Antibiofilm and antivirulence efficacy of Pleurotus platypus methanolic extract against Staphylococcus aureus through ROS generation and cell membrane disruption.

Multi-drug resistance is recognized as a significant worldwide public health concern in the current century. Biofilm formation further exacerbates bacterial resistance to antibacterial medications, host immunological responses, and phagocytosis, resulting in long-lasting chronic illnesses. Investigating natural resources is a very potent approach for developing alternative anti-infective medications to effectively control multi-drug resistant bacterial infections.

Design, Synthesis, and Characterization of Polyoxotungstate-Decorated Ionic Liquid-Based Hybrid Material, [BmIm][SiWO] toward Rapid Adsorption of Dye and Antibacterial Activities.

A multifunctional polyoxometalate-ionic liquid (POM-IL)-based hybrid material comprising silicotungstic acid, [BmIm][SiWO], has been synthesized and demonstrated its efficiency toward methylene blue removal and as an antibacterial agent. Single-crystal XRD analysis confirms that the material crystallizes in monoclinic symmetry (SG: ), with lattice parameters = 13.1396(5) Å, = 16.

Protein kinase C iota promotes glycolysis via PI3K/AKT/mTOR signalling in high grade serous ovarian cancer.

Background: Epithelial ovarian cancer, especially high grade serous ovarian cancer (HGSOC) is by far, the most lethal gynecological malignancy with poor prognosis and high relapse rate. Despite of availability of several therapeutic interventions including poly-ADP ribose polymerase (PARP) inhibitors, HGSOC remains unmanageable and identification of early detection biomarkers and therapeutic targets for this lethal malady is highly warranted. Aberrant expression of protein kinase C iota (PKCί) is implicated in many cellular and physiological functions involved in tumorigenesis including cell proliferation and cell cycle deregulation.

Pharmacological inhibition of protein kinase D2/Aurora kinase A signalling axis suppresses G2/M cell cycle progression and proliferation of epithelial ovarian cancer cells.

Epithelial ovarian cancer (EOC) is the deadliest gynecological malignancy with poor prognosis and patient survival outcome. Protein kinase D2 (PKD2) belongs to Ca/calmodulin-dependent serine/threonine kinase family and its aberrant expression is associated with many cellular and physiological functions associated with tumorigenesis including cell proliferation. We show that PKD2 is activated during G2/M cell cycle transition and its catalytic inactivation by small molecule inhibitor CRT0066101 or genetic knockdown caused suppression of EOC cell proliferation followed by a delay into mitotic entry.

Applications of Inorganic Nanomaterials against Tuberculosis: A Comprehensive Review.

Tuberculosis (TB) continues to pose a significant global health threat, with millions of new infections recorded annually. Current treatment strategies, such as Directly Observed Treatment (DOT), face challenges, including patient non-compliance and the emergence of drug-resistant TB strains. In response to these obstacles, innovative approaches utilizing inorganic/metallic nanomaterials have been developed to enhance drug delivery to target alveolar macrophages, where Mycobacterium tuberculosis resides.

Protein kinase D2-Aurora kinase A-ERK1/2 signalling axis drives neuroendocrine differentiation of epithelial ovarian cancer.

Epithelial ovarian cancer (EOC) is deadliest gynecological malignancy with poor prognosis and patient survival. Despite development of several therapeutic interventions such as poly-ADP ribose polymerase (PARP) inhibitors, EOC remains unmanageable and discovery of novel early detection biomarkers and treatment targets are highly warranted. Although neuroendocrine differentiation (NED) is implicated in different human cancers including prostate adenocarcinoma and lung cancer, mechanistic studies concerning NED of epithelial ovarian cancer are lacking.

Unraveling Multicopper [Cu] and [Cu] Clusters with Rare μ-Sulfato and Linear μ-Oxido-Bridges as Potent Antibiofilm Agents against Multidrug-Resistant .

In this research article, two multicopper [Cu] and [Cu] clusters, [Cu(cpdp)(μ-SO)(Cl)(HO)]·3HO () and [Cu(cpdp)(μ-O)(Cl)(HO)]·2Cl () (Hcpdp = ,'-bis[2-carboxybenzomethyl]-,'-bis[2-pyridylmethyl]-1,3-diaminopropan-2-ol), have been explored as potent antibacterial and antibiofilm agents. Their molecular structures have been determined by a single-crystal X-ray diffraction study, and the compositions have been established by thermal and elemental analyses, including electrospray ionization mass spectrometry. Structural analysis shows that the metallic core of is composed of a trinuclear [Cu] assembly encapsulating a μSO group, whereas the structure of represents a hexanuclear [Cu] assembly in which two trinuclear [Cu] motifs are exclusively bridged by a linear μO group.

A trinuclear Zn (II) schiff base dicyanamide complex attenuates bacterial biofilm formation by ROS generation and membrane damage and exhibits anticancer activity.

A trinuclear Zn (II) complex, [(ZnL{N(CN)})Zn], termed complex 1 has been synthesized by the reaction of an aqueous solution of sodium dicyanamide to the methanolic solution of Zn (CHCOO), 2HO and corresponding Schiff base (HL) which is derived from 1:2 condensation of 1, 4 butane diamine with 3-ethoxy salicylaldehyde. Complex 1 is characterized by elemental analysis, IR, UV and Single X-ray diffraction study. Drug resistance is a growing global public health concern that has prompted researchers to look into advanced alternative treatment modalities.

Pharmacological inhibition of protein kinase D suppresses epithelial ovarian cancer via MAPK/ERK1/2/Runx2 signalling axis.

Epithelial ovarian cancer (EOC) is the most lethal gynaecological malignancy with poor prognosis and dismal patient survival. Although protein kinase D (PKD) isoforms, especially PKD2 and PKD3 are critical for many cellular and physiological functions involved in carcinogenesis including cell proliferation and angiogenesis, their role in human EOC remains unknown. Towards the goal to identify novel prognostic biomarker and therapeutic interventions against EOC, this study aimed to elucidate the molecular roles of PKD2, PKD3 and highly selective, pan-PKD inhibitor CRT0066101 in this lethal pathology.

A mononuclear N,N,N,O donor schiff base Cu(II) complex inhibits bacterial biofilm formation and promotes apoptosis and cell cycle arrest in prostate cancer cells.

In this work, we report a distorted square pyramidal mononuclear copper(II) complex [Cu(L)(NCS)] (1) which was obtained by the reaction of the aqueous solution of ammonium thiocyanate to a methanolic solution of copper nitrate trihydrate and corresponding Schiff-base ligands. Schiff bases, HL (CHNO) act as a tetradentate Schiff base, derived from 1:1 condensation of o-hydroxyacetophenone and diethylenetriamine. The synthesized complex has been successfully characterized based on elemental analysis and Infrared (IR) spectroscopy.

Design, Synthesis and Evaluation of a Series of Zinc(II) Complexes of Anthracene-Affixed Multifunctional Organic Assembly as Potential Antibacterial and Antibiofilm Agents against Methicillin-Resistant .

A novel class of zinc(II)-based metal complexes, i.e., [Zn(acdp)(μ-Cl)]·2HO (), [Zn(acdp)(μ-NO)]·2HO (), and [Zn(acdp)(μ-OCCF)]·2HO () (Cl = chloride; NO = nitrate; CFCO = trifluoroacetate) of anthracene-affixed multifunctional organic assembly, Hacdp (Hacdp = ,'-bis[anthracene-2-ylmethyl]-,'-bis[carboxymethyl]-1,3-diaminopropan-2-ol), have emerged as promising antibacterial and antibiofilm agents in the domain of medicinal chemistry.

Runt-related transcription factors in human carcinogenesis: a friend or foe?

Purpose: Cancer is one of the deadliest pathologies with more than 19 million new cases and 10 million cancer-related deaths across the globe. Despite development of advanced therapeutic interventions, cancer remains as a fatal pathology due to lack of early prognostic biomarkers, therapy resistance and requires identification of novel drug targets.

Methods: Runt-related transcription factors (Runx) family controls several cellular and physiological functions including osteogenesis.

Development of Copper Nanoparticle Conjugated Chitosan Microparticle as a Stable Source of 2nm Copper Nanoparticle Effective against Methicillin- resistant .

Background: Copper nanoparticle (CuNP) has well-established antimicrobial activity. Instability in an aqueous medium due to aggregation into larger particles, conversion into metal ions, and oxidation into metal oxides are the major limitations of its practical use against bacterial infections.

Objective: Development of CuNP Conjugated Chitosan Microparticles as a reservoir that will release CuNP effective against notorious bacteria like Methicillin-resistant Staphylococcus aureus.

Recent advances in understanding the molecular role of phosphoinositide-specific phospholipase C gamma 1 as an emerging onco-driver and novel therapeutic target in human carcinogenesis.

Phosphoinositide metabolism is crucial intracellular signaling system that regulates a plethora of biological functions including mitogenesis, cell proliferation and division. Phospholipase C gamma 1 (PLCγ1) which belongs to phosphoinositide-specific phospholipase C (PLC) family, is activated by many extracellular stimuli including hormones, neurotransmitters, growth factors and modulates several cellular and physiological functions necessary for tumorigenesis such as cell survival, migration, invasion and angiogenesis by generating inositol 1,4,5-triphosphate (IP3) and diacylglycerol (DAG) via hydrolysis of phosphatidylinositol 4,5-biphosphate (PIP2). Cancer remains as a leading cause of global mortality and aberrant expression and regulation of PLCγ1 is linked to a plethora of deadly human cancers including carcinomas of the breast, lung, pancreas, stomach, prostate and ovary.

Recent advancements in therapeutic targeting of the Warburg effect in refractory ovarian cancer: A promise towards disease remission.

Epithelial ovarian cancer, the most lethal gynecological malignancy, is diagnosed at advanced stage, recurs and displays chemoresistance to standard chemotherapeutic regimen of taxane/platinum drugs. Despite development of recent therapeutic approaches including poly-ADP ribose polymerase inhibitors, this fatal disease is diagnosed at advanced stage and heralds strategies for early detection and improved treatment. Recent literature suggests that high propensity of ovarian cancer cells to consume and metabolize glucose via glycolysis even in the presence of oxygen (the 'Warburg effect') can significantly contribute to disease progression and chemoresistance and hence, it has been exploited as novel drug target.

Combination of and Heat-Induced Promastigotes Cures Drug-Resistant Infection: Critical Role of Interleukin-6-Producing Classical Dendritic Cells.

The major issues in available therapeutic modalities against leishmaniasis are cost, toxicity, and the emergence of drug resistance. The aim of this work was to develop a successful therapeutic adjuvant against drug-resistant infection by means of combining with heat-induced promastigotes (HIP). One-month postinfected BALB/c mice were administered subcutaneously with (10 cells) and HIP (100 μg) for 5 days.

Development of bicalutamide-loaded PLGA nanoparticles: preparation, characterization and in-vitro evaluation for the treatment of prostate cancer.

In this study we report the development and optimization of poly (D, L-lactide-co-glycolide) (PLGA) polymer encapsulated poorly aqueous soluble nonsteroidal antiandrogen drug bicalutamide, to develop a sustained release formulation for the treatment of prostate cancer. The bicalutamide-loaded PLGA nanoparticles were prepared by single emulsion (O/W) solvent evaporation method, and different process parameters like polymer concentration in the organic phase, surfactant concentration in aqueous phase and centrifugation speed for separation of nanoparticles were evaluated to optimize the drug-loaded nanoparticles. The optimum formulation of bicalutamide-loaded PLGA nanoparticles characterized extensively by different analytical techniques like laser light scattering to determine average particle size and size distribution, scanning electron microscopy (SEM) for surface morphology, powder X-ray diffraction (PXRD) for surface chemistry and differential scanning calorimetry (DSC) for thermogram properties.

Induction of apoptosis by zerumbone isolated from Zingiber zerumbet (L.) Smith in protozoan parasite Leishmania donovani due to oxidative stress.

In the present context of emergence of resistance aligned with the conventional anti-leishmanial drugs and occasional treatment failure compelled us to continue the search for replaceable therapeutic leads against Leishmania infection. Various ginger spices of the Zingiberaceae family are widely used as spices, flavouring agents, and medicines in Southeast Asia because of their unique flavour as well as due to their medicinal properties. Zerumbone, a natural component of Zingiber zerumbet (L.

A novel triterpene from Astraeus hygrometricus induces reactive oxygen species leading to death in Leishmania donovani.

Aim: The effect of astrakurkurone, a novel triterpene, isolated from Indian mushroom Astraeus hygrometricus has been investigated to elucidate the mechanisms involved in selective cell death of Leishmania donovani.

Materials & Methods: The hypotheses were investigated using flow-cytometry, scanning electron microscopy and confocal microscopy.

Results: The time dependent elevation of astrakurkurone-induced reactive oxygen species (ROS) was found intimately associated with apoptosis.

Synthesis and biological evaluation of ferrocenylquinoline as a potential antileishmanial agent.

The emergence of resistance against antileishmanial drugs in current use necessitates the search for new classes of antileishmanial compounds. Herein we report the design, synthesis, and evaluation of a novel ferrocenylquinoline for activity against Leishmania donovani. 7-Chloro-N-[2-(1H-5-ferrocenyl-1,2,3-triazol-1-yl)ethyl]quinolin-4-amine (1) was generated by coupling an iron(II) ethynylferrocene species with 4-(2-ethylazido)amino-7-chloroquinoline using click chemistry.

Selective inhibition of Leishmania donovani by active extracts of wild mushrooms used by the tribal population of India: An in vitro exploration for new leads against parasitic protozoans.

The study was intended at evaluating the anti-proliferating effect of mushrooms used in traditional folklore of Santal tribal population in India against Leishmania donovani (MHOM/IN/83/AG83). A total of eighteen extracts, three estracts from each mushroom [(80% ethanol extracted; Fa), (water-soluble polysaccharide fraction; Fb), (polyphenolic fraction; Fc)], from six wild mushrooms were obtained. These extracts were tested against the promastigotes and amastigotes for their antileishmanial capacity.