Inhibiting brushite crystal growth: molecular docking exploration of phytoconstituents and their interaction with human serum albumin.

In our preliminary studies, the extract demonstrated inhibition of calcium phosphate (brushite) crystals. Human serum albumin (HSA) is known to act as a promoter of brushite crystal growth. Therefore, the present study aims to explore the molecular mechanisms involved in brushite crystal nephrolithiasis by conducting molecular docking of phytoconstituents from with HSA.

7-Hydroxy-3-(4'-methoxyphenyl) coumarin (C12) attenuates bleomycin-induced acute lung injury and fibrosis through activation of SIRT3.

Silent mating-type information regulation 2 homology 3 (SIRT3) is a member of the sirtuins family expressed in mitochondria performs deacetylation of metabolic enzymes and promotes longevity. 7-hydroxy-3-(4'-methoxyphenyl) coumarin (C12) is a small molecule first ever known for its direct activation of SIRT3. SIRT3 performs its function by balancing the redox system by activating manganese superoxide dismutase (MnSOD) and 8-Oxoguanine glycosylase (OGG1).

Phyto-metabolomic investigation of biologically active fraction of leaf.

(Wight & Arn.) Benth., leaves are used traditionally in variety of diseases.

2-(4-Bromobenzyl) tethered 4-amino aryl/alkyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-]pyrimidines: design, synthesis, anticancer assessment dual topoisomerase-I/II inhibition, and studies.

A series of 2-(4-bromobenzyl) tethered 4-amino aryl/alkyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-]pyrimidines (7a-7u) were designed, synthesized, characterized and screened against a panel of cancer cell lines. Compound 7a, in particular, emerged as a potent antiproliferative agent against FaDu cells (HTB-43) with an IC value of 1.73 μM.

Beyond peptides: Unveiling the design strategies, structure activity correlations and protein-ligand interactions of small molecule inhibitors against PD-1/PD-L1.

The landscape of cancer treatment has been transformed by the emergence of immunotherapy, especially through the use of antibodies that target the PD-1/PD-L1 pathway. Recently, there has been a notable increase in interest surrounding immune checkpoint inhibitors for cancer therapy. While antibody-based approaches have drawbacks like high costs and prolonged activity, the approval of monoclonal antibodies such as pembrolizumab and nivolumab has paved the way for a range of alternative therapies, including peptides, peptidomimetics, and small-molecule inhibitors.

Development of novel tetrazole-based pyruvate kinase M2 inhibitors targeting U87MG glioblastoma cells.

Glioblastoma (GB), the most aggressive and life-threatening primary brain tumor in adults, poses significant therapeutic challenges. Tumor pyruvate kinase M2 (PKM2) has been implicated in the proliferation and survival of glioma cells. In this study, we designed and synthesized a series of 23 novel tetrazole-based derivatives.

Trans-nasal brain delivery of anti-TB drugs by methyl-β-cyclodextrin microparticles show efficient mycobacterial clearance from central nervous system.

Central nervous system tuberculosis (CNS-TB) is the most severe extra-pulmonary manifestation of tuberculosis (TB), facing significant challenges due to the limited penetration of anti-TB drugs (ATDs) across the blood-brain barrier (BBB) and their insufficient concentrations at the site of infection. This study aimed to enhance the efficacy of ATDs by encapsulating them in methyl-β-cyclodextrin (M-β-CD) microparticles (ATD-MP) using spray drying, intended for intranasal delivery to manage CNS-TB. M-β-CD microparticles loaded with isoniazid (INH) and rifampicin (RIF) exhibited spherical shapes with slightly deflated surfaces and particle sizes of 6.

Ultrashort Peptide Hydrogels Biomaterials with Potent Antibacterial Activity.

For the past few decades, ultrashort peptide hydrogels have been at the forefront of biomaterials due to their unique properties like biocompatibility, tunable mechanical properties, and potent antibacterial activity. These ultrashort peptides self-assemble into a hydrogel matrix with nanofibrous networks. In this minireview, we have explored the design and self-assembly of these ultrashort peptide hydrogels by focusing on their antibacterial properties.

New 7-hydroxycoumarin acetamide derivatives as human carbonic anhydrase IX and XII inhibitors: Design, synthesis, biological evaluation and molecular docking studies.

Carbonic anhydrases (CAs) are crucial in regulating various physiological processes in the body. The overexpression of isoforms human carbonic anhydrases (hCA) IX and hCA XII is linked to tumour progression. The selective inhibition of CA IX and CA XII isoforms can result in the development of better cancer treatment strategies.

The Opportunities and Challenges of Mesenchymal Stem Cells-Derived Exosomes in Theranostics and Regenerative Medicine.

Cell-secreted nanovesicles of endosomal origin, called exosomes, are vital for mediating intracellular communication. As local or distal transporters of intracellular cargo, they reflect the unique characteristics of secretory cells and establish cell-specific interactions via characteristic surface proteins and receptors. With the advent of rapid isolation, purification, and identification techniques, exosomes have become an attractive choice for disease diagnosis (exosomal content as biomarkers), cell-free therapy, and tissue regeneration.

(Re)building the nervous system: A review of neuron-glia interactions from development to disease.

Neuron-glia interactions are fundamental to the development and function of the nervous system. During development, glia, including astrocytes, microglia, and oligodendrocytes, influence neuronal differentiation and migration, synapse formation and refinement, and myelination. In the mature brain, glia are crucial for maintaining neural homeostasis, modulating synaptic activity, and supporting metabolic functions.

Ethidium Bromide Degradation by Cold Atmospheric Plasma in Water and the Assessment of Byproduct Toxicity for Environmental Protection.

Ethidium bromide (Et-Br) is a widely used fluorescent dye in molecular biology and biotechnology laboratories for visualizing nucleic acids in agarose gel electrophoresis. However, concerns have been raised about its environmental impact and potential health risks due to its persistence and toxicity. The potential accumulation and long-term effects on the environment necessitate the removal of Et-Br from water.

Imperatorin, a natural furanocoumarin alleviates chronic neuropathic pain by targeting GABAergic tone in an animal model of spinal cord injury.

Chronic neuropathic pain (CNP) caused by spinal cord injury (SCI) has long-term implications, that result in functional deficit. In this study, we explored imperatorin, a natural furanocoumarin isolated from the dried pulp of L. Imperatorin (10 mg/kg, i.

Influence of polymer and surfactant-based precipitation inhibitors on supersaturation-driven absorption of Ibrutinib from high-dose lipid-based formulations.

There is a growing pharmaceutical interest in supersaturated lipid-based formulations (Super-LbF) as an innovative strategy to enhance drug loading capacities while simultaneously reducing pill burden. This approach involves increasing the drug concentration above its equilibrium solubility in a lipid solution, achieved through temperature-induced supersaturation or the dissolution of lipophilic ionic salts. However, the physical instability and potential drug precipitation upon the dispersion of LbF remain critical.

Development of 3-indolyl substituted phenyl pyrazolo-carboxamide hybrids as potential type II VEGFR-2 inhibitors and in vitro cytotoxicity studies.

The progression of tumors is intricately linked to angiogenesis, the formation of new blood vessels, driven primarily by the release of growth factors such as Vascular Endothelial Growth Factor (VEGF). Targeting VEGF signaling through its receptor kinase (VEGFR-2) has emerged as a promising anti-angiogenic strategy for cancer therapy. In this study, we designed and synthesized a series of novel chemical entities based on 3-indolyl substituted phenyl pyrazole-carboxamides through docking studies upon considering the structure of sorafenib and its pattern of type II inhibition of VEGFR-2.

Traditional uses, phytochemistry, pharmacology, and nutraceutical potential of horse gram (Macrotyloma uniflorum): A systematic review.

Macrotyloma uniflorum is known for being a rich source of protein, fat, fiber, carbohydrates, vitamins, and micronutrients. Since ancient times, it has been used as a pulse and traditional remedy in the Himalayan Mountains for curing kidney and bladder stones, bronchitis, asthma, piles, leukoderma, and heart diseases. Horse gram contains bioactive compounds such as phenolic acids, flavonoids, and tannins, which contribute to its health advantages.

Memantine Alleviates PTSD-like Symptoms and Improves Dendritic Arborization through Modulation of the HPA Axis and Neuroinflammation in Rats.

Post-traumatic stress disorder (PTSD) poses significant neurological and psychiatric challenges. Investigations into the glutamatergic system, particularly the N-methyl-D-aspartate (NMDA) receptor, are crucial for understanding PTSD mechanisms. This study aimed to evaluate the therapeutic potential of the non-competitive NMDA receptor antagonist memantine in mitigating PTSD symptoms and to explore its underlying cellular and molecular impacts.

Capsaicin nanocrystals burdened topical polymeric gel: An encouraging tactic for alleviation of paclitaxel-induced peripheral neuropathy.

Chemotherapy-induced peripheral neuropathy (CIPN) is triggered by clinically recommended chemotherapeutics. Topical capsaicin (CAP) is a US-FDA-approved therapeutic entity for the mitigation of CIPN. Besides good skin permeation efficiency, CAP concentration in a topical dermal dosage form must be controlled due to its dose-dependent therapeutic and adverse effects.

Exploring role of citrus fruits in comorbid neurodegenerative disorders associated with psoriasis.

A neurodegenerative illness is a disorder in which the brain and/or spinal cord's neurons, or nerve cells, gradually deteriorate and disappear. These illnesses often get worse with time and can seriously affect movement, cognition, and other neurological functions. Psoriasis is a long-term autoimmune skin condition marked by fast skin cell growth that results in red, elevated areas coated in silvery-white scales.

Discovery of novel hybrid tryptamine-rivastigmine molecules as potent AChE and BChE inhibitors exhibiting multifunctional properties for the management of Alzheimer's disease.

Contemporary research evidence has corroborated a gradual loss of central cholinergic neurons in Alzheimer's Disease (AD). This progressive deterioration leads to cognitive dysfunction and impaired motor activity, culminating in the brain cell's death in the disease. The approved drugs for AD treatment can only offer relief from symptoms without addressing the underlying pathological hallmarks of the disease.

Aminocarbonylation using CO surrogates.

Aminocarbonylation reactions play a critical role in the synthesis of amides. Traditional aminocarbonylation processes often rely on carbon monoxide (CO) gas, a highly toxic and challenging reagent to handle. Recent advancements in CO surrogates address these challenges.

Development of bioengineered 3D patient derived breast cancer organoid model focusing dynamic fibroblast-stem cell reciprocity.

Three-dimensional (3D) models, such as tumor spheroids and organoids, are increasingly developed by integrating tissue engineering, regenerative medicine, and personalized therapy strategies. These advanced 3Dmodels are not merely endpoint-driven but also offer the flexibility to be customized or modulated according to specific disease parameters. Unlike traditional 2D monolayer cultures, which inadequately capture the complexities of solid tumors, 3D co-culture systems provide a more accurate representation of the tumor microenvironment.