Synthesis, characterization and application of chitosan functionalized and functional graphene oxide membranes for desalination of water by pervaporation.

The use of graphene sheets in water treatment is increasing due to its adsorption capacity, reactivity, catalytic action and surface area. The challenges linked to wastewater treatment are vast due to the constant influx of various pollutants. Can the challenges of water desalination and purification be encountered by graphene-based composites and membranes?.The current work describes the synthesis of graphene oxide (GO) using modified Hummers' method. GO was functionalized with chitosan and used as adsorbents. On the other hand, it was reported that the surface of thin-film-composite (TFC) polyamide membranes was modified in order to desalinate highly saline water using pervaporation. The findings showed that GO synthesized by modified Hummers' method has a greater capacity for the adsorption of sodium ion and have better regeneration performance. Functionalization with chitosan increased adsorption capacity from 680.2 to 740.5 mg/g at the initial concentration of 45,000 mg/l of Na+ ions. On the other hand, modification in membrane comprises the chlorine treatment of surface of polyamide membrane. Layer-by-layer (LbL) deposition of positively charged polyethyleneimine (PEI) and negatively charged graphene oxide (GO) was followed. The PEI/GO LbL membrane's pure water flux was twice as high as compare to the original membrane. The synthesized membrane was tested against the aqueous solutions containing Na2SO4, MgSO4, NaCl and MgCl2 salts for their desalination. At different concentrations, a water flux of 8.9 kg/m2h with a huge salt rejection (>99.9%) was attained for every tested salt. It was observed that CS functionalized GO and GO membrane showed higher adsorption capacity and improved regeneration performance can be measured as an operational and active adsorbent for sea water desalination.

Exploring the sensing potential of Fe-decorated h-BN toward harmful gases: a DFT study.

Gas sensing technology has a broad impact on society, ranging from environmental and industrial safety to healthcare and everyday applications, contributing to a safer, healthier, and more sustainable world. We studied pure and Fe-decorated hexagonal boron nitride (h-BN) gas sensor for monitoring of carbon-based gases using density functional theory (DFT). The calculations utilized the Generalized Gradient Approximation with the Perdew-Burke-Ernzerhof (GGA-PBE) exchange-correlation functional. The novelty of our study lies in the investigation of the adsorption of harmful gases such as carbonyl sulfide, carbinol, carbimide, and carbonyl fluoride on both pure and Fe-decorated h-BN. The deviation in structural, electronic, and adsorption properties of h-BN due to Fe decoration has been studied along with the sensing ability to design said material towards carbon monoxide (CO), carbon dioxide (CO2), carbonyl sulfide (COS), carbinol, (CH4O), carbimide (CH2N2), and carbonyl fluoride (CF2O) gases. Gases such as CO, COS, CH2N2, and CF2O exhibited chemisorption, while CO2, and CH4O exhibited physisorption behavior. The introduction of Fe altered the semiconductor properties of h-BN and rendered it metallic. Enhanced electronic properties were observed due to a robust hybridization occurring between the d-orbitals of Fe-decorated BN and the gas molecules. The extended recovery periods observed for gases, aside from CO2, indicate their adhesive interactions with Fe-decorated h-BN. The reduction in desorption duration as temperature rises allows Fe-decorated h-BN to function as a reversible gas sensor. This research opens up a novel pathway for the synthesis and advancement of cost-effective, environmentally friendly double-atom catalysts with high sensitivity for capturing and detecting molecules such as CO, COS, CH2N2, CO2, CH4O, and CF2O.

Mass spectrometric study of low energy Cs+ ion-induced sputtered fragmentation of PADC polymer.

In this study, low-energy cesium (Cs+ ) ion-induced sputtered fragmentation of poly allyl diglycol carbonate (PADC) was investigated using mass spectrometry. The collision-induced dissociation mechanism revealed emission of various fragments, including monoatomic (H- , C1 - , O1 - ), diatomic (C2 - ), and multiatomic (C3 - , CO2 - , C2 O2 - , C3 O2 - ) species within the Cs+ ion energy range of 1-5 keV. The anion current of these fragments exhibited a linear increase with rising incident Cs+ ion energy, indicating a corresponding rise in fragment abundance. Analysis of normalized yield indicated that at 1 keV incident energy, the dominant fragment was monoatomic hydrogen (H- ), followed by diatomic carbon (C2 - ), monoatomic carbon (C1 - ), and monoatomic oxygen (O1 - ). Although C2 - remained dominant up to 5 keV, other fragments exhibited varying normalized yields at different ion energy steps. The sputter yield estimation revealed that monoatomic hydrogen (H- ) and diatomic carbon (C2 - ) exhibited the highest yields, increasing exponentially beyond 3 keV, while multiatomic fragments like C3 - , CO2 - , C2 O2 - , and C3 O2 - displayed the lowest yields. The sputter dissociation mechanism pointed to dehydrogenation, chain scission, and bond breakage as the primary processes during low-energy Cs+ ion impact. Postsputtering Scanning Electron Mircoscope (SEM) micrographs show craters, pits, and micropores on the PADC surface, indicating significant surface degradation. X-ray Diffraction (XRD) spectra exhibited reduced diffraction intensity, while Fourier Transform Infrared Spectroscopy (FTIR) analysis indicated the absence of molecular bands in the IR spectrum, confirming extensive surface damage due to Cs+ ion-induced sputtering.

An efficient synthesis and characterization of La@MOF-808: A promising strategy for effective arsenic ion removal from water.

Addressing serious waterborne arsenic issues, for the first time, lanthanum-doped MOF-808 (La@MOF-808) has been developed to remove total arsenic (Total As) and arsenite [As(III)] from water. This study involves the solvothermal synthesis of La@MOF-808, its characterization via FTIR, XRD, TGA, and SEM, in which distinct physicochemical attributes were identified, and the adsorption capacity of arsenic ions. The saturated adsorption capacity of La@MOF-808 for Total As and As(III) reached 282.9 mg g-1 and 283.5 mg g-1, as compared to 229.7 mg g-1 and 239.1 mg g-1 for pristine MOF-808, respectively. XRD and ATR-FTIR analyses underscored the central roles of electrostatic interactions and hydroxyl groups in the pollutant adsorption process. The impact of temperature, concentration, pH, and exposure duration times on adsorption performance was thoroughly investigated. The Langmuir model showed the maximum adsorption capacities (qmax) of La@MOF-808 was 307.7 mg g-1 for Total As and 325.7 mg g-1 for As(III), surpassing those of MOF-808 adsorbent, which suggests that monolayer adsorption occurred. Optimal adsorption was observed in a pH range of 2.0-7.0, and thermodynamic studies classified the process as spontaneous and endothermic. The adsorbent retains high capacity across repeated cycles, outperforming many standard adsorbents. Lanthanum doping markedly enhances MOF-808's arsenic removal, underscoring its potential for water treatment.

Characterization for optimizing the integrated management of solid waste for energy recovery and circular economy.

Municipal solid waste (MSW) management poses a significant environmental challenge in municipalities across developing nations worldwide. Our studies were focused on characterizing the waste and analyzing the chemical properties of mixed waste fractions to assess their potential for waste-to-energy conversion. The objective of our study was to scrutinize the existing state of the MSW management system and gauge its waste generation rates. Specific ASTM methods were employed to carry out both physical and chemical characterizations. The outcomes reveal that the city generates a daily volume of 1155 tons of domestic solid waste (DSW), translating to a generation rate of 0.51 kg-1 capita-1 day-1. When analyzed by source, organic matter emerged as the predominant constituent, accounting for 73.74% of the waste, followed by combustible content waste at 15.17%. The moisture content of MSW ranged between 26 and 58% throughout the seasons, while volatile solids varied from 22.35 to 99.74%. Among the components screened, carbon and oxygen stood out as the dominant elements. The calorific values encompassed a broad range, ranging from 14.87 MJ kg-1 for leather waste to a substantial 25,629.27 MJ kg-1 for organic waste. To alleviate the escalating burden of increasing solid waste generation, alternative treatment approaches were recommended. These include composting, biomethane plants, the establishment of recycling facilities, and the enhancement of existing landfill sites to scientifically designed landfills. In summary, the findings from this study provide valuable insights for regulatory bodies and municipal authorities. These insights can guide the formulation of policies concerning waste sampling, characterization, segregation, and the implementation of education and awareness campaigns.

[1, 8]-Naphthyridine derivatives as dual inhibitor of alkaline phosphatase and carbonic anhydrase.

[1,8]-Naphthyridine derivatives have been reported to possess important biological activities and may serve as attractive pharmacophores in the drug discovery process. [1,8]-Naphthyridine derivatives (1a-1l) were evaluated for inhibitory potential for isozymes of carbonic anhydrase (CA) and alkaline phosphatase (ALP). CAs have been reported to carry out reversible hydration of CO2 into HCO3-, secretion of electrolytes, acid-base regulation, bone resorption, calcification, and biosynthetic reactions. Whereas ALPs hydrolyze monophosphate esters with the release of inorganic phosphate and play an important role in bone mineralization. Both enzymes have been found to be over-expressed and raised functional activities in patients suffering from rheumatoid arthritis. The discovery of dual inhibitors of these enzymes may provide a synergistic effect to cure bone disorders such as rheumatoid arthritis and ankylosing spondylitis. Among the test compounds, the most potent inhibitors for CA-II, CA-IX, and CA-XII were 1e, 1g, and 1a with IC50 values of 0.44 ± 0.19, 0.11 ± 0.03 and 0.32 ± 0.07 µM, respectively. [1,8]-Naphthyridine derivatives (1a-1l) were approximately 4 folds more potent than standard CA inhibitor acetazolamide. While in the case of ALPs, the most potent compounds for b-TNAP and c-IAP were 1b and 1e with IC50 values of 0.122 ± 0.06 and 0.107 ± 0.02 µM, respectively. Thus, synthesized derivatives proved to be 100 to 800 times more potent as compared to standard inhibitors of b-TNAP and c-IAP (Levamisole and L-phenyl alanine, respectively). In addition, selectivity and dual inhibition of [1,8]-Naphthyridine derivatives confer precedence over known inhibitors. Molecular docking and molecular simulation studies were also conducted in the present studies to define the type of interactions between potential inhibitors and enzyme active sites.

Development and Pharmacokinetic Evaluation of Novasomes for the Trans-nasal Delivery of Fluvoxamine Using Arachidonic Acid-Carboxymethyl Chitosan Conjugate.

Depression is the major mental illness which causes along with loss of interest in daily life, a feeling of hopelessness, appetite or weight changes, anger and irritability. Due to the hepatic first-pass metabolism, the absolute bioavailability of fluvoxamine (FVM) after oral administration is about 50%. By avoiding the pre-systemic metabolism, nasal delivery would boost bioavailability of FVM. Additionally, the absorption is anticipated to occur more quickly than it would via the oral route because of the existence of microvilli and high vasculature. A nonionic surfactant, cholesterol and an arachidonic acid-carboxymethyl chitosan (AA-CMCS) conjugate were used to develop FVM-loaded novasomes. To investigate the effects of surfactant concentration, AA-CMCS conjugate concentration and stirring speed on the novasomes' characteristics, a Box-Behnken design was used. The dependent variables chosen were zeta potential, polydispersity index and particle size. The AA-CMCS conjugate was confirmed by 1H-NMR and FTIR. Using Design Expert software (version 7; Stat-Ease Inc., Minneapolis, MN, USA), novasomes were further optimized. The chosen optimal formulation (NAC8) was made up of AA-CMCS conjugate, Span 60 and cholesterol. Particle size, zeta potential and PDI values for NAC8 formulation were 101 nm, -35 mV and 0.263, respectively. The NAC8 formulation's DSC and TGA analysis demonstrated that the medication had been uniformly and amorphously distributed throughout the novasomes. The NAC8 formulation showed 99% and 90% FVM release and permeation, respectively, and the novasome adherence time was 24 h. An improved antidepressant effect along with five-fold increase in bioavailability of FVM was observed after trans-nasal administration of NAC8 formulation compared to the reference commercially available Flumin® tablets. FVM-loaded novasomes administered via the nasal route may therefore constitute an advancement in the management of depression.

Risk assessment of toxic and hazardous metals in paddy agroecosystem by biochar-for bio-membrane applications.

Toxic and carcinogenic metal (loid)s, such arsenic (As) and cadmium (Cd), found in contaminated paddy soils pose a serious danger to environmental sustainability. Their geochemical activities are complex, making it difficult to manage their contamination. Rice grown in Cd and As-polluted soils ends up in people's bellies, where it can cause cancer, anemia, and the deadly itai sickness. Solving this issue calls for research into eco-friendly and cost-effective remediation technology to lower rice's As and Cd levels. This research delves deeply into the origins of As and Cd in paddy soils, as well as their mobility, bioavailability, and uptake mechanisms by rice plants. It also examines the current methods and reactors used to lower As and Cd contamination in rice. Iron-modified biochar (Fe-BC) is a promising technology for reducing As and Cd toxicity in rice, improving soil health, and boosting rice's nutritional value. Biochar's physiochemical characteristics are enhanced by the addition of iron, making it a potent adsorbent for As and Cd ions. In conclusion, Fe-BC's biomembrane properties make them an attractive option for remediating As- and Cd-contaminated paddy soils. More efficient mitigation measures, including the use of biomembrane technology, can be developed when sustainable agriculture practices are combined with these technologies.

Disulfide Bridged Nanoparticles of Thiolated Sodium Alginate and Eudragit RS100 for Oral Delivery of Paclitaxel: In Vitro and In Vivo Evaluation.

Most biopharmaceutics classification system (BCS) class IV drugs have limited oral bioavailability due to poor solubility and poorer permeability. This work aims to investigate the possibility of utilizing disulfide bridged nanoparticles to improve BCS IV drug solubility and oral absorption. Disulfide bridged nanoparticles were made using thiolated sodium alginate (TSA) and thiolated eudragit RS100 (TERS100). This study used paclitaxel (PTL) as a model drug to create PTL-loaded nanoparticles using the air oxidation approach. PTL-loaded nanoparticles boosted the solubility of PTL by over 11 times (∼59 µg/mL). The nanoparticles had particle sizes of 103 nm, polydispersity indices of 0.034, and zeta potentials of -21 mV, respectively. Nanoparticles demonstrated 75.34% and 89.18% entrapment and loading efficiency of PTL, respectively. The PTL release data from nanoparticles had good sustained release properties. The effective permeability of PTL from nanoparticles was 2.19-fold higher than that of pure PTL suspension. The relative bioavailability of PTL with disulfide bridged nanoparticles was 237.11%, which was much higher than that of PTL suspension, according to the pharmacokinetic data. These results show that disulfide bridged nanoparticles have a wide range of clinical applications.

Exploring chromone sulfonamides and sulfonylhydrazones as highly selective ectonucleotidase inhibitors: Synthesis, biological evaluation and in silico study.

Ectonucleotidases, a well-known superfamily of plasma membrane located metalloenzymes plays a central role in mediating the process of purinergic cell signaling. Major functions performed by these enzymes include the hydrolysis of extracellular nucleosides and nucleotides which are considered as important cell-signaling molecules. Any (patho)-physiologically induced disruption in this purinergic cell signaling leads to several disorders, hence these enzymes are important drug targets for therapeutic purposes. Among the major challenges faced in the design of inhibitors of ectonucleotidases, an important one is the lack of selective inhibitors. Access to highly selective inhibitors via a facile synthetic route will not only be beneficial therapeutically, but will also lead to an increase in our understanding of intricate interplay between members of ectonucleotidase enzymes in relation to their selective activation and/or inhibition in different cells and tissues. Herein we describe synthesis of highly selective inhibitors of human intestinal alkaline phosphatase (h-IAP) and human tissue non-specific alkaline phosphatase (h-TNAP), containing chromone sulfonamide and sulfonylhydrazone scaffolds. Compound 1c exhibited highest (and most selective) h-IAP inhibition activity (h-IAP IC50 = 0.51 ± 0.20 µM; h-TNAP = 36.5%) and compound 3k showed highest activity and selective inhibition against h-TNAP (h-TNAP IC50 = 1.41 ± 0.10 µM; h-IAP = 43.1%). These compounds were also evaluated against another member of ectonucleotidase family, that is rat and human ecto-5'-nucleotidase (r-e5'NT and h-e5'NT). Some of the compounds exhibited excellent inhibitory activity against ecto-5'-nucleotidase. Compound 2 g exhibited highest inhibition against h-e5'NT (IC50 = 0.18 ± 0.02 µM). To rationalize the interactions with the binding site, molecular docking studies were carried out.

An assessment of the efficacy of biochar and zero-valent iron nanoparticles in reducing lead toxicity in wheat (Triticum aestivum L.).

Soil heavy metal contamination is increasing rapidly due to increased anthropogenic activities. Lead (Pb) is a well-known human carcinogen causing toxic effects on humans and the environment. Its accumulation in food crops is a serious hazard to food security. Developing environment-friendly and cost-efficient techniques is necessary for Pb immobilization in the soil. A pot experiment was executed to determine the role of biochar (BC), zero-valent iron nanoparticles (n-ZVI), and zero-valent iron nanoparticles biochar composite (n-ZVI-BC) in controlling the Pb mobility and bioaccumulation in wheat (Triticum aestivum L.). The results showed that BC and n-ZVI significantly enhanced the wheat growth by increasing their photosynthetic and enzymatic activities. Among all the applied treatments, the maximum significant (p ≤ 0.05) improvement in wheat biomass was with the n-ZVI-BC application (T3). Compared to the control, the biomass of wheat roots, shoots & grains increased by 92.5, 58.8, and 49.1%, respectively. Moreover, the soil addition of T3 amendment minimized the Pb distribution in wheat roots, shoots, and grains by 33.8, 26.8, and 16.2%, respectively. The outcomes of this experiment showed that in comparison to control treatment plants, soil amendment with n-ZVI-BC (T3) increased the catalase (CAT), superoxide dismutase (SOD) activity by 49.8 and 31.1%, respectively, ultimately declining electrolyte leakage (EL), malondialdehyde (MDA) and hydrogen peroxide (H2O2) content in wheat by 38.7, 33.3, and 38%respectively. In addition, applied amendments declined the Pb mobility in the soil by increasing the residual Pb fractions. Soil amendment with n-ZVI-BC also increased the soil catalase (CAT), urease (UR), and acid phosphatase (ACP) activities by 68, 59, and 74%, respectively. Our research results provided valuable insight for the remediation of Pb toxicity in wheat. Hence, we can infer from our findings that n-ZVI-BC can be considered a propitious, environment friendly and affordable technique for mitigating Pb toxicity in wheat crop and reclamation of Pb polluted soils.

Synthesis and Evaluation of Amide and Thiourea Derivatives as Carbonic Anhydrase (CA) Inhibitors.

Series of sulfonamide-substituted amide (9-11), benzamide (12-15), and 1,3-disubstituted thiourea (17-26) derivatives were synthesized from a common precursor, i.e., substituted benzoyl chlorides. Structures of all of the synthesized compounds were characterized by spectroscopic techniques (1H nuclear magnetic resonance (NMR),13C NMR, and Fourier transform infrared spectroscopy (FTIR)). All of the amide (9-15) and thiourea (17-26) derivatives were screened against human carbonic anhydrases, hCA-II, hCA IX, and hCA-XII. Sulfonamide-substituted amides 9, 11, and 12 were found to be excellent selective inhibitors with IC50 values of 0.18 ± 0.05, 0.17 ± 0.05, and 0.58 ± 0.05 µM against hCA II, hCA IX, and hCA XII, respectively. Compound 9 was found to be highly selective for hCA II and about 6-fold more potent as compared to the standard antagonist, acetazolamide. Safe toxicity profiling of the most potent and selective compounds was determined against normal BHK-21 and HEK-293 T cells. Molecular docking studies were performed, which described the type of interactions between the synthesized compounds and enzyme proteins. In addition, in silico absorption, distribution, metabolism, and excretion (ADME) studies were performed, which showed that all of the synthesized molecules fulfilled the druggability criteria.

Biomedical waste management associated with infectious diseases among health care professionals in apex hospitals of a typical south asian city.

Biomedical waste from healthcare activities poses a higher hazard of infection and damage than other types of trash. The main objective of the study was to assess the awareness knowledge and practices of biomedical waste management (BMWM) among health care professionals in the health care units. The cross-sectional study was carried out to access the awareness, knowledge and practices of health care professionals for BMWM. Using a qualitative approach, the study was escorted in two Apex hospitals i.e. the Allied Hospital and the District Head Quarter Hospital, Faisalabad, Pakistan from August 5, 2019 to October 15, 2019. More than 90% of respondents knew the phrase BMWM, but just 35.4% had awareness about biomedical waste regulations. About 71.6% of the respondents were familiar with biomedical waste's color-coding segregation. The study concludes gap in the awareness, knowledge and practices for BMWM. The sanitary workers of the hospitals had no knowledge about BMWM and the BMWM/healthcare waste management rule 2005 established in Pakistan due to the lack of training regarding waste management and the segregation process. Some of the staff members were aware of the BMWM practices under the rules and regulations of Pakistan but were unable to implement at their work place. It is necessary to dispose of the biomedical waste according to the established terms and conditions of BMWM rules (2005) of Pakistan. Weak structure of BMWM was observed at the study sites due to the lack of training, liabilities and absence of penalties against improper biomedical waste disposal as violation of the rules and regulations. It's a dire need of the time to consider the biomedical waste as hazardous waste and make policies for its safe disposal and ensure the implementation of the policies in all the medical centers of Pakistan.

Effect of sodium alginate supplementation on weight management and reproductive hormones in polycystic females.

Dietary fiber is getting attention these days due to its tendency to improve the reproductive performance in human beings. Sodium alginate (SA) is one of the natural dietary fibers. The present study aimed to evaluate the effect of SA on serum insulin, blood sugar, lipid profile, estrogen and testosterone in polycystic (PCOS) females. A single in vivo trial was conducted on thirty adult PCOS females (25 ± 5 years old) with a body mass index (BMI) of 27.5 ± 3.5 kg m-2. Blood samples of all PCOS females were drawn for the initial biochemical analysis and considered as the negative control (NC). A complete randomized design was used to divide the NC group into three equal subgroups (n = 9) i.e. SA3: with 0.03 g; SA6: with 0.06 g per kg body weight per day of sodium alginate; the positive control (PC): metformin 500 mg day-1 for 60 days (two months). A significant reduction (p < 0.05) in the body weight, BMI, blood sugar, serum insulin, lipids and testosterone was observed, while a significant incremental effect (p < 0.05) was observed in the high-density lipoprotein level. The percentages of some physical parameters were also improved like obesity, menstrual cycle, physical activity, psychological issues and hirsutism. Therefore, the study concluded that SA exhibited therapeutic potential for weight management and the improvement of serum testosterone in PCOS females.

Therapeutic potentials and structure-activity relationship of 1,3-benzodioxole N-carbamothioyl carboxamide derivatives as selective and potent antagonists of P2X4 and P2X7 receptors.

P2X receptors (P2XRs) are ligand-gated membrane ion channels. ATP binds to open these ion channels and results in membrane depolarization. Hyperactivities and overexpression of P2XRs are related to various pathophysiological conditions such as chronic pain, inflammatory diseases, rheumatoid arthritis, various neurological disorders, and cancer. Inhibition of P2XRs is a potential drug target that is an emerging therapeutic tool for disease management. In the present study, 17 new compounds were synthesized based on 1,3-benzodioxole-5-carboxylic acid and were investigated for P2XRs inhibition. Ca2+ influx assay was performed on P2XRs expressed h-1321N1 astrocytoma cell lines. The synthesized compounds exhibited high potency and selectivity towards h-P2X4R and h-P2X7R. In silico studies were carried out that began with the development of a homology model for h-P2X7R with subsequent molecular docking studies of the most potent P2XRs antagonists. 9o (N-((2-bromo-4-isopropylphenyl)carbamothioyl)benzo[d] [1,3]dioxole-5-carboxamide) was found to have significant inhibitory potential and selectivity for h-P2X4R with an IC50 ± SEM of 0.039 ± 0.07 µM. Whereas, 9q (N-(quinolin-8-ylcarbamothioyl)benzo[d] [1,3]dioxole-5-carboxamide) was selective and most potent antagonist for h-P2X7R with an IC50 ± SEM of 0.018 ± 0.06 µM. Both antagonists, 9o and 9q, exhibited a non-competitive negative allosteric mode of antagonism.

Purinergic receptors modulators: An emerging pharmacological tool for disease management.

Purinergic signaling is mediated through extracellular nucleotides (adenosine 5'-triphosphate, uridine-5'-triphosphate, adenosine diphosphate, uridine-5'-diphosphate, and adenosine) that serve as signaling molecules. In the early 1990s, purines and pyrimidine receptors were cloned and characterized drawing the attention of scientists toward this aspect of cellular signaling. This signaling pathway is comprised of four subtypes of adenosine receptors (P1), eight subtypes of G-coupled protein receptors (P2YRs), and seven subtypes of ligand-gated ionotropic receptors (P2XRs). In current studies, the pathophysiology and therapeutic potentials of these receptors have been focused on. Various ligands, modulating the functions of purinergic receptors, are in current clinical practices for the treatment of various neurodegenerative disorders and cardiovascular diseases. Moreover, several purinergic receptors ligands are in advanced phases of clinical trials as a remedy for depression, epilepsy, autism, osteoporosis, atherosclerosis, myocardial infarction, diabetes, irritable bowel syndrome, and cancers. In the present study, agonists and antagonists of purinergic receptors have been summarized that may serve as pharmacological tools for drug design and development.

Design and synthesis of adamantane-1-carbonyl thiourea derivatives as potent and selective inhibitors of h-P2X4 and h-P2X7 receptors: An Emerging therapeutic tool for treatment of inflammation and neurological disorders.

P2X receptors are potential therapeutic targets for the treatment of various neurodegenerative disorders, pain, inflammation, hypertension, and cancer. Adamantane ring has been reported to exhibit significant inhibitory potential towards P2X receptors, especially for P2X7R. We have utilized uniqueness of adamantane moiety in our synthesized compounds and introduced various substitutions that enhanced the potency as well as selectivity for P2XR subtypes. Among synthesized derivatives, 4n and 5b were found to be most potent and selective inhibitors for h-P2X4R and h-P2X7R, respectively. 4n was found to be highly selective for h-P2X4R with IC50 ± SEM = 0.04 ± 0.01 µM, that is 22 times more potent than BX-430, a standard selective inhibitor of h-P2X4R. 5b has IC50 ± SEM of 0.073 ± 0.04 µM, which is comparable with the known antagonists of h-P2X7R. 4n and 5b were studied for mode of inhibition of P2XRs and both were found to be negative allosteric modulators. In silico studies were also conducted to find the type of interactions as well as mode of inhibition.

Genetic Factors Underlying Single Fiber Quality in A-Genome Donor Asian Cotton (Gossypium arboreum).

The study of A-genome Asian cotton as a potential fiber donor in Gossypium species may offer an enhanced understanding of complex genetics and novel players related to fiber quality traits. Assessment of individual fibers providing classified fiber quality information to the textile industry is Advanced Fiber Information System (AFIS) in the recent technological era. Keeping the scenario, a diverse collection of 215 Asiatic cotton accessions were evaluated across three agro-ecological zones of China. Genome-Wide Association Studies (GWAS) was performed to detect association signals related to 17 AFIS fiber quality traits grouped into four categories viz: NEPs, fiber length, maturity, and fineness. Significant correlations were found within as well as among different categories of various traits related to fiber quality. Fiber fineness has shown a strong correlation to all other categories, whereas these categories are shown interrelationships via fiber-fineness. A total of 7,429 SNPs were found in association with 17 investigated traits, of which 177 were selected as lead SNPs. In the vicinity of these lead SNPs, 56 differentially expressed genes in various tissues/development stages were identified as candidate genes. This compendium connecting trait-SNP-genes may allow further prioritization of genes in GWAS loci to enable mechanistic studies. These identified quantitative trait nucleotides (QTNs) may prove helpful in fiber quality improvement in Asian cotton through marker-assisted breeding as well as in reviving eroded genetic factors of G. hirsutum via introgression breeding.

Synthesis of Sulfonamide Tethered (Hetero)aryl ethylidenes as Potential Inhibitors of P2X Receptors: A Promising Way for the Treatment of Pain and Inflammation.

P2X receptors have the ability to regulate various physiological functions like neurotransmission, inflammatory responses, and pain sensation. Such physiological properties make these receptors a new target for the treatment of pain and inflammation. Several antagonists of P2X receptors have been studied for the treatment of neuropathic pain and neurodegenerative disorders but potency and selectivity are the major issues with these known inhibitors. Sulfonamide derivatives were reported to be potent inhibitors of P2X receptors. In this study, sulfonamide carrying precursor hydrazide was synthesized by a facile method that was subsequently condensed with methyl (hetero)arylketones to obtain a series of new (hetero)aryl ethylidenes. These compounds were screened for inhibitory potential against h-P2X2, h-P2X4, h-P2X5, and h-P2X7 receptors to find their potency and selectivity. Computational studies were performed to confirm the mode of inhibition as well as type of interaction between ligand and target site. In calcium signaling experiments, compound 6h was found to be the most potent and selective inhibitor of h-P2X2 and h-P2X7 receptors with IC50 ± standard error of the mean (SEM) values of 0.32 ± 0.01 and 1.10 ± 0.21 µM, respectively. Compounds 6a and 6c exhibited selective inhibition for h-P2X7 receptor, whereas 6e, 7a, and 7b expressed selective inhibitions toward h-P2X2 receptor that were comparable to the positive control suramin and pyridoxalphosphate-6-azophenyl-2',4'-disulfonic acid (PPADS).

Toxicity of biogenic zinc oxide nanoparticles to soil organic matter cycling and their interaction with rice-straw derived biochar.

Given the rapidly increasing use of metal oxide nanoparticles in agriculture as well as their inadvertent addition through sewage sludge application to soils, it is imperative to assess their possible toxic effects on soil functions that are vital for healthy crop production. In this regard, we designed a lab study to investigate the potential toxicity of one of the most produced nanoparticles, i.e. zinc oxide nanoparticles (nZnO), in a calcareous soil. Microcosms of 80 g of dry-equivalent fresh soils were incubated in mason jars for 64 days, after adding 100 or 1000 mg of biogenically produced nZnO kg-1 soil. Moreover, we also added rice-straw derived biochar at 1 or 5% (w: w basis) hypothesizing that the biochar would alleviate nZnO-induced toxicity given that it has been shown to adsorb and detoxify heavy metals in soils. We found that the nZnO decreased microbial biomass carbon by 27.0 to 33.5% in 100 mg nZnO kg-1 soil and by 39.0 to 43.3% in 1000 mg nZnO kg-1 soil treatments across biochar treatments in the short term i.e. 24 days after incubation. However, this decrease disappeared after 64 days of incubation and the microbial biomass in nZnO amended soils were similar to that in control soils. This shows that the toxicity of nZnO in the studied soil was ephemeral and transient which was overcome by the soil itself in a couple of months. This is also supported by the fact that the nZnO induced higher cumulative C mineralization (i.e. soil respiration) at both rates of addition. The treatment 100 mg nZnO kg-1 soil induced 166 to 207%, while 1000 mg nZnO kg-1 soil induced 136 to 171% higher cumulative C mineralization across biochar treatments by the end of the experiment. However, contrary to our hypothesis increasing the nZnO addition from 100 to 1000 mg nZnO kg-1 soil did not cause additional decrease in microbial biomass nor induced higher C mineralization. Moreover, the biochar did not alleviate even the ephemeral toxicity that was observed after 24d of incubation. Based on overall results, we conclude that the studied soil can function without impairment even at 1000 mg kg-1 concentration of nZnO in it.