In Silico Modeling of Myelin Oligodendrocyte Glycoprotein Disulfide Bond Reduction by Phosphine-Borane Complexes.

Background: Neurodegenerative diseases can cause vision loss by damaging retinal ganglion cells in the optic nerve. Novel phosphine-borane compounds (PBs) can protect these cells from oxidative stress via the reduction of disulfide bonds. However, the specific targets of these compounds are unknown.

Revealing the temporal dynamics of fish assemblage pattern, feeding guilds in relation to habitat quality parameters in a coastal wetland of the Indian Sundarban eco-region.

The present study was conducted from April 2016 to March 2017 in a freshwater-dominated coastal wetland of the Indian Sundarban ecoregion to illustrate the fish diversity, and abundance and the predictor variables determining fish assemblage structure in the wetland. A total of 27 fish species belonging to 13 orders, 16 families, and 23 genera with Cyprinidae (18.5%) as the most dominant family were recorded from the wetland.

Comparative metagenomic analysis from Sundarbans ecosystems advances our understanding of microbial communities and their functional roles.

The Sundarbans mangrove, located at the mouth of the Ganges and Brahmaputra Rivers, is the world's largest tidal mangrove forest. These mangroves are also one of the most striking sources of microbial diversity, essential in productivity, conservation, nutrient cycling, and rehabilitation. Hence, the main objective of this study was to use metagenome analysis and provide detailed insight into microbial communities and their functional roles in the Sundarbans mangrove ecosystem.

Assessing the trophic status of a tropical microtidal estuary applying TRIX and Random Forest - A combined approach.

The present study assessed the trophic status of a medium-sized microtidal estuary, Rushikulya, India using a combination of mutimetric trophic indices (TRIX, TRBIX) and a machine learning approach (Random Forest). A total of 108 samples were considered to build a predictive model for chlorophyll a (Chl a) and 17 response water variables by observing two annual periods (2021-2023) at six sampling sites. Mean values of TRIX (5.

Probing river health status: a study based on index of biotic integrity (IBI) in Tapti River of Deccan plateau, India.

Anthropogenic activities impacted the ecological health of rivers by altering the physical habitat and water flow as well as by pollution. Monitoring of biotic groups for gauging the river health is a prerequisite for assessing the extent of degradation and formulating management guidelines for river restoration. An assessment using fish-based index of biotic integrity (IBI) was carried out in the Central Indian river, Tapti, for probing its health status.

Changes in soil microbial biomass and organic C pools improve the sustainability of perennial grass and legume system under organic nutrient management.

Introduction: The perennial grass-legume cropping system benefits soil because of its high biomass turnover, cover cropping nature, and different foraging behaviors. We investigated the response of soil organic carbon (SOC) pools and their stock to organic and inorganic nutrient management in the Guinea grass and legume (cowpea-Egyptian clover) cropping system.

Methods: Depth-wise soil samples were collected after harvesting the Egyptian clover.

New record of two isopods and from riverine freshwater fishes in the river Tapti.

The present paper deals with the infestation of freshwater fishes , and by the parasitic isopods and in Tapti, a westward freshwater flowing river of India. The isopods H. Milne Edwards, 1840 and Stebbing, 1907 were identified with the taxonomic keys of Milne Edwards (1840) and Stebbing (1907), respectively.

Variability in the zooplankton assemblages in relation to environmental variables in the tidal creeks of Sundarbans estuarine system, India.

The present study illustrates a holistic account of zooplankton community dynamics in relation to physicochemical variables in the tidal creeks of Indian Sundarbans estuarine system. Eleven water variables and zooplankton samples were collected in a monthly basis from the six sampling locations between July 2016 and June 2018. Out of the 11 water parameters, seven parameters (temperature, salinity, dissolved oxygen, turbidity, PO - P, NO - N, and NO - N) varied significantly (p ≤ 0.

Development and Characterization of Natural Product Derived Macromolecules Based Interpenetrating Polymer Network for Therapeutic Drug Targeting.

Interpenetrating polymer network (IPN)-based bead formulations were exploited by cross-linking different hydrophilic polymers in different combinations and at different ratios. Polyvinyl alcohol, xanthan gum, guar gum, gellan gum, and sodium alginate (Na-alginate) were used in this work as hydrophilic polymers to enhance the solubility of diclofenac sodium and also to target the delivery at preferred locations. IPN beads based on polysaccharides were prepared by the ionic gelation method.

Predicting Absorption-Distribution Properties of Neuroprotective Phosphine-Borane Compounds Using In Silico Modeling and Machine Learning.

Phosphine-borane complexes are novel chemical entities with preclinical efficacy in neuronal and ophthalmic disease models. In vitro and in vivo studies showed that the metabolites of these compounds are capable of cleaving disulfide bonds implicated in the downstream effects of axonal injury. A difficulty in using standard in silico methods for studying these drugs is that most computational tools are not designed for borane-containing compounds.

A Review on Designing Poly (Lactic-co-glycolic Acid) Nanoparticles as Drug Delivery Systems.

Poly (lactic-co-glycolic acid) (PLGA) is a versatile synthetic polymer comprehensively used in the pharmaceutical sector because of its biocompatibility and biodegradability. These benefits lead to its application in the area of nanoparticles (NPs) for drug delivery for over thirty years. This article offers a general study of the different poly (lactic-co-glycolic acid) nanoparticles (PNPs), preparation methods such as emulsification-solvent evaporation, coacervation, emulsification solvent diffusion, dialysis, emulsification reverse salting out, spray drying nanoprecipitation, and supercritical fluid technology, from the methodological point of view.

Epidemiology of ROP update - Africa is the new frontier.

Several epidemics of blindness due to retinopathy of prematurity (ROP) have been described, with the most recent (the third) occurring in middle income countries in Latin America and Eastern Europe initially, and more recently in the more advanced economies in Asia. In these settings, which are characterized by variation in the quality of neonatal care and inadequate coverage of ROP screening and treatment, larger, more mature infants are affected as well as extremely preterm infants. In 2010 the annual incidence of blindness and visual impairment from ROP globally was estimated to be 32,300, with the lowest incidence in sub-Saharan countries.

Synthesis and characterization of interpenetrating polymeric networks based bio-composite alginate film: A well-designed drug delivery platform.

This study aimed to develop and characterize the calcium alginate films loaded with diclofenac sodium and other hydrophilic polymers with different degrees of cross-linking obtained by external gelation process. To the formed films different physicochemical evaluation were performed which showed an initial character of the films. The films produced by this external gelation process were found thicker (0.

Extraembryonic heparin-binding epidermal growth factor-like growth factor deficiency compromises placentation in mice.

Heparin-binding epidermal growth factor (EGF)-like growth factor (HBEGF) is expressed in the embryo and uterus at the implantation site, stimulating trophoblast invasive activity essential for placentation. The effect of extraembryonic HBEGF deficiency on placental development was investigated by breeding mice heterozygous for the Hbegf null mutation. On gestation day 13.

Ethosomes as Novel Vesicular Carrier: An Overview of the Principle, Preparation and its Applications.

Background: In the study of lipid vesicular carriers in permeation enhancement of drug molecules across skin after the success story of liposomes, ethosomes are a recent addition. There are a number of published reviews but still, there is a lack of reviews representing various aspects in a systematic way with a detailed description of current research works. This review serves to fill this deficiency along with special emphasize on its preparation methods and applications.

Examination of VDR/RXR/DRIP205 Interaction, Intranuclear Localization, and DNA Binding in Ras-Transformed Keratinocytes and Its Implication for Designing Optimal Vitamin D Therapy in Cancer.

Retinoid X receptor (RXR) occupies a central position within the nuclear receptor superfamily, serving as an obligatory partner to numerous other nuclear receptors, including vitamin D receptor (VDR). In the current study, we examined whether phosphorylation of RXRα at serine 260 affects VDR/RXR and VDR interacting protein (DRIP) 205 coactivator recruitment, interactions, and binding of the VDR/human RXRα (hRXRα)/DRIP205 complex to chromatin. Serine 260 is a critical amino acid on the hRXRα that is located in close spatial proximity to regions of coactivator and corepressor interactions.

Discovery of Novel Allosteric HCV NS5B Inhibitors. 2. Lactam-Containing Thiophene Carboxylates.

Lomibuvir () is a non-nucleoside, allosteric inhibitor of the hepatitis C virus NS5B polymerase with demonstrated clinical efficacy. Further development efforts within this class of inhibitor focused on improving the antiviral activity and physicochemical and pharmacokinetic properties. Recently, we reported the development of this series, leading to compound , a molecule with comparable potency and an improved physicochemical profile relative to .

Optimization of preparation method for ketoprofen-loaded microspheres consisting polymeric blends using simplex lattice mixture design.

In the present investigation, simplex lattice mixture design was applied for formulation development and optimization of a controlled release dosage form of ketoprofen microspheres consisting polymers like ethylcellulose and Eudragit(®)RL 100; when those were formed by oil-in-oil emulsion solvent evaporation method. The investigation was carried out to observe the effects of polymer amount, stirring speed and emulsifier concentration (% w/w) on percentage yield, average particle size, drug entrapment efficiency and in vitro drug release in 8h from the microspheres. Analysis of variance (ANOVA) was used to estimate the significance of the models.

Discovery of Novel Thiophene-Based, Thumb Pocket 2 Allosteric Inhibitors of the Hepatitis C NS5B Polymerase with Improved Potency and Physicochemical Profiles.

The hepatitis C viral proteins NS3/4A protease, NS5B polymerase, and NS5A are clinically validated targets for direct-acting antiviral therapies. The NS5B polymerase may be inhibited directly through the action of nucleosides or nucleotide analogues or allosterically at a number of well-defined sites. Herein we describe the further development of a series of thiophene carboxylate allosteric inhibitors of NS5B polymerase that act at the thumb pocket 2 site.

Polycomb repressive complex 1 controls uterine decidualization.

Uterine stromal cell decidualization is an essential part of the reproductive process. Decidual tissue development requires a highly regulated control of the extracellular tissue remodeling; however the mechanism of this regulation remains unknown. Through systematic expression studies, we detected that Cbx4/2, Rybp, and Ring1B [components of polycomb repressive complex 1 (PRC1)] are predominantly utilized in antimesometrial decidualization with polyploidy.

Control of regional decidualization in implantation: Role of FoxM1 downstream of Hoxa10 and cyclin D3.

Appropriate regulation of regional uterine stromal cell decidualization in implantation, at the mesometrial triangle and secondary decidual zone (SDZ) locations, is critical for successful pregnancy, although the regulatory mechanisms remain poorly understood. In this regard, the available animal models that would specifically allow mechanistic analysis of site-specific decidualization are strikingly limited. Our study found that heightened expression of FoxM1, a Forkhead box transcription factor, is regulated during decidualization, and its conditional deletion in mice reveals failure of implantation with regional decidualization defects such as a much smaller mesometrial decidua with enlarged SDZ.

Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 2: non-symmetric inhibitors with potent activity against genotype 1a and 1b.

The discovery of non-symmetric thienoimidazole-containing HCV NS5A inhibitors is described. The inhibitors herein reported display high potencies against both genotype 1a and 1b. In this follow-up manuscript, we discuss the importance of the linker aromaticity to achieve high potency, particularly against genotype 1a.