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A new series of 2 H -chromene-based sulfonamide derivatives 3 - 12 has been synthesized and characterized using different spectroscopic techniques. The synthesized 2 H -chromenes were synthesized by reacting activated methylene with 5-(piperidin-1-ylsulfonyl)salicylaldehyde through one-step condensation followed by intramolecular cyclization. Virtual screening of the designed molecules on α-glucosidase enzymes (PDB: 3W37 and 3A4A) exhibited good binding affinity suggesting that these derivatives may be potential α-glucosidase inhibitors. I n-vitro α-glucosidase activity was conducted firstly at 100 µg/mL, and the results demonstrated good inhibitory potency with values ranging from 90.6% to 96.3% compared to IP = 95.8% for Acarbose. Furthermore, the IC 50 values were determined, and the designed derivatives exhibited inhibitory potency less than 11 µg/mL. Surprisingly, two chromene derivatives 6 and 10 showed the highest potency with IC 50 values of 0.975 ± 0.04 and 0.584 ± 0.02 µg/mL, respectively, compared to Acarbose (IC 50 = 0.805 ± 0.03 µg/mL). Moreover, our work was extended to evaluate the in-vitro α-amylase and PPAR-γ activity as additional targets for diabetic activity. The results exhibited moderate activity on α-amylase and potency as PPAR-γ agonist making it a multiplet antidiabetic target. The most active 2 H -chromenes 6 and 10 exhibited significant activity to PPAR-γ with IC 50 values of 3.453 ± 0.14 and 4.653 ± 0.04 µg/mL compared to Pioglitazone (IC 50 = 4.884±0.29 µg/mL) indicating that these derivatives improve insulin sensitivity by stimulating the production of small insulin-sensitive adipocytes. In-silico ADME profile analysis indicated compliance with Lipinski's and Veber's rules with excellent oral bioavailability properties. Finally, the docking simulation was conducted to explain the expected binding mode and binding affinity. [Display omitted] • A new series of 6-sulfonamide- 2H -chromenes were designed and synthesized. • All the tested derivatives were screened by Virtual screened as α-glucosidase inhibitors. • The in-vitro α-glucosidase activity was evaluated as inhibitory percentage and IC 50 and SAR was conducted in detail. • The most active two derivatives 6 and 10 were further studies for α-amylase and PPAR-γ transactivation assay. • In-silico ADME and molecular docking was performed to confirm the experimental results for the most potent compounds. [ABSTRACT FROM AUTHOR]

Bio-fertilization is a sustainable agricultural practice that includes using bio-fertilizers to increase soil nutrient content resulting in higher productivity. Soil micro-flora has been exposed to improve soil fertility and increase biomass productivity and identified as a correct environmentally friendly bio-based fertilizer for pollution-free agricultural applies. The majority of cyanobacteria can fix nitrogen from the atmosphere and several species including Anabaena sp., Nostoc sp., and Oscillatoria angustissima is known to be effective cyanobacterial based bio fertilizers. Acutodesmus dimorphus , Spirulina platensis Chlorella vulgaris , Scenedesmus dimorphus , Anabaena azolla , and Nostoc sp. are some of the green microalgae and cyanobacteria species that have been successfully used as bio fertilizers to boost crop growth. Also, Chlorella vulgaris is one of the most commonly used microalgae in bio fertilizer studies. The addition of seaweed species that are Sargassum sp. and Gracilaria verrucosa leads to chemical changes as a soil fertility indicator on clay and sandy soils, and the addition of seaweed conditioner to soil can improve its organic content, return pH to normal, and reduce C/N ratio in both sandy and clay soil. This review provides an effective approach to increase soil fertility via environmentally friendly bio-based fertilizer using micro and macro algae. Instead of the usage of inorganic and organic fertilizers that have polluted impacts to soil as aggregation of heavy metals, in addition to there their human carcinogenic effects. [ABSTRACT FROM AUTHOR]

• The differential diagnosis of superficial corneal opacities is challenging. • It includes 3 described overlapping entities: SND, PHSCD, and Acquired Corneal Sub-Epithelial Hypertrophy (ACSH). • Our case series match the newly proposed entity of ACSH. • ACSH should be accurately identified following keratoplasty to be successfully managed by simple surgical peeling without corneal re-grafting. Acquired Corneal Sub-Epithelial Hypertrophy (ACSH) has been described in patients with peripheral superficial corneal opacities following penetrating keratoplasty and might present similar to Salzmann's nodular degeneration (SND) or peripheral hypertrophic sub-epithelial corneal degeneration (PHSCD). We describe the clinical presentation, topographic findings and the surgical outcome of three cases, which fit the appearance and characteristics of ACSH. Three patients (3 eyes) with paracentral or peripheral corneal opacification were reviewed to describe their clinical examination (SL), morphology of the opacity (depth, diameter and density) and document their topographic changes before and after surgical intervention by peeling of the epithelium with or without superficial keratectomy under the microscope in addition to brief description of their histopathological examination. All 3 cases were secondary to corneal procedures [Penetrating keratoplasty (PKP) in 1 for pseudophakic bullous keratopathy and deep anterior lamellar keratoplasty (DLK) in 2 for advanced keratoconus]. All cases presented with reduced vision, astigmatic changes in topography or manifest refraction. The visual acuity, symptoms, and topographical findings all improved after treatment. Histopathologically, all cases fit the newly described entity of ACSH. Careful clinical judgement guided by corneal topography are needed for proper the diagnosis of acquired corneal opacification that results in reduction of vision to identify ACSH from other similar conditions (PHSCD and SND). Peeling of the thickened epithelial and sub-epithelial tissue is curative avoiding the need for corneal re-grafting. [ABSTRACT FROM AUTHOR]

Understanding the mechanical behavior of nanoscale structures is crucial in the development of advanced nanotechnologies. In this study, a novel approach to investigate the thermal lateral vibration of cracked nanobeams immersed in an elastic matrix is investigated. For this purpose, Reddy's third-order shear deformation theory (TSDT) is considered. In contrast to Timoshenko beam theory (First-order Shear Deformation Theory, FSDT), TSDT does not depend on a shear correction coefficient. The nano-scale effect is modeled using Eringen's nonlocal continuum mechanics theory. The nonlocal form of the governing equation is obtained through the application of Hamilton's principle. The weak form of the finite element global mass and stiffness matrices are obtained using Lagrange linear and Hermitian cubic interpolation. To model the crack in bending vibration, two rotational springs are used for TSDT, unlike the use of a single rotational spring in traditional Bernoulli–Euler (Classical Beam Theory, CBT) and FSDT. The stiffness of the springs is adjusted based on the severity of the crack. The influences of the nonlocal parameter, beam slenderness, position of crack, crack severity, Pasternak and Winkler foundation parameters, thermal effects and boundary conditions on the natural frequencies are investigated. The model's outcomes are compared with findings from prior publications, demonstrating a strong level of agreement. This study contributes to the growing research on nanostructures by presenting a novel approach to understanding the dynamics of cracked nanobeams using Reddy beam analysis-based solutions. • Reddy cracked Nanobeam solved using finite element method. • Novel model evaluates crack element based on Reddy Nanobeam analysis. • Influences of nonlocal parameter, slenderness ratio, thermal effects, etc. investigated. • Model results agree with published results. [ABSTRACT FROM AUTHOR]

Graphical abstract Abstract Remarkable efforts are currently devoted to the area of nanodiamonds (NDs) research due to their superior properties viz : biocompatibility, minute size, inert core, and tunable surface chemistry. The use of NDs for the delivery of anticancer drugs has been at the forefront of NDs applications owing to their ability to increase chemosensitivity, sustain drug release, and minimize drug side effects. Accelerated steps towards the move of NDs from bench side to bedside have been recently witnessed. In this review, the effects of NDs production and purification techniques on NDs' final properties are discussed. Special concern is given to studies focusing on NDs use for anticancer drug delivery, stability enhancement and mediated targeted delivery. The aim of this review is to put the results of studies oriented towards NDs-mediated anticancer drug delivery side by side such that the reader can assess the potential use of NDs in clinics and follow up the upcoming results of clinical testing of NDs on animals and humans. [ABSTRACT FROM AUTHOR]

Methylmercury (MeHg) toxicity is associated with extensive neuronal degeneration of dorsal root ganglia (DRG). This study aimed to assess the ameliorative effect of bee venom (BV) on methyl mercury chloride (MeHgCl)-induced peripheral neurotoxicity using DRGs in rats. Forty-eight adult male Sprague Dawley rats were allocated into four equal groups: G I: control (gavaged MilliQ water 1 ml/rat), G II: subcutaneously injected with BV (0.5 mg/kg b.wt), G III: gavaged MeHgCl (6.7 mg/kg b.wt), and G IV: received MeHgCl+BV. Dosing was done five times/week for 2 weeks. Ataxic behavior and visual impairments were significantly increased, whereas the movement behavior and motility gait were suppressed in the MeHgCl group. MeHgCl significantly decreased total antioxidant capacity (TAC) in DRG and significantly decreased the serum levels of glutathione (GSH), catalase (CAT), and superoxide dismutase (SOD). Tumor necrosis factor-alpha (TNF-α) and interleukin 1β (IL-1β) levels were significantly elevated, whereas interleukin 10 (IL-10) levels were significantly decreased in the MeHgCl group compared with the control group. DRGs of the MeHgCl-exposed rats showed pyknotic shrunken neurons with perineural vacuolations, demyelination of nerve axons, and proliferation of the satellite cells. MeHgCl significantly induced a higher positive index ratio of Iba-1, SOX10, neurofilament, pan-neuron, and vimentin immunostaining in the DRG. BV administration significantly mitigated the MeHgCl-induced alterations in oxidative stress-related indices. BV modified the immunostaining of Iba-1, SOX10, neurofilament, pan-neuron, and vimentin-positive index ratio in the DRG of the MeHgCl group. Our findings acknowledged that BV could enhance in vivo neuroprotective effects against MeHgCl-induced DRGs damage in male rats. • Bee venom ameliorates dorsal root ganglia neural (DRG) degeneration induced by methyl mercury. • Bee venom modifies neuro-behavioral alterations induced by methyl mercury in male rats. • Bee venom suppressed serum inflammatory cytokines induced by methyl mercury in rats. • Bee venom boosts the antioxidants serum levels of SOD, CAT, and GSH altered by methyl mercury. • Methyl mercury altered Iba1, Sox10, neurofilament, pan neuron, and vimentin expression in DRG. [ABSTRACT FROM AUTHOR]

Searching for new compounds with anti-inflammatory properties is a significant target since inflammation is a major cause of pain. A series of pyrazole, imidazopyrazolone, and pyrazolopyrimidine derivatives were designed and synthesized by reaction of 3,5-diamino-1 H -pyrazole derivative with cyclic and acyclic carbonyl reagents. The structure of the newly synthesized derivatives were fully characterized using different spectroscopic data and elemental analysis, and therefore, evaluated as COX-2 inhibitors. The in vitro COX-2 activity of the tested derivatives 2 – 13 displayed moderate to good potency with two derivatives 8 and 13 that exhibiting high potency to COX-2 with IC 50 values of 5.68 ± 0.08 and 3.37 ± 0.07 μM compared with celecoxib (IC 50 = 3.60 ± 0.07 μM) and meloxicam (IC 50 = 7.58 ± 0.13 μM). Furthermore, the most active pyrazolo[1,5-a]pyrimidine derivatives 8 and 13 were evaluated to measure the levels of pro-inflammatory proteins such as TNF-α and IL-6 using qRT-PCR in RAW264.7 cells, and the results showed down-regulation of two immunomodulatory proteins. Surprisingly, these derivatives 8 and 13 revealed a decrease in IL-6 level with inhibition percentages of 65.8 and 70.3%, respectively, compared with celecoxib (% = 76.8). Further, compounds 8 and 13 can regulate and suppress the TNF-α with percentage inhibition of 63.1 and 59.2% to controls, while celecoxib displayed an inhibition percentage of 72.7. The Quantum chemical calculation was conducted, and data explained the structural features crucial to the activity. The molecular docking simulation and ADMET predictions revealed that the most active derivatives have good binding affinity, possess appropriate drug-likeness properties and low toxicity profiles. Finally, compounds 8 and 13 demonstrated COX-2 inhibitors with α-TNF and IL-6 suppression capabilities as a dual-action strategy to get more effective treatment. [Display omitted] • A new pyrazole, imidazo [1,2-b]pyrazole, and pyrazolo [1,5-a]pyrimidine derivatives were synthetized and characterized. • The in vitro COX-2 activity of the designed derivatives 2–13 were evaluated. • The structure-activity relationship was enriched. • The pro-inflammatory proteins such as TNF-α and IL-6 were determined for the most active derivatives. • Theoretical studies were performed, including DFT calculation, molecular docking studies, and in silico ADMET prediction. [ABSTRACT FROM AUTHOR]

• Chitosan adsorbed on nanodiamonds and reversed their surface charge from negative to positive side. • Further dextran sulphate coating rendered drug release alkaline-triggered. • TPP- treated, but not dextran sulphate, nanoparticles displayed augmented cytotoxicity. • Chitosan-coated nanodiamonds enhanced doxorubicin retention in bovine urinary bladder. Nanodiamonds (NDs) are an emerging delivery system with a massive surface area qualifying them for efficient loading with various drugs. However, NDs easily scavenge ions upon mixing with physiological media leading to rapid aggregation. Herein, chitosan was employed to endue steric stabilization to NDs and confer adhesiveness to the particles improving their retention in the urinary bladder. The effect of chitosan molecular weight and pH on the particle size and surface charge of chitosan-coated doxorubicin-loaded NDs (Chi-NDX) was investigated. Selected formula exhibited high drug loading efficiency (>90 %), small particle size (<150 nm), good colloidal stability, acid-favored drug release but limited stability in cell culture media. After further stabilization with TPP or dextran sulfate, selected TPP-treated formula displayed more potent cytotoxic effect compared with free doxorubicin and uncoated nanoparticles, and higher drug retention in ex vivo bovine bladder. Therefore, TPP-Chi-NDX is suggested as a promising system for mucosal anticancer delivery. [ABSTRACT FROM AUTHOR]

• Deltamethrin (DLM)-treated fish showed increased creatinine, urea and bilirubin as well as hepatic enzymes (ALP, AST, and ALT). • Blood haemato-immunological variables were decreased in fish exposed to DLM. • DLM toxicity downregulated the transcription of IL-1β and IL-8 , while upregulated HSP70 and CASP3. • The histopathological images revealed damage in gills, intestine, spleen, and liver of fish exposed to DLM. • Lactobacillus plantarum L-137 presented protective effects and restored the antioxidative capacity and the wellbeing of Nile tilapia. Deltamethrin (DLM) is a synthetic pyrethroid used for agricultural purposes to control insects and has been found to pollute the aquatic environment and leads to serious health problems. Lactobacillus plantarum l -137 (L-137) has gained more popularity as functional supplement for its immunomodulatory effects and antioxidant potential. This study was designed to examine the potential of l -137 on liver function, histopathology, immune and antioxidant related gene expressions in Nile tilapia exposed to subacute DLM for 30 days. Fish (mean weight of 28.18 ± 1.34 g) was distributed into four groups (triplicates): the first and second groups fed the control diet, while the third and fourth groups fed l -137 at 50 mg/kg and the second and fourth groups were exposed to DLM (15 μg/L) in rearing water (control, DLM, l -137 and DLM + L-137, respectively). DLM-treated fish groups showed a significant increase in blood biochemical parameters (creatinine, urea and bilirubin) as well as hepatic enzymes (ALP, AST and ALT) (P < 0.05). Blood total protein, globulin, albumin, WBCs, RBCs, Hb, phagocytic index, phagocytic and lysozyme activities were significantly decreased in fish exposed to DLM (P < 0.05). Additionally, DLM toxicity downregulated the transcription of immune genes (IL-1β and IL-8), while upregulated the stress related genes (HSP70 and CASP3). The histopathological images of Nile tilapia exposed to DLM revealed damage in gills, intestine, spleen and liver which confirmed the toxic effects. Conversely, l -137 presented protective effects and restored the aforementioned parameters when fish exposed to DLM and fed l -137. Further, l -137 restored the antioxidative capacity (CAT and GPx). Thus, l -137 supplementation exhibited defensive effects against DLM toxicity in Nile tilapia through improving blood biochemical responses, immune, and antioxidant related gene expressions as well as histopathological effects. [ABSTRACT FROM AUTHOR]