Spectrochemical Investigation of di methoxy Aniline Dithiocarbamate metal complexes-Biological activity

Dithiocarbomates are a class of sulfur-based metal-chelating compounds commonly used in industry, agriculture, and medicine. 2,6 di methoxy Aniline dithiocarbamate  Complexes of Copper and Ruthenium have been prepared  and Characterized by Spectroscopic methods like IR,NMR and also analysis of Biological activity. The investigation of these complexes confirmed that the stability of metal–ligands coordination through, S & S,N atoms as bidendate chelates.

Synthesis, Characterization and Biological activities of 2-Amino-3-Methyl pyridine New Dithiocarbamate metal complexes

Dithiocarbamates are a class of sulfur-based metal-chelating compounds with various applications in medicine. A new series of new transition metal [Cu(II), and Ni(II)] complexes of dithiocarbamates were synthesized from 2-Amino-3-Methyl pyridine and Carbon disulfide and further characterized. The investigation of these complexes confirmed that the stability of metal–ligands coordination through, S&S,N atoms as bidendate chelates.. It is necessary to understand the binding properties in developing new potential Protein targeting against neurological disorders. Keywords:2-Amino-3-Methylpyridine,MetalComplexes,Dithiocarbamates,neurological disorders

Response of cardamom (Elettaria cardamomum Maton) seedlings to vesicular arbuscular mycorrhizal fungi

The growth response of cardamom (Elettaria cardamomum) seedlings (cv, Malabar) to 13 different vesicular arbuscular mycorrhizal fungi was tested under mat house conditions at Bangalore, India, In general, seedlings inoulated with the fungi grew taller, had more number of leaves and tillers, increased seedling biomass and uptake of nutrients compared to control seedlings, Among the various mycorrhizal fungi tested, seedlings inoculated with Gigaspora margarita and Glomus monosporum exhibited significantly higher growth with increased uptake of nutrients, &nbsp

Formulation Development of Losartan Potassium Microspheres Using Natural Polysaccharides and Their In-Vitro Evaluation

ABSTRACT The present work is regarding formulation and development of Losartan potassium microspheres using chitosan and guar gum as release retarding natural polysaccharides and their in vitro evaluation. Losartan potassium is used as antihypertensive belonging to angiotensin antagonist. Losartan potassium was successfully encapsulated into chitosan and guar gum microspheres. Totally nine formulations were prepared by varying the ratio of chitosan and guar gum using span-85 as an emulsifier and glutaraldehyde as a chemical cross linking agent. The microspheres were evaluated for particle size, encapsulation efficiency, drug loading capacity, mucoadhesion studies, stability studies, in vitro drug release studies. Particle sizes, as measured by the optical microscopic technique, were of an average size in the range 30.2 mm (LCG1) to 36.5 mm (LCG3). The swelling index was in the range 0.45-0.78. The SEM study showed that microspheres have smooth surfaces. Microspheres were characterised by differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR) spectroscopy to confirm the absence of chemical interactions between drug and polymer and to know the formation of microspheres structure. The optimised batch LCG 1 released 97.45 % at 10 h Phosphate buffer pH7.4 as dissolution medium.With regard to release kinetics, the data of the optimized formula were best fitted with the Higuchi model (r 2 = 0.671) and showed zero order release (r 2 = 0.980) with non-Fickian diffusion mechanism. The findings of the present study conclusively state that chitosan (1:2 of drug to polymer ratio) microspheres of Losartan potassium are potential for the sustained drug delivery of the drug in hypertension

Response of cardamom (Elettaria cardamomum Maton) seedlings to vesicular arbuscular mycorrhizal fungi

The growth response of cardamom (Elettaria cardamomum) seedlings (cv, Malabar) to 13 different vesicular arbuscular mycorrhizal fungi was tested under mat house conditions at Bangalore, India, In general, seedlings inoulated with the fungi grew taller, had more number of leaves and tillers, increased seedling biomass and uptake of nutrients compared to control seedlings, Among the various mycorrhizal fungi tested, seedlings inoculated with Gigaspora margarita and Glomus monosporum exhibited significantly higher growth with increased uptake of nutrients, &nbsp

Preparation of Fluconazole β-Cyclodextrin Complex Ocuserts: In Vitro and In Vivo Evaluation

The main purpose of the present study was to develop ocuserts of Fluconazole β-CD (beta-cyclodextrin) complex and to evaluate both in vitro and in vivo. Fluconazole was made complex with β-CD, and the release rate was controlled by HPMC K4M and ethyl cellulose polymers using dibutyl Phthalate as permeability enhancer. Drug-polymer interactions were studied by Fourier transform infrared spectroscopic studies. The formulated ocuserts were tested for physicochemical parameters of in vitro release and in vivo permeation in rabbits. The optimized formulations (F-5 and F-8) were subjected to stability studies. The formulated ocuserts were found to have good physical characters, thickness, diameter, uniformity in weight, folding endurance, less moisture absorption, and controlled release of drug both in vitro and in vivo. The optimized formulations retained their characteristics even after stability studies. The study clearly showed that this technique was an effective way of formulating ocuserts for retaining the drug concentration at the intended site of action for a sufficient period of time and to elicit the desired pharmacological response

Systems analysis of bioenergetics and growth of the extreme halophile Halobacterium salinarum

Halobacterium salinarum is a bioenergetically flexible, halophilic microorganism that can generate energy by respiration, photosynthesis, and the fermentation of arginine. In a previous study, using a genome-scale metabolic model, we have shown that the archaeon unexpectedly degrades essential amino acids under aerobic conditions, a behavior that can lead to the termination of growth earlier than necessary. Here, we further integratively investigate energy generation, nutrient utilization, and biomass production using an extended methodology that accounts for dynamically changing transport patterns, including those that arise from interactions among the supplied metabolites. Moreover, we widen the scope of our analysis to include phototrophic conditions to explore the interplay between different bioenergetic modes. Surprisingly, we found that cells also degrade essential amino acids even during phototropy, when energy should already be abundant. We also found that under both conditions considerable amounts of nutrients that were taken up were neither incorporated into the biomass nor used as respiratory substrates, implying the considerable production and accumulation of several metabolites in the medium. Some of these are likely the products of forms of overflow metabolism. In addition, our results also show that arginine fermentation, contrary to what is typically assumed, occurs simultaneously with respiration and photosynthesis and can contribute energy in levels that are comparable to the primary bioenergetic modes, if not more. These findings portray a picture that the organism takes an approach toward growth that favors the here and now, even at the cost of longer-term concerns. We believe that the seemingly "greedy" behavior exhibited actually consists of adaptations by the organism to its natural environments, where nutrients are not only irregularly available but may altogether be absent for extended periods that may span several years. Such a setting probably predisposed the cells to grow as much as possible when the conditions become favorable

Binding adaptation of GS 441524 diversifies macro domains and downregulate SARS CoV 2 de MARylation capacity

Viral infection in cells triggers a cascade of molecular defense mechanisms to maintain host cell homoeostasis. One of these mechanisms is ADP ribosylation, a fundamental post translational modification PTM characterized by the addition of ADP ribose ADPr on substrates. Poly ADP ribose polymerases PARPs are implicated in this process and they perform ADP ribosylation on host and pathogen proteins. Some viral families contain structural motifs that can reverse this PTM. These motifs known as macro domains MDs are evolutionarily conserved protein domains found in all kingdoms of life. They are divided in different classes with the viral belonging to Macro D type class because of their properties to recognize and revert the ADP ribosylation. Viral MDs are potential pharmaceutical targets, capable to counteract host immune response. Sequence and structural homology between viral and human MDs are an impediment for the development of new active compounds against their function. Remdesivir, is a drug administrated in viral infections inhibiting viral replication through RNA dependent RNA polymerase RdRp . Herein, GS 441524, the active metabolite of the remdesivir, is tested as a hydrolase inhibitor for several viral MDs and for its binding to human homologs found in PARPs. This study presents biochemical and biophysical studies, which indicate that GS 441524 selectively modifies SARS CoV 2 MD de MARylation activity, while it does not interact with hPARP14 MD2 and hPARP15 MD2. The structural investigation of MD GS 441524 complexes, using solution NMR and X ray crystallography, discloses the impact of certain amino acids in ADPr binding cavity suggesting that F360 and its adjacent residues tune the selective binding of the inhibitor to SARS CoV 2 M

Investigations into a putative role for the novel BRASSIKIN pseudokinases in compatible pollen-stigma interactions in Arabidopsis thaliana.

BACKGROUND: In the Brassicaceae, the early stages of compatible pollen-stigma interactions are tightly controlled with early checkpoints regulating pollen adhesion, hydration and germination, and pollen tube entry into the stigmatic surface. However, the early signalling events in the stigma which trigger these compatible interactions remain unknown. RESULTS: A set of stigma-expressed pseudokinase genes, termed BRASSIKINs (BKNs), were identified and found to be present in only core Brassicaceae genomes. In Arabidopsis thaliana Col-0, BKN1 displayed stigma-specific expression while the BKN2 gene was expressed in other tissues as well. CRISPR deletion mutations were generated for the two tandemly linked BKNs, and very mild hydration defects were observed for wild-type Col-0 pollen when placed on the bkn1/2 mutant stigmas. In further analyses, the predominant transcript for the stigma-specific BKN1 was found to have a premature stop codon in the Col-0 ecotype, but a survey of the 1001 Arabidopsis genomes uncovered three ecotypes that encoded a full-length BKN1 protein. Furthermore, phylogenetic analyses identified intact BKN1 orthologues in the closely related outcrossing Arabidopsis species, A. lyrata and A. halleri. Finally, the BKN pseudokinases were found to be plasma-membrane localized through the dual lipid modification of myristoylation and palmitoylation, and this localization would be consistent with a role in signaling complexes. CONCLUSION: In this study, we have characterized the novel Brassicaceae-specific family of BKN pseudokinase genes, and examined the function of BKN1 and BKN2 in the context of pollen-stigma interactions in A. thaliana Col-0. Additionally, premature stop codons were identified in the predicted stigma specific BKN1 gene in a number of the 1001 A. thaliana ecotype genomes, and this was in contrast to the out-crossing Arabidopsis species which carried intact copies of BKN1. Thus, understanding the function of BKN1 in other Brassicaceae species will be a key direction for future studies