyphenols in cereals and legumes

Polyphenols in cereals and legumes have been receiving considerable attention largely because of their adverse influence on color, flavor, and nutritional quality. These compounds belong to the flavonoid and tannin groups and are mostly located in the seed coat or pericarp of the grains. The pearl millet flavonoids have been identified as C‐glycosylflavones by the combined use of paper chromatography and UV spectroscopy. Although nontoxic, physiological and nutritional significance of these compounds occurring in high amounts in the pearl millet grain are still not clearly understood. In view of aesthetic quality, bleaching of the millet grains in acidic solution is recommended. A large proportion of current assays involves spectrophotometry of tannin or its chromogen and tannin‐protein interaction. Sorghum and legume tannins have been characterized as condensed tannins. Several factors such as plant type, age of the plant or plant parts, stage of development, and environmental conditions govern the polyphenol contents in plants. Polyphenols are known to interact with proteins and form tannin‐protein complexes leading to either inactivation of enzymes or making proteins insoluble. These are implicated in decreasing the activities of digestive enzymes, protein and amino acid availabilities, mineral uptake, vitamin metabolism, and depression of growth. Polyphenols are known to cause certain ultrastructural changes in the different parts of experimental animals. A correlation between dietary tannins and occurrence of esophageal cancer has been established. Bird resistance and seed germination in food crops have been correlated to high contents of polyphenols. The antinutritional activity of polyphenols can be reduced by removing polyphenols from the grains by chemical treatments or removing pericarp and testa by pearling. Treatment of alkaline reagents and ammonia can remove 90% of the polyphenols. Supplementation of polyphenols‐rich diet with protein can alleviate the growth‐depressing effect of polyphenols.     

Singlet exciton fission in nanostructured organic solar cells

Singlet exciton fission is an efficient multiexciton generation process in organic molecules. But two concerns must be satisfied before it can be exploited in low-cost solution-processed organic solar cells. Fission must be combined with longer wavelength absorption in a structure that can potentially surpass the single junction limit, and its efficiency must be demonstrated in nanoscale domains within blended devices. Here, we report organic solar cells comprised of tetracene, copper phthalocyanine, and the buckyball C(60). Short wavelength light generates singlet excitons in tetracene. These are subsequently split into two triplet excitons and transported through the phthalocyanine. In addition, the phthalocyanine absorbs photons below the singlet exciton energy of tetracene. To test tetracene in nanostructured blends, we fabricate coevaporated bulk heterojunctions and multilayer heterojunctions of tetracene and C(60). We measure a singlet fission efficiency of (71 ± 18)%, demonstrating that exciton fission can efficiently compete with exciton dissociation on the nanoscale.     

Iterative Antimicrobial Candidate Selection from Informed D‐/L‐Peptide Dimer Libraries

Growing resistance to antibiotics, as well as newly emerging pathogens, stimulate the investigation of antimicrobial peptides (AMPs) as therapeutic agents. Here, we report a new library design concept based on a stochastic distribution of natural AMP amino acid sequences onto half‐length synthetic peptides. For these compounds, a non‐natural motif of alternating D ‐ and L ‐backbone stereochemistry of the peptide chain predisposed for β‐helix formation was explored. Synthetic D ‐/L ‐peptides with permuted half‐length sequences were delineated from a full‐length starter sequence and covalently recombined to create two‐dimensional compound arrays for antibacterial screening. Using the natural AMP magainin as a seed sequence, we identified and iteratively optimized hit compounds showing high antimicrobial activity against Gram‐positive and Gram‐negative bacteria with low hemolytic activity. Cryo‐electron microscopy characterized the membrane‐associated mechanism of action of the new D ‐/L ‐peptide antibiotics.     

Stress relaxation behavior of composite and eutectic Sn-Ag solder joints

Stress relaxation experiments were carried out at 25 C and 150 C on 96.5Sn-3.5Ag eutectic solder and Sn-Ag composite solder joints (Sn-Ag eutectic solder with 20 vol.% Cu₆Sn₅ reinforcements incorporated by in-situ methods). The magnitude of the stress drop during relaxation depends primarily upon the plastic shear strain imposed prior to the stress relaxation process. For sequential stress relaxation experiments that include unloading, the stress drop is nearly independent of the accumulated plastic shear strain. However, for sequential stress relaxation that does not include unloading, the stress relaxation is more dependent upon the cumulative plastic shear strain history. The stress in single shear lap joints does not relax to zero stress, as is observed in stress relaxation of bulk tension specimens, even at 150 C. Creep strain rates extracted from the relaxation data were much lower with smaller pre-strains in both eutectic Sn-Ag and composite solder joints. The stress exponent values (n) calculated from the stress relaxation test data ranged from 7 to 15 for both eutectic and composite solder joints, which were consistent with conventional creep data. These stress-relaxation behaviors can be explained on the basis of dislocation recovery processes that occur during relaxation and when specimens are unloaded.     

Ecofriendly biodegradation and detoxification of Reactive Red 2 textile dye by newly isolated Pseudomonas sp. SUK1

The aim of this work is to evaluate textile dyes degradation by novel bacterial strain isolated from the waste disposal sites of local textile industries. Detailed taxonomic studies identified the organisms as Pseudomonas species and designated as strain Pseudomonas sp. SUK1. The isolate was able to decolorize sulfonated azo dye (Reactive Red 2) in a wide range (up to 5 g l(-1)), at temperature 30 degrees C, and pH range 6.2-7.5 in static condition. This isolate also showed decolorization of the media containing a mixture of dyes. Measurements of COD were done at regular intervals to have an idea of mineralization, showing 52% reduction in the COD within 24h. Induction in the activity of lignin peroxidase and azoreductase was observed during decolorization of Reactive Red 2 in the batch culture, which represented their role in degradation. The biodegradation was monitored by UV-vis, IR spectroscopy, HPLC. The final product, 2-naphthol was characterized by GC-mass spectroscopy. The phytotoxicity study revealed the degradation of Reactive Red 2 into non-toxic product by Pseudomonas sp. SUK1.     

Lanthanum(Ⅲ) sorption studies on poly[dibenzo-18-crown-6] and its separation from uranium(Ⅵ) and thorium(Ⅳ) in L-valine medium

The sorption study of La(Ⅲ) was carried out on poly[dibenzo-18-crown-6] and L-valine medium. The quantitative adsorption of La(Ⅲ) was found at 1x10-2 to 1x10-5 mol/L L-valine. The various eluting agents were found efficient eluents for La(Ⅲ). The capacity of crown polymer for La(Ⅲ) was found to be 0.43 ±0.01 mmol/g. The tolerance limit of various cations and anions for La(Ⅲ) was determined.La(Ⅲ) was quantitatively separated from other metal ions in binary as well as multicomponont mixtures. The study was extended to sequen-tial separation of La(Ⅲ), U(Ⅵ) and Th(Ⅳ). The good separation yields were obtained and had good reproducibility (±2%). The method in-corporated the determination of La(Ⅲ) in real sample. The method was simple, rapid and selective.