Tubulin- and ROS-dependent antiproliferative mechanism of a potent analogue of noscapine, N-propargyl noscapine.

Aim: To rationally-design, synthesize, characterize, biologically evaluate, and to elucidate the anticancer mechanism of action of a novel analogue of noscapine, N-propargyl noscapine (NPN), as a potential drug candidate against triple-negative breast cancer (TNBC).

Materials And Methods: After the synthesis and IR, H, C NMR and mass spectral characterization of NPN, its antiproliferative efficacy against different cancer cell lines was investigated using Sulforhodamine B assay. Cell cycle progression was analysed using flow cytometry.

Cefoperazone sodium liposomal formulation to mitigate P. aeruginosa biofilm in Cystic fibrosis infection: A QbD approach.

Cystic fibrosis (CF), an atypical genetic disorder, develops due to mutations in cystic fibrosis transmembrane conductance regulator gene, which consequently leads to infection and inflammation. CF infections are commonly characterized by the presence of an extracellular polymeric substance (EPS) matrix or the 'biofilm', which presents an entry barrier for the antibiotics. The current research work focuses on systematic Quality by Design based development of cefoperazone sodium loaded liposome formulation.

Molecular study of binding of Plasmodium ribosomal protein P2 to erythrocytes.

The ribosomal protein P2 of Plasmodium falciparum, (PfP2), performs certain unique extra-ribosomal functions. During the few hours of cell-division, PfP2 protein moves to the external surface of the infected erythrocytes (IE) as an SDS-resistant oligomer, and at that stage treatment with specific anti- PfP2 antibodies results in an arrest of the parasite cell-division. Amongst the oligomeric forms of PfP2, mainly the homo-tetramer is peripherally anchored on the external surface of the IE.

The reorganization of conformations, stability and aggregation of serum albumin isomers through the interaction of glycopeptide antibiotic teicoplanin: A thermodynamic and spectroscopy study.

The drugs-protein binding study is of growing importance for drug-repurposing against amyloidosis. In this work, we study the binding of teicoplanin (TPN), a glycopeptide antibiotic, with bovine serum albumin (BSA) in its neutral (N), physiological (P) and basic (B) forms, which exist at pH 6, pH 7.4 and pH 9, respectively.

Internally functionalized multifaceted organochalcogen compounds.

Two families of internally functionalized multifaceted organochalcogen compounds based on flexible and rigid backbones, viz., N,N-dimethylaminoalkyl and pyridyl/pryrimidyl groups, have been designed and developed in the author's group. These compounds exhibit remarkable ligand chemistry and often show unprecedented reactivity leading to the formation of several serendipitous products.

All-in-one NMR spectroscopy of small organic molecules: complete chemical shift assignment from a single NMR experiment.

A new class of NOAH NMR experiments (NOAH-AST and NOAH-AST), with the abbreviations, A: 1,1-ADEQUATE, S: sensitivity improved version of multiplicity-edited (ME)-HSQC, T: TOCSY, and T: pure shift TOCSY, are reported to obtain complete chemical shift assignments of small organic molecules from a single NMR experiment. While NOAH-AST provides C-C, H-C, and H-H connectivities for molecules with well resolved chemical shifts, NOAH-AST experiments discern H-H connectivities even in complex organic molecules such as steroids at ultra-high resolution. These methods are very flexible and allow to record data through non-uniform-sampling, which reduces the experimental time to a great extent.

Unraveling the anti-biofilm potential of green algal sulfated polysaccharides against Salmonella enterica and Vibrio harveyi.

One of the main reasons for the bacterial resistance to antibiotics is caused by biofilm formation of microbial pathogens during bacterial infections. Salmonella enterica and Vibrio harveyi are known to form biofilms and represent a major health concern worldwide, causing human infections responsible for morbidity and mortality. The current study aims to investigate the effect of purified sulfated polysaccharides (SPs) from Chlamydomonas reinhardtii (Cr) on planktonic and biofilm growth of these bacteria.

Glutamic acid-coated FeO nanoparticles for tumor-targeted imaging and therapeutics.

We have developed surface functionalised FeO magnetic nanoparticles (MNPs) based system that can be used for tumor-targeted multimodal therapies and MR imaging. Biocompatible, non-essential amino acid (glutamic acid) was introduced onto the surface of FeO MNPs to provide functional sites for binding of chemotherapeutic drugs. These glutamic acid-coated FeO MNPs (GAMNPs) exhibit good water-dispersibility, magnetic responsivity and pH dependent charge conversal feature.

Enterococcus durans with mosquito larvicidal toxicity against Culex quinquefasciatus, elucidated using a Proteomic and Metabolomic approach.

Various bacteria from the Bacillus species have been used as pesticides against mosquito larvae for more than a decade. The prolonged use of these bacterial species by little alteration within their genome, using various permutations and combinations of mosquito-cidal toxins, has proven unsuccessful in controlling the mosquito population. In our current study we report Enterococcus sp.

Reactivity Parameters and Substitution Effect in Organic Acids.

We investigate a few density functional theory-based reactivity indices of chemistry, with a view to arrive at an intercomparison and also consider their applications toward the problems of chemical significance. In particular, we propose to use the concepts of fugality and atom-atom polarizability to study the acidic strength of substituted benzoic acid derivatives. The nature of the variations and trends in the correlation of reactivity parameters and p values is shown to provide an insight into the applicability of these concepts to such reactions.

Functional characterization of an inducible bidirectional promoter from Fusarium oxysporum f. sp. cubense.

Bidirectional promoters (BDPs) are regulatory DNA sequences (~1000 bp long) intervening two genes arranged on opposite strands with their 5' ends in close proximity. These genes are mostly co-expressed; but, instances of anti-correlation and independent transcription have been observed. In fungal systems, BDPs have shown to provide an improved genetic circuit by assembling and regulating transcription of different genes of a common metabolic pathway.

Herbalome of Chandraprabha vati, a polyherbal formulation of Ayurveda prevents fibrillation of lysozyme by stabilizing aggregation-prone intermediate state.

Lysozyme amyloidosis (ALys) is caused by the deposition of amyloid-like fibrils of lysozyme in the tissues of the gastrointestinal tract, liver and kidneys. The treatment/prevention of ALys is not known yet. Therefore, searching for therapeutic agents for amyloidosis is of great value.

Tryptone-stabilized gold nanoparticles induce unipolar clustering of supernumerary centrosomes and G1 arrest in triple-negative breast cancer cells.

Gold nanoparticles of different sizes, shapes, and decorations exert a variety of effects on biological systems. We report a novel mechanism of action of chemically modified, tryptone-stabilized gold nanoparticles (T-GNPs) in the triple-negative breast cancer (TNBC) cell line, MDA-MB-231. The T-GNPs, synthesized using HAuCl.

Cell death mechanisms in eukaryotes.

Like the organism they constitute, the cells also die in different ways. The death can be predetermined, programmed, and cleanly executed, as in the case of apoptosis, or it can be traumatic, inflammatory, and sudden as many types of necrosis exemplify. Nevertheless, there are a number of cell deaths-some of them bearing a resemblance to apoptosis and/or necrosis, and many, distinct from each-that serve a multitude of roles in either supporting or disrupting the homoeostasis.

Polyamine acetylation and substrate-induced oligomeric states in histone acetyltransferase of multiple drug resistant Acinetobacter baumannii.

Histone acetyltransferase (Hpa2) is an unusual acetyltransferase, with a wide range of substrates; including histones, polyamines and aminoglycosides antibiotic. Hpa2 belongs to GNAT superfamily and GNATs are well known for the formation of homo-oligomers. However, the reason behind their oligomerization remained unexplored.

Excitation functions of the Zn(p,xn)Ga reactions.

The excitation functions for Zn(p,n)Ga and Zn(p,2n)Ga have been calculated for incident proton energies from threshold values to 30 MeV using the statistical model code TALYS-1.6. The (p,n) and (p,2n) cross sections have been calculated using both phenomenological Koning and Delaroche (KD) and semimicroscopic Jeukenne-Lejeune-Mahaux-Bruyeres (JLMB) optical model potentials.

The physical basis of fabrication of amyloid-based hydrogels by lysozyme.

The fabrication of amyloid-based hydrogels has attracted remarkable attention within the field of materials science and technology. These materials have a multitude of potential applications in the biomaterials field such as developing scaffolds for tissue engineering, drug delivery and hygiene products. Despite the potential new applications of these materials, the physical nature of their assembly is not well understood.

Stimulus-Responsive Supramolecular Host-Guest Assembly of a Cationic Pyrene Derivative with Sulfated β-Cyclodextrin.

In general, aggregation-prone organic molecules are prevented from self-aggregation in the presence of macrocyclic hosts like β-cyclodextrin because of their preference for the formation of inclusion complex with guest molecules. On the contrary, sulfate-laced β-cyclodextrin has been recently reported to induce the aggregation of some of the non-aggregation-prone organic dyes, which have been subsequently utilized for biosensing applications. In the present contribution, we report the interaction of a cationic organic probe molecule, 1-pyrene methyl amine (PMA), which belongs to one of the most useful families of organic fluorescent probes, that is, pyrene, with a sulfated β-cyclodextrin derivative (SCD).

Oral administration of 3,3'-diselenodipropionic acid prevents thoracic radiation induced pneumonitis in mice by suppressing NF-kB/IL-17/G-CSF/neutrophil axis.

The incidence of symptomatic radiation induced lung pneumonitis (RILP), a major dose limiting side effect of thoracic radiotherapy, is in the range of 15-40%. Therapeutic options for the prevention and treatment of RILP are limited. Hence there is a need for developing novel radioprotectors to prevent RILP which can be patient compliant.

Natural compound safranal driven inhibition and dis-aggregation of α-synuclein fibrils.

Self-assembly of α-synuclein (α-Syn) is linked with a variety of neurodegenerative diseases collectively called as α-synucleiopathies. Therefore, discovering suitable inhibitors for this self-association process of α-Syn is a subject of intense research. In this background, we have demonstrated here that the natural compound, Safranal, delays/inhibits α-Syn fibrillation/aggregation, and we have also characterized its mode of action.

Triphala inhibits alpha-synuclein fibrillization and their interaction study by NMR provides insights into the self-association of the protein.

The process of assembly and accumulation of the intrinsically disordered protein (IDP), alpha-synuclein (αSyn) into amyloid fibrils is a pathogenic process leading to several neurodegenerative disorders such as Parkinson's disease, multiple system atrophy and others. Although several molecules are known to inhibit αSyn fibrillization, the mechanism of inhibition is just beginning to emerge. Here, we report the inhibition of fibrillization of αSyn by Triphala, a herbal preparation in the traditional Indian medical system of Ayurveda.

Perturbation of tubulin structure by stellate gold nanoparticles retards MDA-MB-231 breast cancer cell viability.

Gold nanoparticles (GNPs) of different sizes and shapes have been investigated extensively for their therapeutic potential against several diseases including cancer. However, the mechanisms with which they affect the cells are yet to be fully comprehended. In this study, we report the strong antiproliferative potential of novel, star-shaped ("stellate") GNPs that target tubulin-the building-block protein of the cytoskeletal filaments called microtubules-and disrupt microtubule network integrity.

Deciphering the anti-Parkinson's activity of sulphated polysaccharides from Chlamydomonas reinhardtii on the α-Synuclein mutants A30P, A53T, E46K, E57K and E35K.

Parkinsonism-linked mutations in alanine and glutamic acid residues of the pre-synaptic protein α-Synuclein (α-Syn) affect specific tertiary interactions essential for stability of the native state and make it prone to more aggregation. Many of the currently available drugs used for the treatment of Parkinson's disease (PD) are not very effective and are associated with multiple side effects. Recently, marine algae have been reported to have sulphated polysaccharides which offers multiple pharmaceutical properties.

Evaluating the antibacterial and antibiofilm potential of sulphated polysaccharides extracted from green algae Chlamydomonas reinhardtii.

Aim Of The Study: In this study, antibacterial and antibiofilm potential of sulphated polysaccharides (SPs) extracted from Chlamydomonas reinhardtii (Cr) was evaluated against Neisseria mucosa, Escherichia coli, Streptococcus sp. and Bacillus subtilis.

Methods And Results: Antibacterial potential of Cr-SPs was evaluated by agar-cup diffusion, time-kill and colony-forming ability (CFU), minimum inhibitory and bactericidal concentration assays.

Vertical flow paper-based plasmonic device for cysteine detection.

Cystinuria, is an autosomal recessive genetic disorder involving increasingly high levels of poorly soluble cysteine in urine leading to formation of stones. Developing a facile, low-cost, point-of-care and selective sensor for diagnosis of cysteine is imperative. Accordingly, for the detection of cysteine, the present study demonstrates an inexpensive colorimetric, paper-based vertical flow plasmonic micro-well device with a two-minute turn-around time.