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1.
Lung India ; 41(2): 93-97, 2024 Mar 01.
Article in English | MEDLINE | ID: mdl-38700401

ABSTRACT

BACKGROUND: Endobronchial ultrasound-guided transbronchial fine-needle aspiration (EBUS-TBNA) has replaced mediastinoscopy as the preferred investigation for evaluating mediastinum in staging lung cancer. There is little evidence of mediastinal staging by EBUS-TBNA from India. OBJECTIVES: To study endobronchial ultrasound's diagnostic accuracy in staging lung cancer. METHODOLOGY: We retrospectively analysed patients operated on for lung cancer where EBUS was performed preoperatively for mediastinal staging. We compared the histological findings obtained from different mediastinal lymph nodes (LNs) by EBUS-TBNA with the pathology of the same LNs obtained after surgical dissection as the reference standard. RESULTS: Seventy-six patients underwent curative surgery for lung cancer. The diagnostic accuracy, sensitivity, specificity, positive predictive value and negative predictive value of EBUS-TBNA in predicting mediastinal metastasis were 93.9%, 40%, 99%, 80% and 94.6%, respectively. Of the 115 LNs sampled, EBUS-TBNA was false negative in six nodes, resulting in an up-staging of six patients. CONCLUSIONS: EBUS-TBNA has a high diagnostic accuracy for lung cancer staging.

2.
J Phys Chem Lett ; 15(17): 4711-4720, 2024 May 02.
Article in English | MEDLINE | ID: mdl-38657124

ABSTRACT

We present a comprehensive scale-bridging characterization approach for supported catalytically active liquid metal solutions (SCALMS) which combines lab-based X-ray microscopy, nano X-ray computed tomography (nano-CT), and correlative analytical transmission electron microscopy. SCALMS catalysts consist of low-melting alloy particles and have demonstrated high catalytic activity, selectivity, and long-term stability in propane dehydrogenation (PDH). We established an identical-location nano-CT workflow which allows us to reveal site-specific changes of Ga-Pt SCALMS before and after PDH. These observations are complemented by analytical transmission electron microscopy investigations providing information on the structure, chemical composition, and phase distribution of individual SCALMS particles. Key findings of this combined microscopic approach include (i) structural evolution of the SCALMS particles' GaOx shell, (ii) Pt segregation toward the oxide shell leading to the formation of Ga-Pt intermetallic phases, and (iii) cracking of the oxide shell accompanied by the release of liquid Ga-Pt toward the porous support.

3.
J Biomol Struct Dyn ; 39(17): 6500-6514, 2021 10.
Article in English | MEDLINE | ID: mdl-32794423

ABSTRACT

Novel macrocyclic Schiff base complexes [[ML]X; where M = Cu(II), Co(II), Ni(II), Zn(II), Mn(II) and VO(IV); L = macrocyclic ligand; X = Cl2 and SO42-] have been synthesized and characterized by microanalytical, 1H, 13C NMR, IR, Mass, UV-Vis, EPR spectral studies, as well as conductivity data. All the complexes exhibit square-planar geometry except vanadium complex. Magnetic susceptibility measurements and high conductance data reveal the monomeric and electrolytic nature of the complexes. Electronic absorption, cyclic voltammetry, viscosity measurements have been carried out on the interaction of the complexes with DNA. The results suggest that the complexes bind to DNA by intercalation via the aromatic ring of the macrocycle into the base pairs of DNA. Using gel electrophoresis experiment in the presence and absence of oxidant (H2O2) the nuclease cleavage activity of the complexes has been performed on plasmid DNA. The results demonstrate that most of the complexes have promising superoxide dismutase (SOD)-mimetic activity. The in vitro cytotoxicity of ligand and its complexes has also been evaluated against human breast and colon carcinoma cells. Binding interactions and energies of ligand and its metal complexes [ML]2+ (M = VO(IV), Mn(II), Co(II), Ni(II), Cu(II), Zn(II)) against the receptors EGFR and HER2 are performed using the Auto dock module. Consequently, it is found that the ligand is strong inhibitor for EGFR and HER2 while [VOL]SO4 is good inhibitor for EGFR and [ZnL]Cl2 is moderate inhibitor for HER2. The antimicrobial activity of the ligand and its complexes against bacteria Salmonella typhi, Staphylococcus aureus, Escherichia coli and Bacillus subtilis and fungi Aspergillus niger, Aspergillus flavus, Candida Albicans and Rhizoctonia bataicola. The complexes have higher activities than the macrocyclic free Schiff base. Communicated by Ramaswamy H. Sarma.


Subject(s)
Anti-Infective Agents , Coordination Complexes , Anti-Infective Agents/pharmacology , Coordination Complexes/pharmacology , Copper , DNA , Humans , Hydrogen Peroxide , Ligands , Microbial Sensitivity Tests , Molecular Docking Simulation , Pentanes , Schiff Bases , Superoxide Dismutase , Zinc
4.
Cancer Med ; 5(8): 2000-11, 2016 08.
Article in English | MEDLINE | ID: mdl-27184932

ABSTRACT

Integrin αvß6 is involved in the transition from ductal carcinoma in situ (DCIS) to invasive ductal carcinoma (IDC) of the breast. In addition, integrin ß6 (ITGB6) is of prognostic value in invasive breast cancers, particularly in HER2+ subtype. However, pathways mediating the activity of integrin αvß6 in clinical progression of invasive breast cancers need further elucidation. We have examined human breast cancer specimens (N = 460) for the expression of integrin ß6 (ITGB6) mRNA by qPCR. In addition, we have examined a subset (N = 147) for the expression of αvß6 integrin by immunohistochemistry (IHC). The expression levels of members of Rho-Rac pathway including downstream genes (ACTR2, ACTR3) and effector proteinases (MMP9, MMP15) were estimated by qPCR in the HER2+ subset (N = 59). There is a significant increase in the mean expression of ITGB6 in HER2+ tumors compared to HR+HER2- and triple negative (TNBC) subtypes (P = 0.00). HER2+ tumors with the highest levels (top quartile) of ITGB6 have significantly elevated levels of all the genes of the Rho-Rac pathway (P-values from 0.01 to 0.0001). Patients in this group have a significantly shorter disease-free survival compared to the group with lower ITGB6 levels (HR = 2.9 (0.9-8.9), P = 0.05). The mean level of ITGB6 expression is increased further in lymph node-positive tumors. The increased regional and distant metastasis observed in HER2+ tumors with high levels of ITGB6 might be mediated by the canonical Rho-Rac pathway through increased expression of MMP9 and MMP15.


Subject(s)
Breast Neoplasms/genetics , Breast Neoplasms/metabolism , Gene Expression Regulation, Neoplastic , Integrin beta Chains/genetics , Receptor, ErbB-2/metabolism , Signal Transduction , rac GTP-Binding Proteins/metabolism , Adult , Aged , Breast Neoplasms/mortality , Breast Neoplasms/pathology , Female , Gene Amplification , Gene Expression , Humans , Immunohistochemistry , In Situ Hybridization, Fluorescence , Middle Aged , Neoplasm Metastasis , Prognosis , Proportional Hazards Models , ROC Curve , Receptor, ErbB-2/genetics
5.
J Photochem Photobiol B ; 154: 67-76, 2016 Jan.
Article in English | MEDLINE | ID: mdl-26690017

ABSTRACT

New series of bio-essential metal based complexes linked by Schiff base ligand (L) and 2,2'-bipyridine (bpy) have been synthesized and characterized by diverse spectral techniques such as elemental analysis, magnetic susceptibility, molar conductivity measurements, FT-IR, UV-Vis., (1)H NMR, (13)C NMR, EPR and Mass. The spectral data suggest that the metal complexes espouse octahedral geometry around the metal ions. Interactions of the complexes with CT DNA have been explored by electronic absorption, ethidium bromide displacement assay, viscosity measurements, cyclic voltammetry and differential pulse voltammetry in order to evaluate the possible DNA-binding mode and to calculate the corresponding DNA-binding constants. The DNA interaction studies propose that the intercalative mode of interaction and the complexes exhibit oxidative cleavage of pUC19 DNA in the presence of hydrogen peroxide as activator. The synthesized Schiff base ligand and its metal complexes have been screened for anti-microbial activity by micro dilution method against two Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis), two Gram-negative bacteria (Escherichia coli and Salmonella typhi) and three fungi strains (Fusarium solani, Aspergillus niger and Candida albicans) revealing that the complexes are good anti-pathogenic agents than the ligand. Moreover, molecular docking analysis has been performed to confirm the nature of binding of the complexes with DNA.


Subject(s)
Coordination Complexes/chemical synthesis , 2,2'-Dipyridyl/chemistry , Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Binding Sites , Coordination Complexes/metabolism , Coordination Complexes/pharmacology , DNA/chemistry , DNA/metabolism , DNA Cleavage/drug effects , Electrochemical Techniques , Fungi/drug effects , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Ligands , Molecular Docking Simulation , Nucleic Acid Conformation , Plasmids/chemistry , Plasmids/metabolism , Schiff Bases/chemistry , Viscosity
6.
Mater Sci Eng C Mater Biol Appl ; 53: 239-51, 2015 Aug.
Article in English | MEDLINE | ID: mdl-26042712

ABSTRACT

The coordination of therapeutically interesting designed complexes of stoichiometry [ML(Met)Cl2] [where M=Cu(II), Co(II), Ni(II), Mn(II) and Zn(II), L=benzylidene-4-aminoantipyrine and Met=methionine] has been ascertained on the basis of physicochemical techniques. Their interaction with CT DNA reveals that they are good intercalators. The anticancer mechanism of our complexes is documented from their enhanced DNA splitting personalities under physiological conditions. To reveal the chemotherapeutic action of these complexes, we explored the inflammatory response, analgesic and antioxidant activities. Moreover, all the complexes show good antimicrobial activity against few bacterial and fungal strains. Our study has identified the mechanism of action of these complexes on inhibiting tumor cells and suggested that they have great potential as novel anticancer agents.


Subject(s)
Anti-Inflammatory Agents/chemistry , Antineoplastic Agents/chemistry , DNA/chemistry , Intercalating Agents/chemistry , Metals, Heavy/chemistry , Animals , Anti-Inflammatory Agents/pharmacology , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Cell Survival/drug effects , Edema , Humans , Intercalating Agents/pharmacology , Mice , Nuclear Magnetic Resonance, Biomolecular , Rats , Schiff Bases
7.
J Photochem Photobiol B ; 149: 93-102, 2015 Aug.
Article in English | MEDLINE | ID: mdl-26057019

ABSTRACT

Organic and inorganic entities [Cu(II), Co(II), Ni(II) and Zn(II)] have been bridged by N2O2 type heterocyclic imine (CN) ligand for the synthesis of novel organic-inorganic bridged complexes of the type [M(H2L)]. The synthesized complexes were characterized by spectral techniques such as FT-IR, UV-visible, (1)H NMR, (13)C NMR, EPR, ESI-Mass, elemental analysis, magnetic susceptibility and molar conductivity measurements. The metal complexes adopt square planar geometrical arrangement around the metal ions. DNA binding ability of these complexes has been explored by different techniques viz. electronic absorption, fluorescence, cyclic voltammetry, differential pulse voltammetry and viscosity measurements. These studies prove that CT DNA interaction of the complexes follows intercalation mode. The oxidative cleavage of the complexes with pUC19 DNA has been investigated by gel electrophoresis. Molecular docking calculations have been performed to understand the nature of binding of the complexes with DNA. Moreover, the anti-pathogenic actions of the complexes were tested in vitro against few bacteria and fungi by disk diffusion method. The data reveal that the complexes have higher anti-pathogenic activity than the ligand.


Subject(s)
Coordination Complexes/chemical synthesis , Coordination Complexes/pharmacology , Heterocyclic Compounds/chemistry , Imines/chemistry , Molecular Docking Simulation , Oxygen/chemistry , Animals , Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/chemistry , Anti-Infective Agents/metabolism , Anti-Infective Agents/pharmacology , Cattle , Chemistry Techniques, Synthetic , Coordination Complexes/chemistry , Coordination Complexes/metabolism , DNA/chemistry , DNA/metabolism , DNA Cleavage/drug effects , Ligands , Nucleic Acid Conformation , Viscosity
8.
J Photochem Photobiol B ; 148: 160-167, 2015 Jul.
Article in English | MEDLINE | ID: mdl-25931401

ABSTRACT

A new series of metal(II) complexes using a symmetric Schiff base ligand, obtained by the condensation reaction of 4-formyl-N,N-dimethylaniline with benzene-1,2-diamine were synthesized and characterized. The various physico-chemical data indicate that the complexes have octahedral geometry. The intrinsic binding constant of the complexes with DNA is explored. The UV-Vis., circular dichorism, fluorescence emission spectral data and the viscosity measurements indicate that the complexes bind to calf thymus DNA (CT DNA) by intercalative mode. The intrinsic binding constants of Cu(II), Ni(II), Co(II) and Zn(II) complexes are found to be 7.1×10(4), 5.2×10(4), 1.8×10(5) and 6.3×10(4) M(-1), respectively. The cleavage studies of these complexes are investigated by gel electrophoresis method in the presence of peroxide. The complexes exhibit enhanced biological activities compared to the free ligand.


Subject(s)
Anti-Infective Agents/chemistry , Chelating Agents/chemistry , Coordination Complexes/chemistry , DNA/chemistry , Schiff Bases/chemistry , Aniline Compounds/chemistry , Animals , Anti-Infective Agents/metabolism , Anti-Infective Agents/pharmacology , Cattle , Coordination Complexes/chemical synthesis , Coordination Complexes/pharmacology , DNA/metabolism , Fungi/drug effects , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Intercalating Agents/chemical synthesis , Intercalating Agents/chemistry , Intercalating Agents/pharmacology , Ligands , Metals/chemistry , Microbial Sensitivity Tests
9.
J Cancer ; 5(2): 156-65, 2014.
Article in English | MEDLINE | ID: mdl-24563670

ABSTRACT

BACKGROUND: The 2010 guidelines by ASCO-CAP have mandated that breast cancer specimens with ≥1% positively staining cells by immunohistochemistry should be considered Estrogen Receptor (ER) positive. This has led to a subclass of low-ER positive (1-10%) breast cancers. We have examined the biology and clinical behavior of these low ER staining tumors. METHODS: We have developed a probabilistic score of the "ER-positivity" by quantitative estimation of ER related gene transcripts from FFPE specimens. Immunohistochemistry for ER was done on 240 surgically excised tumors of primary breast cancer. Relative transcript abundance of 3 house-keeping genes and 6 ER related genes were determined by q-RT PCR. A logistic regression model using 3 ER associated genes provided the best probability function, and a cut-off value was derived by ROC analysis. 144 high ER (>10%), 75 ER negative and 21 low-ER (1-10%) tumors were evaluated using the probability score and the disease specific survival was compared. RESULTS: Half of the low-ER positive tumors were assigned to the ER negative group based on the probability score; in contrast 95% of ER negative and 92% of the high ER positive tumors were assigned to the appropriate ER group (p<0.0001). The survival of the low-ER group was intermediate between that of the high ER positive and ER negative groups (p<0.05). CONCLUSION: Our results suggest that the newly lowered ASCO-CAP criteria for ER positivity, leads to the false categorization of biologically ER negative tumors as ER positive ones. This may have particular relevance to India, where we have a much higher proportion of ER negative tumors in general.

10.
Spectrochim Acta A Mol Biomol Spectrosc ; 125: 404-13, 2014 May 05.
Article in English | MEDLINE | ID: mdl-24566120

ABSTRACT

A series of novel Co(II), Cu(II), Ni(II) and Zn(II) complexes were synthesized from Schiff base(s), obtained by the condensation of 4-aminoantipyrine with furfural and amino acid (glycine(L1)/alanine(L2)/valine(L3)) and respective metal(II) chloride. Their structural features and other properties were explored from the analytical and spectral methods. The binding behaviors of the complexes to calf thymus DNA were investigated by absorption spectra, viscosity measurements and cyclic voltammetry. The intrinsic binding constants for the above synthesized complexes are found to be in the order of 10(2) to 10(5) indicating that most of the synthesized complexes are good intercalators. The binding constant values (Kb) clearly indicate that valine Schiff-base complexes have more intercalating ability than alanine and glycine Schiff-base complexes. The results indicate that the complexes bind to DNA through intercalation and act as efficient cleaving agents. The in vitro antibacterial and antifungal assay indicates that these complexes are good antimicrobial agents against various pathogens. The IC50 values of [Ni(L1)2] and [Zn(L1)2] complexes imply that these complexes have preferable ability to scavenge hydroxyl radical.


Subject(s)
Amino Acids/metabolism , Ampyrone/metabolism , DNA/metabolism , Schiff Bases/metabolism , Amino Acids/chemistry , Ampyrone/chemistry , Animals , Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Antioxidants/pharmacology , Bacteria/drug effects , Cattle , Coordination Complexes/chemical synthesis , Coordination Complexes/chemistry , Dimethyl Sulfoxide/chemistry , Electric Conductivity , Electrochemical Techniques , Electron Spin Resonance Spectroscopy , Electrons , Fungi/drug effects , Ligands , Magnetic Resonance Spectroscopy , Mass Spectrometry , Microbial Sensitivity Tests , Schiff Bases/chemical synthesis , Schiff Bases/chemistry , Solutions , Spectrophotometry, Infrared , Viscosity
11.
Article in English | MEDLINE | ID: mdl-23981416

ABSTRACT

A novel bidentate Schiff base ligand has been synthesized using 2,4-dihydroxybenzophenone and aniline. Its mixed ligand complexes of MAB type [M=Mn(II), Co(II), Ni(II), Cu(II) and Zn(II); HA=Schiff base and B=2-aminophenol/2-aminobenzoic acid] have been synthesized and characterized on the basis of spectral data UV-Vis, IR, (1)H NMR, FAB-Mass, EPR, SEM and magnetic studies. All the complexes were soluble in DMF and DMSO. Elemental analysis and molar conductance values indicate that the complexes are non-electrolytes. HA binds with M(II) ions through azomethine and deprotonated phenolic group and B binds through the primary amine group and deprotonated phenolic/carboxylic groups. Using FAB-Mass the cleavage pattern of the ligand (HA) has been established. All the complexes adopt octahedral geometry around the metal ions. It has been confirmed with the help of UV-Vis, IR, (1)H NMR and FAB-Mass spectral data. DNA binding activities of the complexes 1d and 2d are studied by UV-Vis spectroscopy and cleavage studies of Schiff base ligand and its complexes 1d and 2d have been by agarose gel electrophoresis method. In vitro biological activities of the free ligand (HA) and their metal complexes (1a-1e and 2a-2e) were screened against few bacteria, Escherichia coli, Staphylococcus saphyphiticus, Staphylococcus aureus, Pseudomonas aeruginosa and fungi Aspergillus niger, Enterobacter species, Candida albicans by well diffusion technique.


Subject(s)
Aminophenols/chemistry , Anti-Infective Agents/pharmacology , Deoxyribonucleases/metabolism , Schiff Bases/chemistry , ortho-Aminobenzoates/chemistry , Anti-Infective Agents/chemistry , DNA/metabolism , Electron Spin Resonance Spectroscopy , Mass Spectrometry , Microscopy, Electron, Scanning , Thermogravimetry
12.
Afr J Psychiatry (Johannesbg) ; 16(5): 356-63, 2013 Sep.
Article in English | MEDLINE | ID: mdl-24051669

ABSTRACT

OBJECTIVE: National and international child and adolescent mental healthcare policy and action advocate that the health and well being of children should be increasingly given greater attention. The purpose of this study was to describe the demographic, socio economic and clinical profile of the users at the child and adolescent mental health clinic of the Rahima Moosa Mother and Child Hospital (RMMCH). METHOD: A descriptive, retrospective clinical audit from users' clinical files was performed over a one-year period from January to December 2007. Descriptive statistical analyses of demographic and socio-economic variables were made and these variables were compared with the presenting clinical problems. Odds ratios were calculated for variables that showed a statistically significant association (p-value less than 0.05). RESULTS: A total of 303 users attended this clinic. Statistical comparisons between demographic data and disorders revealed that being male increased the likelihood of presenting with AHDH and disruptive behaviour disorders; being female increased the likelihood of being sexually abused. Race showed a significant association with parent-child relationship difficulties. Regarding socio-economic variables, the identity of the caregiver of the child influenced the risk of disruptive behaviour disorders, sexual abuse, neglect and academic problems. Where the child was placed was a risk factor for disruptive behaviour disorders, sexual abuse, neglect and academic problems. Whether the mother of a user was alive or deceased, was found to be related to ADHD and disruptive behaviour and whether the father of a user was alive or deceased, was found to be related to sexual abuse and academic problems. The education level of the caregiver showed a significant association with sexual abuse, neglect and academic problems; the marital status of the parent (widowed mother) showed a significant association with bereavement. Household income was associated with sexual abuse, neglect and academic problems. CONCLUSION: This study demonstrated the impact that socio-economic circumstances have on the prevalence of childhood disorders; hence the urgent need for government and social welfare departments to improve the socio-economic status of communities. There is a need to improve psychiatric services for the population served by this hospital, including more clinics in its catchment area, as well as child psychiatry training posts and extended social work services.


Subject(s)
Child Abuse , Child Welfare , Mental Disorders , Adolescent , Child , Child Abuse/prevention & control , Child Abuse/psychology , Child Abuse/statistics & numerical data , Child Behavior , Demography , Female , Humans , Male , Mental Disorders/epidemiology , Mental Disorders/psychology , Mental Health Services/statistics & numerical data , Prevalence , Retrospective Studies , Socioeconomic Factors , South Africa/epidemiology , Surveys and Questionnaires , Urban Health
13.
J Chromatogr Sci ; 51(5): 471-6, 2013.
Article in English | MEDLINE | ID: mdl-23097581

ABSTRACT

A novel stability-indicating reversed-phase high-performance liquid chromatographic (HPLC) method has been developed for the quantitative determination of darunavir ethanolate, an HIV-1 protease inhibitor. The chromatographic separation was achieved using an X-Bridge C18 (150 × 4.6 mm × 3.5 µm) HPLC column in isocratic mode employing 0.01M ammonium formate (pH.3.0) buffer and acetonitrile in the ratio of 55:45 (v/v) with a flow rate of 1.0 mL/min. The detector wavelength was monitored at 265 nm and the column temperature was maintained at 30°C. Darunavir ethanolate was exposed to thermal, photolytic, acid, base and oxidative stress conditions. Considerable degradation of the drug substance was found to occur under acid, base and oxidative stress conditions. The peak homogeneity data of darunavir ethanolate obtained by photodiode array detection demonstrated the specificity of the method in the presence of degradants. The degradation products were well resolved from primary peak of darunavir, indicating that the method is specific and stability-indicating. The HPLC method was validated as per International Conference on Harmonization guidelines with respect to specificity, precision, linearity, accuracy and robustness. Regression analysis showed a correlation coefficient value greater than 0.999. The accuracy of the method was established based on the recovery obtained for darunavir ethanolate.


Subject(s)
Chromatography, High Pressure Liquid/methods , HIV Protease Inhibitors/chemistry , Sulfonamides/chemistry , Chromatography, Reverse-Phase/methods , Darunavir , Drug Stability
14.
Mater Sci Eng C Mater Biol Appl ; 33(2): 884-91, 2013 Mar 01.
Article in English | MEDLINE | ID: mdl-25427502

ABSTRACT

This research work reports the in vitro antitumor personality of few novel peptide nanocomplexes synthesized via a phase-assisted, modified Brust-Schiffrin methodology. Here, a series of metallo(copper, cobalt, nickel and zinc) nanocomplexes engineered with a pre-prepared peptide [N,N'-(1,2-ethylene)-bis-hippuricamide] have been synthesized for damaging the Dalton's lymphoma ascites tumor model. All the peptide nanocomplexes are spectrally, thermally and morphologically examined. The peptide bound zinc and cobalt nanocomplexes deliver excellent antitumor behavior against both the animal and human cancer cell lines, which has been pre-documented by their efficient DNA damaging skills under physiological conditions. Additionally, all the nanocomplexes are evaluated for the inhibition of microbial augmentation against few fungal and bacterial strains. The above results demonstrate that, a consecutive development of these kinds of peptide nanocomplexes may exemplify their uniqueness in biomedical applications as useful molecular-level devices.


Subject(s)
Antineoplastic Agents/pharmacology , Lymphoma/metabolism , Nanocomposites/chemistry , Peptides/pharmacology , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Antineoplastic Agents/chemistry , Ascites , Bacteria/drug effects , Biotechnology , Cell Line, Tumor , DNA Damage/drug effects , Fungi/drug effects , HeLa Cells , Humans , Metals, Heavy/chemistry , Metals, Heavy/pharmacology , Neoplasms, Experimental/metabolism , Peptides/chemistry
15.
Article in English | MEDLINE | ID: mdl-22947646

ABSTRACT

Present study reports a green chemistry approach for the biological synthesis of silver nanoparticles using the aqueous leaf extract of Pithecellobium dulce, which acts as a reducing and capping agent. It is observed that use of P. dulce leaf extract makes a fast, environmentally benign and convenient method for the synthesis of silver nanoparticles and can reduce silver ions into silver nanoparticles. Silver nanoparticles so prepared have been characterized by UV-Vis, FT-IR, X-ray diffraction, atomic force microscopy and scanning electron microscope studies. Furthermore, these nanoparticles show effective larvicidal activity against Culex quinquefasciatus (LC(50)=21.56 mg/L and r(2)=0.995) due to high surface to volume ratio.


Subject(s)
Extracellular Space/chemistry , Fabaceae/chemistry , Green Chemistry Technology/methods , Insecticides/chemical synthesis , Insecticides/pharmacology , Metal Nanoparticles/chemistry , Silver/pharmacology , Animals , Biological Assay , Culex/drug effects , Larva/drug effects , Metal Nanoparticles/ultrastructure , Microscopy, Atomic Force , Particle Size , Spectrophotometry, Ultraviolet , Spectroscopy, Fourier Transform Infrared , X-Ray Diffraction
16.
Article in English | MEDLINE | ID: mdl-22885083

ABSTRACT

Few transition metal complexes of tetradentate N(2)O(2) donor Schiff base ligands containing 2-hydroxybenzylidene-4-aminoantipyrine and amino acids (alanine/valine) abbreviated to KHL(1)/KHL(2) have been synthesized. All the metal complexes have been fully characterized with the help of elemental analyses, molecular weights, molar conductance values, magnetic moments and spectroscopic data. The Schiff bases KHL(1)/KHL(2) are found to act as tetradentate ligands using N(2)O(2) donor set of atoms leading to a square-planar geometry for the complexes around the metal ions. The binding behaviors of the complexes to calf thymus DNA have been investigated by absorption spectra, viscosity measurements and cyclic voltammetry. The DNA binding constants reveal that all these complexes interact with DNA through minor groove binding mode. The studies on mechanism of photocleavage reveal that singlet oxygen ((1)O(2)) and superoxide anion radical (O(2)(-)) may play an important role in the photocleavage. The Schiff bases and their metal complexes have been screened for their in vitro antibacterial activities against Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus epidermidis, Klebsiella pneumoniae and antifungal activities against Aspergillus niger, Fusarium solani, Culvularia lunata, Rhizoctonia bataicola and Candida albicans by MIC method.


Subject(s)
Amino Acids/metabolism , Ampyrone/metabolism , Benzylidene Compounds/metabolism , DNA/metabolism , Absorption , Ampyrone/chemistry , Animals , Anti-Infective Agents/pharmacology , Bacteria/drug effects , Benzylidene Compounds/chemistry , Cattle , Electric Conductivity , Electrochemical Techniques , Electron Spin Resonance Spectroscopy , Electrons , Electrophoresis, Agar Gel , Fungi/drug effects , Ligands , Magnetic Phenomena , Magnetic Resonance Spectroscopy , Mass Spectrometry , Microbial Sensitivity Tests , Plasmids/metabolism , Schiff Bases/chemical synthesis , Schiff Bases/chemistry , Solutions , Spectrophotometry, Infrared , Spectrophotometry, Ultraviolet , Viscosity
17.
Article in English | MEDLINE | ID: mdl-22446764

ABSTRACT

A series of Cu(II), Ni(II) and Zn(II) complexes of the type ML have been synthesized with Schiff bases derived from o-acetoacetotoluidide, 2-hydroxybenzaldehyde and o-phenylenediamine/1,4-diaminobutane. The complexes are insoluble in common organic solvents but soluble in DMF and DMSO. The measured molar conductance values in DMSO indicate that the complexes are non-electrolytic in nature. All the six metal complexes have been fully characterized with the help of elemental analyses, molecular weights, molar conductance values, magnetic moments and spectroscopic data. The analytical data helped to elucidate the structure of the metal complexes. The Schiff bases are found to act as tetradentate ligands using N(2)O(2) donor set of atoms leading to a square-planar geometry for the complexes around all the metal ions. The binding properties of metal complexes with DNA were investigated by absorption spectra, viscosity measurements and cyclic voltammetry. Detailed analysis reveals that the metal complexes intercalate into the DNA base stack as intercalators. All the metal complexes cleave the pUC19 DNA in presence of H(2)O(2.) The Schiff bases and their complexes have been screened for their antibacterial activity against five bacterial strains (Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus epidermidis, Klebsiella pneumoniae) by disk diffusion method. All the metal complexes have potent biocidal activity than the free ligands.


Subject(s)
Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Coordination Complexes/chemistry , Coordination Complexes/pharmacology , Transition Elements/chemistry , Transition Elements/pharmacology , Animals , Bacteria/drug effects , Bacterial Infections/drug therapy , Cattle , DNA/metabolism , Intercalating Agents/chemistry , Intercalating Agents/pharmacology , Microbial Sensitivity Tests , Nitrous Oxide/chemistry , Schiff Bases/chemistry , Schiff Bases/pharmacology , Spectrum Analysis
18.
Tumour Biol ; 33(2): 315-23, 2012 Apr.
Article in English | MEDLINE | ID: mdl-22362381

ABSTRACT

The proportion of estrogen receptor (ER)-negative and triple-negative (TN) breast cancer in Indian women is higher than that reported in the West, and this difference persists even after their migration to the West. The causes for this significant difference are not entirely clear. Hypermethylation of the ER promoter, an epigenetic alteration, is known to be one of the mechanisms by which the expression of ER is suppressed. Two thirds of breast cancer specimens from an Indian center tested, using the highly sensitive, methylation-specific polymerase chain reaction (MSP) technique, were reported positive. We have used a quantitative assay, the MethyLight, to better assess the extent of methylation in the ESR1 promoter region in 98 breast cancer tumor specimens from Indian women. In addition, the amount of ER transcripts was determined by quantitative reverse transcriptase polymerase chain reaction. Using the stringent cutoff of at least 4% of the target sequence being methylated, 27% of TN tumors were methylated. In addition they demonstrated the highest levels of methylation. In contrast less than 2% ER-positive tumors were hypermethylated. While the proportion of hypermethylated tumors are lower in this study than that estimated using MSP, our results support the notion of increased epigenetic deregulations in ER-negative tumors in general and TN tumors in particular. The development of this assay also permits a rational approach to the selection of patients for clinical trials examining the efficacy of demethylating agents in the treatment of ER-negative breast cancer.


Subject(s)
Breast Neoplasms/genetics , Epigenesis, Genetic , Estrogen Receptor alpha/genetics , Gene Silencing , Aged , Breast Neoplasms/ethnology , CpG Islands , DNA Methylation , Female , Gene Expression Profiling , Gene Expression Regulation, Neoplastic , Genetic Techniques , Humans , India , Middle Aged , Polymerase Chain Reaction/methods , Promoter Regions, Genetic , Sensitivity and Specificity , Sequence Analysis, DNA
19.
Article in English | MEDLINE | ID: mdl-22020164

ABSTRACT

Few novel 4-aminoantipyrine derived Schiff bases and their metal complexes were synthesized and characterized. Their structural features and other properties were deduced from the elemental analysis, magnetic susceptibility and molar conductivity as well as from mass, IR, UV-vis, (1)H NMR and EPR spectral studies. The binding of the complexes with CT-DNA was analyzed by electronic absorption spectroscopy, viscosity measurement, and cyclic voltammetry. The interaction of the metal complexes with DNA was also studied by molecular modeling with special reference to docking. The experimental and docking results revealed that the complexes have the ability of interaction with DNA of minor groove binding mode. The intrinsic binding constants (K(b)) of the complexes with CT-DNA were found out which show that they are minor groove binders. Gel electrophoresis assay demonstrated the ability of the complexes to cleave the pUC19 DNA in the presence of AH(2) (ascorbic acid). Moreover, the oxidative cleavage studies using distamycin revealed the minor groove binding for the newly synthesized 4-aminoantipyrine derived Schiff bases and their metal complexes. Evaluation of antibacterial activity of the complexes against Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus epidermidis, and Klebsiella pneumoniae exhibited that the complexes have potent biocidal activity than the free ligands.


Subject(s)
Ampyrone/pharmacology , Anti-Bacterial Agents/pharmacology , Coordination Complexes/pharmacology , DNA/metabolism , Transition Elements/pharmacology , Ampyrone/chemistry , Animals , Anti-Bacterial Agents/chemistry , Bacteria/drug effects , Bacterial Infections/drug therapy , Cattle , Coordination Complexes/chemistry , Schiff Bases/chemistry , Schiff Bases/pharmacology , Spectrum Analysis , Transition Elements/chemistry
20.
J Pharm Anal ; 2(4): 314-318, 2012 Aug.
Article in English | MEDLINE | ID: mdl-29403760

ABSTRACT

Two highly sensitive methods for the determination of genotoxic alkyl methane sulfonates (AMSs) and alkyl paratoluene sulfonates (APTSs) in lamivudine using hyphenated techniques have been presented. AMSs were determined by GC-MS method using GSBP-INOWAX (30 m×0.25 mm×0.25 µm) column. Temperature program was set by maintaining at 100 °C initially for 3 min, then rised to 220 °C at the rate of 15 °C/min and maintained at 220 °C for 16 min. N,N-dimethyl formamide was used as diluent. APTSs were determined by LC-MS using Zorbax, Rx C8, 250 mm×4.6 mm, 5 µm column as stationary phase. 0.01 M ammonium acetate is used as buffer. The mixture of buffer and methanol in 75:25 (v/v) ratio was used as mobile phase A and mixture of buffer and methanol in 5:95 (v/v) ratio was used as mobile phase B. The gradient program (T/%B) was set as 0/28, 16/50, 17/100, 23/100, 27/28 and 40/28. Both the methods were validated as per International Conference on Harmonization guidelines. Limit of quantitation was found 1.5 µg/mL for AMSs and was in the range of 1.0-1.5 µg/mL for APTSs.

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