RESUMEN

The treatment of Methicillin-resistant staphylococcus aureus (MRSA) infections has become challenging due to the growth of multidrug resistance in the bacteria. Here we report the synthesis of pyridine-coupled pyrazoles as an antimicrobial agent against MRSA. A series of pyridine coupled pyrazoles were synthesized and synthesized compounds were characterized using FT-IR, 1H NMR, and Mass spectroscopy. The ADMET results of all the 14 active compounds are interpreted. To identify the potent compound the synthesized compounds screened for minimum inhibitory concentrations against MRSA and compared with standard drug vancomycin. Among the synthesized compounds 6d exhibited good antibacterial activity with MIC value 21 µg/mL, bacterial cell membrane damage study was studied potassium efflux, and cellular content leakage assay. Anticoagulant study for the potent compound also studied and validated by molecular docking and molecular dynamics simulation studies. The docking study of the synthesized compound was carried out and the study depicted that the pyridine ring of all the analogues binds with the various amino acids in the binding pocket of the active site of the Staphylocoagulase and PBP2a protein of MRSA.

Asunto(s)

RESUMEN

Enterobacter cloacae is normally considered to be an opportunistic human pathogen. Here, we report on the whole-genome sequence of an endophytic E. cloacae, strain "Ghats1", isolated from leaves of the medicinal plant Coscinium fenestratum Gaertn. Functional analysis of the Ghats1 genome revealed an enrichment for genes involved in the uptake and exchange of nutrients, for chemotaxis and for plant colonization. Unexpectedly though, there were no ORFs belonging to the "virulence factors and antibiotic resistance". Moreover, the presence of hydrolytic enzymes and motility functions reveals the characteristics of an endophyte lifestyle of a bacterium that can colonize and adapt to plant environment. These results provide a better understanding of an endophytic lifestyle through plant-microbe interaction, which can be further exploited as a biocontrol agent.

Asunto(s)

RESUMEN

A rare actinobacteria strain designated SCA21, producing bioactive metabolites was isolated from marine sediment of Havelock Island, Andaman and Nicobar Islands, India. Analysis of 16S rRNA sequences suggested that the strain SCA21 belonged to the genus Nocardiopsis. Chemical investigation of the fermentation broth led to the isolation of two pure bioactive compounds (1-2). Compound 1: 4-bromophenol, a bromophenol derivative; Compound 2: Bis (2-ethylhexyl) phthalate, a phthalate ester. The structure of compound 1 and 2 were elucidated by the detailed analysis of FT-IR, HR-ESI-MS, 1D and 2D NMR, along with literature data analysis. The isolated metabolites were evaluated for enzyme inhibition activity against α-glucosidase and α-amylase, free radical scavenging activity against DPPH and ABTS radicals, metal chelating and antibacterial activity against clinical pathogens. 1 and 2 exhibited remarkable enzyme inhibitory activities against α-glucosidase. However, Compound 2 was found less active against α-amylase. They showed significant free radical scavenging activity against DPPH and ABTS radicals. In addition, except the strain Salmonella typhi ATCC 25241 and Listeria cytogens ATCC 13932, 1 and 2 showed broad spectrum inhibitory activity against MRSA ATCC NR-46171, MRSA ATCC-46071, Klebsiella pneumonia ATCC 13883, Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 12600. In conclusion, to best of our knowledge these findings are the first report of isolation of 4-bromophenol and Bis (2-ethylhexyl) phthalate from genus Nocardiopsis, thus suggesting that rare actinomycetes are promising source of therapeutically important bioactive metabolites.

Asunto(s)

RESUMEN

Biogenic synthesis of nanoparticles has received a tremendous attention from the past few decades. The significant progress in the field of nanotechnology has resulted in a cost-effective and eco-friendly process for nanoparticle synthesis. In the present study, the extracellular synthesis of gold nanoparticles was carried out using culture supernatant of Streptomyces griseoruber, actinomycetes isolated from the soil. Bioreduction of gold nanoparticles was confirmed by UV-visible spectrophotometer that showed the peak between 520 and 550 nm. The crystalline nature and mean size of the GNPs were confirmed using XRD. FTIR revealed the possible functional group that could be useful in immobilisation and stabilisation of GNPs. Size and distribution of the biosynthesized GNPs were analysed by HR-TEM that showed the formation of GNPs in the range of 5-50 nm. The synthesised GNPs showed good catalytic activity for the degradation of methylene blue. The study shows the rapid and eco-friendly synthesis of GNPs from Streptomyces griseoruber, and this is the first report on the catalytic activity of GNPs from actinomycetes so far.

RESUMEN

To control the severe problem of microbiologically influenced corrosion, industries require highly potent antibacterial agent which can inhibit the growth of bacteria on man-made surfaces. This need drove the research towards the synthesis of nanoscale antimicrobial compounds. We, therefore, screened several bacteria for the biosynthesis of copper/copper compound nanoparticles which could inhibit the growth of Desulfovibrio marinisediminis, a sulfate reducing bacterium. Supernatant of thirty bacteria isolated from the biofilm formed on ship hull was mixed with 1 mM CuCl2 solution at room temperature. Eight bacterial strains, whose mixtures exhibited colour change, were selected for antimicrobial test. One nanoparticle which has been biosynthesized by Shewanella indica inhibited the growth of D. marinisediminis. Characterization of this particle by UV-visible spectrophotometer, XRD, TEM, DLS and FTIR showed that the particle is polydisperse CuO nanoparticle with average size of 400 nm.

RESUMEN

The opportunistic pathogen Pseudomonas aeruginosa uses biofilm lifestyle to resist antibiotic treatment. In our study, endophytic bacterium Enterobacter aerogenes VT66 quenched the N-acyl homoserine lactone (AHL) molecules produced by P. aeruginosa PAO1. The quorum quenching activity was attributed to the presence of AHL-lactonase. The AHL-lactonase was purified using column chromatography and purified AHL-lactonase was applied for the control of biofilm formation in P. aeruginosa PAO1. The results showed that purified AHL-lactonase obtained with a molecular weight about 30kDa was able to inhibit more than 70% of biofilm in P. aeruginosa PAO1 (P<0.001). Antibiofilm activity of AHL-lactonase was correlated well with results from staining technique used to determine inhibition of biomass and viable cell activity. Therefore, results unambiguously confirm that the AHL-lactonase from E. aerogenes VT66 could be used as antibiofilm therapeutics in P. aeruginosa associated biomedical applications.

Asunto(s)

RESUMEN

In this study, antimicrobial and antioxidant activities of the hexane extract of the root of Ventilago madraspatana were evaluated. Based on the significant bioactivity of crude hexane extract, an active compound was purified from the root extract. The active compound was further purified and identified as aromodendrin-4'-methyl ether by the (1)H NMR spectrum. The isolated compound significantly inhibited Staphylococcus epidermidis with the lowest MIC and MBC at 78 µg/mL (P < 0.05). The compound also exhibited significant anticandidal activity with MIC and MBC values of 312 and 625 µg/mL, respectively. The radical scavenging activity of aromodendrin-4'-methyl ether was evident by its lower IC50 values of 60 µg/mL for DPPH scavenging and 3.2 µg/mL for ABTS scavenging. The compound also exhibited ferrous ion chelation and H2O2 scavenging activities. The study is an attempt to increase the industrial utility of V. madrasapatana.

Asunto(s)

RESUMEN

AHL-lactonase has gained renewed interest due to biotechnological applications such as antiquorum sensing, antibiofilm strategies, biofouling, etc. In our study, the production of AHL-lactonase from endophytic bacteria Enterobacter aerogenes VT66 was optimized by response surface methodology (RSM) using central composite design (CCD) for four different cultural conditions. The relative activity of AHL-lactonase was correlated with amplification of aiiA homologous gene amplification with respect to cultural conditions. Statistical analysis by ANOVA of the quadratic regression model showed that the RSM model constructed is highly significant, as indicated by F-test with a low probability value (p(model) < 0.0001) and high regression coefficient (0.9997) as well as lower coefficient of variation (1.86%) indicate that suitability of variable parameters. The quadratic regression model of AHL-lactonase production in terms of relative activity was built and the optimal cultural conditions for maximum enzyme production were determined as 32.5 °C temperature, pH 7.0, 350 µM of substrate concentration and 33 h of incubation time. The enhanced AHL-lactonase yielded 1.33 fold increases in relative activity and it positively correlated with the amplification of aiiA gene.

Asunto(s)

RESUMEN

With the recent advances in regenerative medicine, nanotechnology has created a niche for itself as a promising avenue in this field. Innumerable studies have been carried out by researchers using virus-based methodologies for the purpose of epigenetic reprogramming. Although this method is ostensibly safe, nonetheless, they are tagged with the risk of viral genome integration into the host genome or insertional mutagenesis. Transient transfection by the use of nanocarriers is the best way to overcome these problems. This review focuses on some of the significant works carried out by researchers utilizing nanocarrier systems that have shown promising results and thus created a landmark in the epigenetic reprogramming.

Asunto(s)

RESUMEN

The aiiA homologous gene known to encode AHL- lactonase enzyme which hydrolyze the N-acylhomoserine lactone (AHL) quorum sensing signaling molecules produced by Gram negative bacteria. In this study, the degradation of AHL molecules was determined by cell-free lysate of endophytic Enterobacter species. The percentage of quorum quenching was confirmed and quantified by HPLC method (p<0.0001). Amplification and sequence BLAST analysis showed the presence of aiiA homologous gene in endophytic Enterobacter asburiae VT65, Enterobacter aerogenes VT66 and Enterobacter ludwigii VT70 strains. Sequence alignment analysis revealed the presence of two zinc binding sites, "HXHXDH" motif as well as tyrosine residue at the position 194. Based on known template available at Swiss-Model, putative tertiary structure of AHL-lactonase was constructed. The result showed that novel endophytic strains of Enterobacter genera encode the novel aiiA homologous gene and its structural importance for future study.

Asunto(s)

RESUMEN

The petroleum ether, chloroform and methanol extracts of Memecylon malabaricum leaves were tested for antimicrobial activity. Only methanol extract has shown activity against bacteria both Gram (+) and Gram (-), and fungi.

Asunto(s)