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1.
Eur J Med Chem ; 135: 434-446, 2017 Jul 28.
Article in English | MEDLINE | ID: mdl-28475971

ABSTRACT

Two mononuclear copper (II) terpyridine complexes namely, [Cu(Btptpy) (ClO4)](ClO4) 1, and [Cu(Bttpy) (ClO4)](ClO4) 2, (Btptpy (L1) = 4'-(Benzothiophene)-2,2':6',2″-terpyridine, Bttpy (L2) = 4'-(Benzylthiazolyl)-2,2':6',2″-terpyridine) have been synthesized and characterized. Single crystal X-ray diffraction shows that, both ligands belong to monoclinic crystal system with space group P21/c (L1) and P21/n (L2). Absorption spectral titration, DNA melting study, circular dichroism and viscosity measurement reveal that, complex 1 and 2 bind with DNA through intercalation. In addition, interaction between the two copper (II) complexes and bovine serum albumin (BSA) has been studied by fluorescence titration, circular dichroism and their protease activity has been investigated using SDS-PAGE gel electrophoresis. Agarose (AGE) and SDS-PAGE gel electrophoresis reveals both complexes have good nucleolytic and proteolytic property in the presence of additive hydrogen peroxide. Both complexes shows remarkable cytotoxic property against triple negative CAL-51 human breast cancer cell line and hepatocellular carcinoma (HepG2) cancer cell lines and bears very less cytotoxicity towards liver normal cell line (Changs). DCF-DA and TBRAS assay also supported that complex 1 and 2 induces elevated level of reactive oxygen species (ROS) and oxidative stress in cancer cells than normal cell line. Furthermore, FACS analysis confirms complex 1 and 2 brings apoptosis by growth phase cell cycle arrest.


Subject(s)
Antineoplastic Agents/pharmacology , DNA/chemistry , Organometallic Compounds/pharmacology , Serum Albumin, Bovine/chemistry , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Cell Line , Cell Proliferation/drug effects , Copper/chemistry , Copper/pharmacology , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Hep G2 Cells , Humans , Molecular Structure , Organometallic Compounds/chemical synthesis , Organometallic Compounds/chemistry , Pyridines/chemistry , Pyridines/pharmacology , Structure-Activity Relationship , Thiazoles/chemistry , Thiazoles/pharmacology , Thiophenes/chemistry , Thiophenes/pharmacology
2.
Spectrochim Acta A Mol Biomol Spectrosc ; 138: 158-63, 2015 Mar 05.
Article in English | MEDLINE | ID: mdl-25498811

ABSTRACT

Single crystals of ethylenediaminium di(4-nitrophenolate) [EDA4NP] were grown by slow evaporation solution growth technique using ethanol as solvent at constant temperature. It crystallizes in monoclinic centrosymmetric space group C2/c with cell dimension a=11.326Ǻ, b=7.264Ǻ, c=20.036Ǻ; ß=93.55°. Fourier Transform Infra Red (FT-IR) spectrum was recorded to identify various functional groups present in EDA4NP. Nuclear Magnetic Resonance (NMR) spectral studies were performed to confirm the functional groups. Thermogravimetric analysis and differential thermal analysis showed that the compound melts at 142.9°C. The material possesses a wide optical transparency window in the visible and near IR region (500-1200nm). The nonlinear refractive index, nonlinear absorption coefficient and third-order nonlinear susceptibility of EDA4NP were estimated to be n2=5.46×10(-8)cm(2)W(-1), ß=0.65×10(-3)cmW(-1) and χ((3))=2.96×10(-6)esu respectively. The limiting behavior observed with the sample is attributed mainly to nonlinear refraction.


Subject(s)
Nitrophenols/chemistry , Crystallization/methods , Crystallography, X-Ray , Differential Thermal Analysis , Magnetic Resonance Spectroscopy , Nonlinear Dynamics , Refractometry , Spectroscopy, Fourier Transform Infrared , Thermogravimetry
3.
Chin J Nat Med ; 11(5): 500-5, 2013 Sep.
Article in English | MEDLINE | ID: mdl-24359774

ABSTRACT

AIM: Dasyatis jenkinsii is used traditionally to treat inflammatory complaints and arthritis by the fisherman community and local population. The present study was designed to scientifically investigate the traditional practice through the analgesic, anti-inflammatory, and organ toxicity studies and characterization of bioactive compounds of crude extracts of D. jenkinsii. METHOD: Solvent extract of homogenized fresh fish was prepared using petroleum ether and diethyl ether. The chemical and spectral analyses of extracts were carried out using FT-IR and GC-MS. Analgesic and anti-inflammatory activities were assessed by hot plate, tail clip, and carrageenan induced rat paw edema methods. The organ toxicity of each extract was assessed on brain, liver, and kidney of mice. RESULTS: The IR spectrum indicated the presence of aromatic and aliphatic compounds. GC-MS analysis revealed the presence of 1-(4-carboxy)phenylnona-2, 5-diene and 3-hydroxymono-glyceryl hydrogen phthalate in the petroleum ether extract and carboxyl serine, dihydrotryptophan, and indolyl carboxylic acid in the diethyl ether extract. Both extracts showed significant analgesic and anti-inflammatory effects in all the methods tested. The vital organs of the test animals were not affected by the crude extracts significantly. CONCLUSIONS: The presence of biologically active compounds in the crude extracts with analgesic and anti-inflammatory properties justifies the traditional knowledge and paves the way for isolation of these compounds for further experimentation.


Subject(s)
Analgesics/administration & dosage , Analgesics/chemistry , Anti-Inflammatory Agents/administration & dosage , Anti-Inflammatory Agents/chemistry , Edema/drug therapy , Pain/drug therapy , Skates, Fish , Animals , Humans , Male , Mice , Rats , Spectroscopy, Fourier Transform Infrared
4.
J Environ Biol ; 34(3): 663-6, 2013 May.
Article in English | MEDLINE | ID: mdl-24617156

ABSTRACT

Genetic diversity was analysed in three populations of the mangrove species, Avicennia marina by using random amplified polymorphic DNA-polymerase chain reaction (RAPD-PCR). Ten random decamer primers were used to score the diversity from three locations of eastcoast of India: Parangipettai (Tamil Nadu), Kakkinada (Andhra Pradesh) and Sundarbans (West Bengal). These primers produced 388 scorable DNA fragments, of which 252 (64.98%) were polymorphic, 182 (46.90%) were monomorphic, and 14 (3.61%) were unique. RAPD banding patterns displayed variations between and within the populations, while, there was no morphological variation.


Subject(s)
Avicennia/genetics , Genetic Markers , Random Amplified Polymorphic DNA Technique , Animals , Avicennia/classification , India , Phylogeny , Polymerase Chain Reaction
5.
Chin J Nat Med ; 10(1): 77-80, 2012 Jan.
Article in English | MEDLINE | ID: mdl-23302537

ABSTRACT

AIM: Mangrove is one of the oldest living tree species and its leaves are among the most extensively studied botanicals in use today. Scientific research throughout the world has found evidence to support the fact that its foliar extracts have great potential against human microbial pathogens. This study highlights the isolation of foliar fungi from Rhizophora mucronata, Avicenna officialis and Avicenna marina. METHOD: It was isolated in Sabouroud's Dextrose Agar and mass cultivation was done in Sabouroud's Dextrose broth. RESULTS: The ethyl acetate extract showed maximum antibacterial activity which inturn checked for different concentration against bacterial pathogens and anticancer activity for Hep2 and MCF7 cell line in vitro. The DNA was isolated from the fungi and the ITS region of 5.8 s RNA was sequenced and assigned to new species as they are separated from the type strains phylogenetic neighbors by sequence similarities. CONCLUSION: This preliminary screening of fungal endophytes revealed their potential to yield potent bioactive compounds for drug discovery programmes.


Subject(s)
Anti-Bacterial Agents/therapeutic use , Antineoplastic Agents/therapeutic use , Avicennia/microbiology , Biological Products/therapeutic use , Hypocrea , Neoplasms/drug therapy , Rhizophoraceae/microbiology , Anti-Bacterial Agents/pharmacology , Antineoplastic Agents/pharmacology , Base Sequence , Biological Products/pharmacology , Cell Line, Tumor , DNA, Fungal , Endophytes , Humans , Hypocrea/genetics , MCF-7 Cells , Phylogeny , Phytotherapy , RNA, Satellite , Species Specificity
6.
Asian Pac J Trop Biomed ; 1(5): 376-80, 2011 Oct.
Article in English | MEDLINE | ID: mdl-23569796

ABSTRACT

OBJECTIVE: To isolate and characterize the bioactive secondary metabolites from Aspergillus ochraceus (A. ochraceus) MP2 fungi. METHODS: The anti bacterial activity of marine sponge derived fungi A. ochraceus MP2 was thoroughly investigated against antagonistic human pathogens. The optimum inhibitory concentration of the fungi in the elite solvent was also determined. The promising extracts that showed good antimicrobial activity were subjected to further analytical separation to get individual distinct metabolites and the eluants were further identified by GC MS instrumental analysis. The molecular characterization of the elite fungal strains were done by isolating their genomic DNA and amplify the internal transcribed spacer (ITS) region of 5.8s rRNA using specific ITS primer. The novelty of the strain was proved by homology search tools and elite sequences was submitted to GENBANK. RESULTS: Three bioactive compounds were characterized to reveal their identity, chemical formula and structure. The first elutant was identified asα- Campholene aldehyde with chemical formula C10 H16 O and molecular weight 152 Da. The second elutant was identified as Lucenin-2 and chemical formula C27 H30 O16 and molecular weight 610 Da. The third elutant was identified as 6-Ethyloct- 3-yl- 2- ethylhexyl ester with Chemical formula C26 H42 O4 with molecular weight 418 Da. CONCLUSIONS: The isolated compounds showed significant antimicrobial activity against potential human pathogens. Microbial secondary metabolites represent a large source of compounds endowed with ingenious structures and potent biological activities.


Subject(s)
Anti-Bacterial Agents/chemistry , Aspergillus ochraceus/chemistry , Bacteria/drug effects , Animals , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/pharmacology , Microbial Sensitivity Tests , Porifera/microbiology
7.
Phys Rev Lett ; 101(24): 246801, 2008 Dec 12.
Article in English | MEDLINE | ID: mdl-19113643

ABSTRACT

We report Coulomb drag measurements on GaAs-AlGaAs electron-hole bilayers. The two layers are separated by a 10 or 25 nm barrier. Below T approximately 1 K we find two features that a Fermi-liquid picture cannot explain. First, the drag on the hole layer shows an upturn, which may be followed by a downturn. Second, the effect is either absent or much weaker in the electron layer, even though the measurements are within the linear response regime. Correlated phases have been anticipated in these, but surprisingly, the experimental results appear to contradict Onsager's reciprocity theorem.

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