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.

Molecular profiling and anti-infective potency of endophytic actinomycetes inhabiting Madhuca insignis Radlk., from Western Ghats of India.

Background: Endophytic actinomycetes are well known for their diverse bioactive entities and considered as an important source for drug development research.

Results: We isolated and identified four potential endophytic Streptomyces species, i.e.

Direct observation of effect of crowding induced macromolecular hydration on molecular breathing in the stem of Fork-DNA by single-molecule FRET microspectroscopy.

The perpetually changing cellular conditions, nucleotide sequence, and environmental effects including osmotic stress have multiple effects on DNA, leading to several conformational alternations and subsequently influencing their activity, too. In this work, single-molecule FRET microspectroscopy has been employed to monitor the breathing dynamics as an effect of molecular crowding in the stem region of Fork-DNA. The structural integrity greatly alters with the presence or absence of nucleotide overhangs and on the nature and concentration of the crowding agent, thus affecting the stability of the stem region and hence the forked DNA.

Molecular profiling of endophytic Streptomyces cavourensis MH16 inhabiting Millingtonia hortensis Linn. and influence of different culture media on biosynthesis of antimicrobial metabolites.

Endophytic actinomycetes, a prolific source of natural products, are well known for their diverse metabolic versatility, and their association with medicinal plants and antimicrobial potential are well worth exploring. We isolated and identified the Streptomyces cavourensis strain MH16 inhabiting the tree Millingtonia hortensis Linn. using phylogenetic analysis based on a 16S rRNA molecular approach.

In Silico Screening and Binding Characterization of Small Molecules toward a G-Quadruplex Structure Formed in the Promoter Region of Oncogene.

Overexpression of oncogene is associated with cancer pathology. Expression of is regulated by the G-quadruplex structure formed in the G-rich segment of nuclease hypersensitive element (NHE III), that is, "", which is localized in the promoter region. Ligand-induced stabilization of the structure has been identified as a novel target for cancer therapeutics.

LINCRNA00273 promotes cancer metastasis and its G-Quadruplex promoter can serve as a novel target to inhibit cancer invasiveness.

Discovery of anti-metastatic drugs is of immense clinical significance as metastasis is responsible for 90% of all cancer deaths. Here we report the inhibitory effect of a bis schiff base (M2) on cancer cell migration and invasion and . M2 has shown good solubility and permeability across the intestinal cell wall and hence can be classified as BCS (Biopharmaceutical classification system) class I.

Chelerythrine down regulates expression of VEGFA, BCL2 and KRAS by arresting G-Quadruplex structures at their promoter regions.

A putative anticancer plant alkaloid, Chelerythrine binds to G-quadruplexes at promoters of VEGFA, BCL2 and KRAS genes and down regulates their expression. The association of Chelerythrine to G-quadruplex at the promoters of these oncogenes were monitored using UV absorption spectroscopy, fluorescence anisotropy, circular dichroism spectroscopy, CD melting, isothermal titration calorimetry, molecular dynamics simulation and quantitative RT-PCR technique. The pronounced hypochromism accompanied by red shifts in UV absorption spectroscopy in conjunction with ethidium bromide displacement assay indicates end stacking mode of interaction of Chelerythrine with the corresponding G-quadruplex structures.

Myricetin arrests human telomeric G-quadruplex structure: a new mechanistic approach as an anticancer agent.

The use of small molecules to arrest G-quadruplex structure has become a potential strategy for the development and design of a new class of anticancer therapeutics. We have studied the interaction of myricetin, a plant flavonoid and a putative anticancer agent, with human telomeric G-quadruplex TTAGGG(TTAGGG)3 DNA. Reverse transcription PCR data revealed significant repression in hTERT expression in MCF-7 breast cancer cells upon increasing the concentration of myricetin.

Reverse Watson-Crick G-G base pair in G-quadruplex formation.

A stable intermediate dimeric G-rich form as a precursor of tetrameric G-quadruplex structures has been detected via MALDI-TOF spectrometry. Molecular dynamics simulation offered detailed insights at the atomic level, assigning reverse Watson-Crick G-G base pairing (not Hoogsteen) in the G-rich dimer. In support of this, cisplatin formed a stable adduct by binding to the dimeric G-rich structure, eliminating the possibility of G-G Hoogsteen hydrogen bond formation.

Tigecycline activity against metallo-β-lactamase-producing bacteria.

Background: [corrected] Treatment of serious life-threatening multi-drug-resistant organisms poses a serious problem due to the limited therapeutic options. Tigecycline has been recently marketed as a broad-spectrum antibiotic with activity against both gram-positive and gram-negative bacteria. Even though many studies have demonstrated the activity of tigecycline against ESBL-producing Enterobacteriaceae, its activity is not well-defined against micro-organisms producing metallo-β-lactamases (MBLs), as there are only a few reports and the number of isolates tested is limited.

Immunolocalization of fascin, an actin-bundling protein and glial fibrillary acidic protein in human astrocytoma cells.

Fascin is a 55-kDa globular protein that functions to organize filamentous-actin into parallel bundles. A role for fascin in cell migration has led to its study in many tumor types. In this report, we investigate fascin in astrocytomas.

p14ARF interacts with DAXX: effects on HDM2 and p53.

The p14(ARF) (ARF) tumour suppressor plays an important role in the cellular response to oncogene activation. In this report, we demonstrate an interaction between ARF and DAXX, a highly conserved protein with identified roles in the regulation of gene expression. HDM2 was shown to interact with each of ARF and DAXX upon upregulation of expression as well as at lower expression levels following transfection of ARF and DAXX.

Sloppy paired 1/2 regulate glial cell fates by inhibiting Gcm function.

Organization of the central nervous system during embryonic development is an intricate process involving a host of molecular players. The Drosophila segmentation genes, sloppy paired (slp) 1/2 have been shown to be necessary for development of a neuronal precursor cell subtype, the NB4-2 cells. Here, we show that slp1/2 also have roles in regulating glial cell fates.

Expression of fascin, an actin-bundling protein, in astrocytomas of varying grades.

Malignant astrocytomas are highly infiltrative neoplasms that invade readily into regions of normal brain. On a cellular basis, the motility and invasiveness of human cancers can be ascribed in part to complex rearrangements of the actin cytoskeleton that are governed by several actinbinding proteins. One such actin-binding protein that has been linked to the invasive behavior of carcinomas is fascin, which serves to aggregate F actin into bundles.

Dose and time-related in vitro effects of glucocorticoid on phagocytosis and nitrite release by splenic macrophages of wall lizard Hemidactylus flaviviridis.

Glucocorticoids (GC) are usually considered to be immunosuppressive and anti-inflammatory. However, recent studies in mammals have demonstrated the diverse effects of GC on non-specific host-defense mechanism, depending on dose or duration of treatment. Hence, in the present study in vitro dose and time-related effects of glucocorticoid, i.

In vitro effect of sex steroids on cytotoxic activity of splenic macrophages in wall lizard (Hemidactylus flaviviridis).

Sexual dimorphism was observed in nitrite release and IL-1-like molecule production by splenic macrophages of the wall lizard (Hemidactylus flaviviridis), with a higher level in females than in males. Gonadectomy in both males and females resulted in a considerable increase of nitrite and IL-1-like molecule secretion, suggesting that the sex hormones inhibit cytotoxic activity of macrophages. To verify this assumption, dose- and time-related in vitro experiments with male and female sex steroids, dihydrotestosterone (DHT) and 17beta-estradiol (E(2)), respectively, were carried out.