Pyridine coupled pyrazole analogues as lethal weapon against MRSA: An in-vitro and in-silico approach.

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.

The whole-genome sequence analysis of Enterobacter cloacae strain Ghats1: insights into endophytic lifestyle-associated genomic adaptations.

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.

Isolation and characterization of bioactive compounds with antibacterial, antioxidant and enzyme inhibitory activities from marine-derived rare actinobacteria, Nocardiopsis sp. SCA21.

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.

Potent activity of bioconjugated peptide and selenium nanoparticles against colorectal adenocarcinoma cells.

Nanomaterial based anticancer treatment is promising nowadays because of their small size that can penetrate and interact both inside and outside the cell surface. In this study, a simple protocol was followed for the conjugation of the biologically synthesized selenium nanoparticles (SeNPs) and short chain synthetic peptide. SeNPs was synthesized by using the culture supernatant of Streptomyces griseoruber, actinomycetes isolated from the soil. The short chain peptide Boc-L-F-OMe was synthesized by the conventional solution phase chemistry using a racemization-free fragment condensation strategy. Peptide interaction with different anticancer receptors was preliminarily studied by docking studies. Biosynthesized SeNPs was conjugated with short chain synthetic peptides by means of cysteine conjugation. Characterization of SeNPs with peptide was done by UV-visible spectroscopy and DLS that showed the red shift in the peak and increase in average particle size and zeta potential, respectively. Bioconjugated SeNPs- peptide was tested for its cytotoxicity against the colon cancer cell line HT-29. Bioconjugated SeNPs-peptide showed enhanced cytotoxic activity when compared to the peptide and nanoparticle alone that was tested at 10-50 µg/ml concentration. Further apoptotic studies were done by AO/PI staining and DNA fragmentation assay that confirms the cytotoxicity of the conjugates. Novel peptide-SeNPs conjugates tested in our study has a significant anticancer activity that can be potentially used for targeting the cancer cells.

Association of C677T polymorphism (rs1801133) in MTHFR gene with depression.

Depression is one of the mental disorders with a state of low mood and aversion to activities that exerts a negative effect on a person's thoughts and behavior. Genetic association studies on MTHFR C677T polymorphism and depression have been repeatedly performed over the last two decades, but results are inconsistent. The aim of the present study was to assess the relationship between MTHFR C677T polymorphism and depression by literature review and meta-analysis. Four electronic databases, PubMed, Google Scholar, Science direct and Springer Link were searched for case control articles focusing on MTHFR C677T polymorphism and the risk of depression. A total of 30 studies including 4,802 cases and 17,362 controls were involved in present meta-analysis. When all the eligible studies were pooled into this meta-analysis,  significant association between depression risk and MTHFR C677T polymorphism was found in three genetic models (Additive model: OR T vs C= 1.20, 95 % CI= 1.00-1.34, p=0.0004; homozygote model: OR TT vs.CC=1.37, 95% CI= 1.13-1.65, p=0.0004; dominant model: OR TT+CT vs CC=1.13, 95 % CI= 0.99-1.28, p=0.04), while meta-analysis with other two genetic models did not show association with other two genetic models ( recessive model: OR TT vs CT+CC= 1.36, 95 % CI = 0.91-2.04, p=0.13; co-dominant model: OR CT vs CC=1.00, 95 % CI=0.93-1.08,p=0.84). Present meta-analysis supports that there is a meager significant association between MTHFR C677T polymorphism and depression risk.

Prevalence of COMT Val158Met polymorphism in Eastern UP population.

Catechol-O-methyltransferase (COMT) is an abundant S-adenosylmethionine (SAM-)-dependent methyltransferase that methylates catechol compounds, including catecholamines and catecholestrogens.COMT  gene located at chromosome 22q11.2 contains a functional polymorphism at codon 158(Val158Met), which has been related to psychiatric diseases and different types of cancer. COMT might affect tHcy levels because as a by-product it converts SAM to S-adenosylhomocysteine (SAH), which is reversibly converted to homocysteine. The aim of the present study was to determine the frequency of COMT Val158Met polymorphism in scheduled caste (SC) population of Jaunpur district. Total 100 healthy unrelated subjects belonging to SC, between the age group of 18 to70 years were randomly selected for the present study. 3 ml blood samples were collected from each subject. The inclusion criteria of subjects for present study are that they should be domicile of Uttar Pradesh, and healthy without any individual/ family history of genetic or metabolic disorders. COMT Val158Met polymorphism analysis was done by PCR-RFLP method. The Val/Val genotype was found in 48 subjects, Val/Met in 40 subjects and Met/Met genotype in 12 subjects. Genotype frequencies of Val/Val, Val/Met and Met/Met were 0.48, 0.40 and 0.12 respectively. The allele frequency of Val allele was found to be 0.68 and Met allele frequency was 0.32.

Effect of gamma irradiation on X-ray absorption and photoelectron spectroscopy of Nd-doped phosphate glass.

X-ray absorption near-edge structure (XANES) and X-ray photoelectron spectroscopy (XPS) of Nd-doped phosphate glasses have been studied before and after gamma irradiation. The intensity and the location of the white line peak of the L3-edge XANES of Nd are found to be dependent on the ratio O/Nd in the glass matrix. Gamma irradiation changes the elemental concentration of atoms in the glass matrix, which affects the peak intensity of the white line due to changes in the covalence of the chemical bonds with Nd atoms in the glass (structural changes). Sharpening of the Nd 3d5/2 peak profile in XPS spectra indicates a deficiency of oxygen in the glasses after gamma irradiation, which is supported by energy-dispersive X-ray spectroscopy measurements. The ratio of non-bridging oxygen to total oxygen in the glass after gamma radiation has been found to be correlated to the concentration of defects in the glass samples, which are responsible for its radiation resistance as well as for its coloration.

Molecular identification of aiiA homologous gene from endophytic Enterobacter species and in silico analysis of putative tertiary structure of AHL-lactonase.

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.

Crystal structure of product-bound complex of UDP-N-acetyl-d-mannosamine dehydrogenase from Pyrococcus horikoshii OT3.

UDP-N-acetyl-d-mannosamine dehydrogenase (UDP-d-ManNAcDH) belongs to UDP-glucose/GDP-mannose dehydrogenase family and catalyzes Uridine-diphospho-N-acetyl-d-mannosamine (UDP-d-ManNAc) to Uridine-diphospho-N-acetyl-d-mannosaminuronic acid (UDP-d-ManNAcA) through twofold oxidation of NAD(+). In order to reveal the structural features of the Pyrococcus horikoshii UDP-d-ManNAcADH, we have determined the crystal structure of the product-bound enzyme by X-ray diffraction to resolution of 1.55Å. The protomer folds into three distinct domains; nucleotide binding domain (NBD), substrate binding domain (SBD) and oligomerization domain (OD, involved in the dimerization). The clear electron density of the UDP-d-ManNAcA is observed and the residues binding are identified for the first time. Crystal structures reveal a tight dimeric polymer chains with product-bound in all the structures. The catalytic residues Cys258 and Lys204 are conserved. The Cys258 acts as catalytic nucleophile and Lys204 as acid/base catalyst. The product is directly interacts with residues Arg211, Thr249, Arg244, Gly255, Arg289, Lys319 and Arg398. In addition, the structural parameters responsible for thermostability and oligomerization of the three dimensional structure are analyzed.

Methylenetetrahydrofolate reductase gene A1298C polymorphism and susceptibility to recurrent pregnancy loss: a meta-analysis.

Environmental and genetic factors are thought to be involved in the pathogenesis of recurrent pregnancy loss (RPL)/spontaneous abortions (SA), which include endocrine, anatomical abnormalities within the genital organs, autoimmune diseases and some gene variants. Methylenetetrahydrofolate reductase (MTHFR) is a key enzyme of the folate/methionine metabolic pathway and it is well established fact that folate deficiency causes pregnancy complications like recurrent pregnancy loss, preeclempsia and birth defects affected pregnancies. MTHFR A1298C polymorphism reduces the enzymatic activity and mimics as folate deficiency. To date, many studies have investigated the association between MTHFR A1298C polymorphism and RPL risk; however, the result is still controversial and inconclusive. The aim of the present study was to address the association of MTHFR A1298C polymorphism with RPL risk by meta­analysis. By searching electronic databases, total seventeen studies were identified for present meta­analysis. Crude odds ratios (OR) with 95 % confidence intervals (CIs) was used to assess the strength of association between A1298C polymorphism and RPL. The results indicate that the A1298C polymorphism is not associated with RPL (ORCvs A = 1.13 ,95 % CI= 0.87­1.46, P = 0.36 ; ORACvs AA = 1.22 ,95 % CI= 0.94­ 1.6, P = 0.13; ORCCvsAA =1.35, 95 % CI= 76­2.36, P = 0.30; ORCC+AC vs AA = 1.15, 95 % CI= 88 ­1.49, P = 0.29; ORCCvs AC+AA = 1.29, 95 % CI= 76 ­2.12, P = 0.34). Further prospective studies were needed to confirm the precise relationship between the MTHFR A1298C polymorphism and RPL.

Genetic polymorphisms of methylenetetrahydrofolate reductase (MTHFR) gene and susceptibility to depression in Asian population: a systematic meta-analysis.

Genetic association studies on MTHFR C677 T polymorphism and depression have been repeatedly performed over the last two decades and results are generally inconsistent. The aim of the present study was to assess the risk of MTHFR C677T polymorphism for depression in Asian population. The author performed a meta-analysis and pooled data from individual case-control studies that examined the association between C677T polymorphism and depression (meta-analysis: 13 studies, 1,120 cases and 1,688 controls).The pooled Odd Ratios (OR) were estimated by both fixed effects and random effects models. Overall, there was an association between MTHFR C677T polymorphism and increased risk of depression under five genetic models (OR T vs. C=1.44, 95% CI= 1.56-1.78, P=0.001; OR TT vs. CC= 1.78, 95% CI 1.17­ 2.69, P=0.006; OR CT vs CC=1.102, 95% CI=0.91-1.32,P=0.31; OR TT vs. CT+CC=1.73, 95% CI= 0.87-3.41, P=0.11; OR TT+CT vs. CC=1.26, 95% CI=0.96-1.64, P=0.08). Sensitivity analysis suggested exclusion of any single study did not alter the overall pooled Ors. In conclusion results of present meta-analysis supports that there is a significant association between MTHFR C677T polymorphism and depression risk, and MTHFR 677T allele contributes to increased risk of depression in Asian individuals.

Genetic diversity studies in pea (Pisum sativum L.) using simple sequence repeat markers.

The genetic diversity among 28 pea (Pisum sativum L.) genotypes was analyzed using 32 simple sequence repeat markers. A total of 44 polymorphic bands, with an average of 2.1 bands per primer, were obtained. The polymorphism information content ranged from 0.657 to 0.309 with an average of 0.493. The variation in genetic diversity among these cultivars ranged from 0.11 to 0.73. Cluster analysis based on Jaccard's similarity coefficient using the unweighted pair-group method with arithmetic mean (UPGMA) revealed 2 distinct clusters, I and II, comprising 6 and 22 genotypes, respectively. Cluster II was further differentiated into 2 subclusters, IIA and IIB, with 12 and 10 genotypes, respectively. Principal component (PC) analysis revealed results similar to those of UPGMA. The first, second, and third PCs contributed 21.6, 16.1, and 14.0% of the variation, respectively; cumulative variation of the first 3 PCs was 51.7%.

[Purification and chemical characterization of antimicrobial compounds from a new soil isolate Streptomyces rimosus MTCC 10792].

A new isolate of Streptomyces sp. from soil of state Chhattisgarh (India) having broad spectrum antibacterial and antifungal activity was obtained. The active strain was identified as Streptomyces rimosus subsp. rimosus with accession number MTCC 10792 based on physiological, biochemical characteristics and 16S rRNA sequence homology studies. Antimicrobial compound produced by S. rimosus was tested against the drug resistance pathogens by the Bauer and Kirby method. The crude active metabolite was extracted using solvent n-butanol and purified by silica column chromatography and HPLC method. The physicochemical characteristics of the one purified compound viz. color, melting point, solubility, elemental analysis; ESIMS, IR,UV, 1HNMR, 13CNMR and chemical reactions have been investigated. Purified antimicrobial compound produced by S. rimosus MTCC 10792 at concentration 25 µg/ml showed antitubercular activity against Mycobacterium tuberculosis H37Rv, Mycobacterium tuberculosis H37Ra as well as broad activity against all tested bacterial and fungal pathogens.

Oxidized Low-density Lipoproteins and Lipopolysaccharides Augment Carotid Artery Plaque Vulnerability in Hypercholesterolemic Microswine.

Atherosclerosis is a chronic inflammatory disease and hypercholesterolemia is a risk factor. This study aims to compare the potency of lipopolysaccharide (LPS) and oxidized low-density lipoproteins (oxLDL) to induce plaque formation and increase plaque vulnerability in the carotid artery of hypercholesterolemic Yucatan microswine. Atherosclerotic lesions at the common carotid artery junction and ascending pharyngeal artery were induced in hypercholesterolemic Yucatan microswine at 5-6 months of age with balloon angioplasty. LPS or oxLDL were administered intraluminally at the site of injury after occluding the arterial flow temporarily. Pre-intervention ultrasound (US), angiography, and optical coherence tomography (OCT) were done at baseline and just before euthanasia to assess post-op parameters. The images from the US, OCT, and angiography in the LPS and the oxLDL-treated group showed increased plaque formation with features suggestive of unstable plaque, including necrotic core, thin fibrous caps, and a signal poor region more with oxLDL compared to LPS. Histomorphology of the carotid artery tissue near the injury corroborated the presence of severe lesions in both LPS and oxLDL-treated pigs but more in the oxLDL group. Vascular smooth muscle and endothelial cells treated with LPS and oxLDL showed increased folds changes in mRNA transcripts of the biomarkers of inflammation and plaque vulnerability compared to untreated cells. Collectively, the results suggest that angioplasty-mediated intimal injury of the carotid arteries in atherosclerotic swine with local administration of LPS or ox-LDL induces vulnerable plaques compared to angioplasty alone and oxLDL is relatively more potent than LPS in inducing vulnerable plaque.

Genotype prevalence and allele frequencies of 5,10-methylenetetrahydrofolate reductase (MTHFR) C677T mutation in two caste groups of India.

The aim of the present study was to investigate the distribution of 5,10-methylenetetrahydrofolate reductase (MTHFR) polymorphism in two caste group populations of eastern Uttar Pradesh. This mutation has been suggested to be positively associated with the risk of several congenital and multifactorial disorders. Frequency of mutant T allele differs in various ethnic and geographical populations of the world. MTHFR C677T mutation analysis was carried out by PCR-RFLP (Polymerase Chain Reaction-Restriction Fragment Length Polymorphism) method and the samples studied were randomly selected from the healthy individuals belonging to two caste populations. In Brahmin samples, genotype frequencies of CC, CT and TT were 0.727, 0.25 and 0.023 respectively whereas in Rajput samples, CC genotype was observed in 88 samples, CT genotype in 25 and TT genotype was found in 2 samples. Frequency of mutant T allele was found to be 0.147 in Brahmin and 0.126 in Rajput populations. The percentage of CT genotype and C allele were high in both the populations.

Design, synthesis of pyridine coupled pyrimidinone/pyrimidinthione as anti-MRSA agent: Validation by molecular docking and dynamics simulation.

Methicillin Resistant Staphylococcus aureus (MRSA) is a major cause of severe hospital and infections acquired by the population and related morbidity and mortality. In this unique situation, there is a need of dynamic strong drug candidates to control MRSA diseases. Thus, the present work focuses on the synthesis and characterization of pyrimidinones and pyrimidinthiones coupled pyridine derivatives as anti-MRSA agent. The synthesized compounds were characterized by different spectroscopic techniques and evaluated against MRSA strain. Among them, 4e and 4 g possessed better antibacterial activity with MIC values of 10 µg and 8 µg respectively. The key determinant of the wide range beta-lactam resistance in MRSA strains is the Penicillin-Binding Protein 2a (PBP2a) but the gene encodes PBP2a which has a low affinity towards ß-lactam antibiotics. Because of this, the present investigation focused on the mechanism of PBP2a protein binding studies by in-silico studies. The synthesized compounds showed very good interactions with PBP2A compared with standard drug Vancomycin, among them compound 4 g showed better interaction with the binding score of -9.8 kcal/mol. Antibacterial activity was validated with molecular docking and molecular dynamic simulation. Simulation results revealed that protein-ligand interactions of 4 g compound stably sustained up to 20,000ps.Communicated by Ramaswamy H. Sarma.

4-acetamido-3-nitrobenzoic acid - structural, quantum chemical studies, ADMET and molecular docking studies of SARS-CoV2.

In December 2019, a new type of SARS corona virus emerged from China and caused a globally pandemic corona virus disease (COVID-19). This highly infectious virus has been named as SARS-CoV-2 by the International Committee of the Taxonomy of Viruses. It has severely affected a large population and economy worldwide. Globally various scientific communities have been involved in studying this newly emerged virus and is lifecycle. Multiple diverse studies are in progress to design novel therapeutic agents, in which understanding of interactions between the target and drug ligand is a significant key for this challenge. Structures of proteins involved in the life cycle of the virus have been revealed in RCSB PDB by researchers. In this study, we employed molecular docking study of 4-Acetamido-3-nitrobenzoic acid (ANBA) with corona virus proteins (spike protein, spike binding domain with ACE2 receptor and Main protease, RNA-dependent RNA polymerase). Single crystal X-ray analysis and density functional theory calculations were carried out for ANBA to explore the structural and chemical-reactive parameters. Intermolecular interactions which are involved in the ligand-protein binding process are validated by Hirshfeld surface analysis. To study the behaviour of ANBA in a living organism and to calculate the physicochemical parameters, ADMET analysis was done using SwissADME and Osiris data warrior tools. Further, Toxicity of ANBA was predicted using pkCSM online software. Based on the molecular docking analysis, we introduce here a potent drug molecule that binds to the COVID-19 proteins.Communicated by Ramaswamy H. Sarma.

Evaluation of methylenetetrahydrofolate reductase gene variant (C677T) as risk factor for bipolar disorder.

Methylenetetrahydrofolate reductase (MTHFR) is a key enzyme in the metabolism of folate, whose role in bipolar disorder is controversial. The aim of the present study was to assess the risk of MTHFR C677T polymorphism for bipolar disorder. The author performed a meta-analysis and pooled data from individual case-control studies that examined the association between C677T polymorphism and bipolar disorder (meta-analysis: 8 studies, 1457 cases and 2169 controls).The pooled Odd Ratios (OR) were estimated by both fixed effects and random effects models. The meta-analysis with fixed effects showed that there was 71% heterogeneity between the eight studies. The fixed effect pooled OR was 1.07 (95% CI; 0.98 to 1.17) and Cochran Q was 24.13 (df = 7; p=0.0011). The study is significant and shows meager association. The random effect pooled OR was 1.07(95% CI; 0.87 to 1.32) and Cochran Q was 24.13 (df = 7; p=0.0011). The random effect pooled OR was also significant and shows meager association between MTHFR C677T genotype and bipolar disorder.

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., Streptomyces misionensis MI22, Streptomyces roietensis MI24, Streptomyces glaucescens MI29, and Streptomyces sp. MI04 inhabiting Madhuca insignis by its characteristic morphological features and 16S rRNA gene sequence analysis. S. misionensis MI22 exhibits a broad spectrum of anti-microbial activity against methicillin-resistant Staphylococcus aureus (25.00 ± 1.00 mm) followed by Bacillus subtilis (23.66 ± 0.57 mm), Escherichia coli (22.00 ± 0.00 mm), and Candida albicans (18.00 ± 0.00 mm). Minimum inhibitory concentrations of the ethyl acetate fraction of S. misionensis MI22 against test pathogens were ranged from 25 to 100 µg/mL. Indeed, strain MI22 also exhibited significant anti-proliferative activity against HeLa cell line with IC50 value 98 µg/mL and showed no cytotoxicity effect to the normal human embryonic kidney cell line in the MTT assay. The anti-microbial metabolites from strain MI22 were detected at Rf 0.55 as depicted by the inhibition zone on the intensive band in TLC-bioautography assay. CONCLUSION: The study indicates that, anti-microbial metabolites of these endophytic Streptomyces species, especially S. misionensis MI22 as a prolific source to discover novel bioactive metabolites to combat multidrug-resistant pathogens.

Effect of peptide-conjugated nanoparticles on cell lines.

Metal nanoparticles are widely used for the delivery and targeting of pharmaceutical, therapeutic and diagnostic agents in cancer therapy in recent years. The multifunctional nanoparticles constructed currently are supposed to show superior effects on cancer cells. This study was conducted to observe the difference between the effect of a biologically important peptide, silver (AgNPs) and gold (AuNPs) nanoparticles and their conjugates on two different cancer cells. Peptide (Boc-L-DP-L-OMe) was acquired from different sources and subjected to conjugation with biosynthesized gold and silver nanoparticles under standard conditions. These conjugates were tested against the colon cancer (HT-29) and breast cancer (MDA MB-231) cell lines. The results clearly depicted the improved activity of nanoparticles in the form of conjugates. Fluorescent dye microscopy and DNA fragmentation assay substantiate the fact that the conjugated nanoparticles cause higher level of disintegration of DNA in cells that consecutively damages and causes apoptosis due to lethality.