17 research outputs found

    Morphological changes in MCF-7 human breast cancer cells in response to Bis-Naphthalimidopropylspermidine-treatment.

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    The effects of bis-naphthalimidopropylspermidine (BNIPSpd), a representative of a novel class of polyamine derivatives with antiproliferative properties on the morphology of MCF-7 human breast cancer cells were studied. BNIPSpd was shown to cause cytoplasmic shrinkage, observed by monitoring the cells by means of phase-contrast microscopy. Chromatin condensation and nucleolar disintegration were also detected by Hoechst 33342 and Giemsa staining the cells, treated with 10 μM BNIPSpd for 8h. Taken together the morhological changes observed strongly suggested that the growth inhibition of MCF- 7 cells in response to BNIPSpd-treatment is realized via an induction of apoptosis. Moreover, nucleolus appears to be an important target in the mode of cytotoxic action of this novel polyamine derivative

    Anti-pancreatic cancer potential of secalonic acid derivatives from endophytic fungi isolated from Ocimum basilicum.

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    The word endophyte means "in the plant" and refers to all microorganisms that live in the intercellular spaces of stems, petioles, roots and leaves of plants causing no apparent symptoms of disease. Seven endophytic fungi were isolated from the medicinal plant of Ocimum basilicum L. The fungal strain, labeled as 2L, was cultivated at large scale on the potato dextrose agar semi solid medium and was extracted with ethyl acetate. Normal phase silica gel column chromatography of the ethyl acetate extract afforded ergosterol (1), secalonic acid A (2) and secalonic acid D (3). The structures of these compounds (1-3) were elucidated unequivocally by UV, IR, MS, a series of 1D & 2D NMR analyses. The cytotoxicity of these compounds was evaluated by the MTT assay against human pancreatic cancer cell line. Secalonic acid A (2) and secalonic acid D (3) exhibited significant anti-pancreatic cancer activity with IC 50 values of 7.3 and 1.6 µM, respectively

    Study into the polyphenol content and antioxidant activity of rapeseed pomace extracts.

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    Rapeseed pomace (RSP) is a waste product obtained after edible oil production from Brassica napus. This study aimed to determine the polyphenol content, radical scavenging activity, ferric iron reducing antioxidant power and the oxygen-radical absorbance capacity assay, of RSP extracts, with regard to their potential application in the treatment or prevention of neurodegenerative diseases. High performance liquid chromatography/mass spectrometry was applied to determine ubiquitous polyphenolic compounds. Three different extraction methods (Soxhlet-, ultra sonic assisted- and accelerated solvent extractions) were applied on 2 harvest years (2012, 2014). From the extracts obtained, the total phenolic content (Folin–Ciocalteu assay) was found to be between 5·54 (SD 0·28) and 2·48 (SD 0·06) gallic acid equivalents/100 mg dry weight. The ferric iron reducing antioxidant power (FRAP assay) is ranging from 0·834 (SD 0·01) to 0·34 (SD 0·01) Trolox equivalents/100μg. The IC50 values for the radical scavenging (DPPH) assay were found to be between 49·23 (SD 14·00) and 180·30 (SD 16·16) μg/mL. Liquid chromatography-mass spectrometry of the RSP extracts showed substantial presence of several phenolic compounds, the most abundant one being sinapic acid (7496·7 (SD198·9) − 1923·3 (SD18·4) mg/kg). Significant differences (2-way ANOVA, p < 0·0001) were found between the 3 different extraction techniques for all the tested antioxidant properties. The strong antioxidant properties demonstrated by the RSP extracts in this study warrants further investigation for their potential use in the treatment or prevention of oxidative stress related diseases

    Revalorisation of rapeseed pomace extracts: an in vitro study into its anti-oxidant and DNA protective properties

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    Rapeseed pomace (RSP) is a waste product obtained after edible oil production from Brassica napus. Analysis of ubiquitous secondary metabolites in RSP samples (two breeds, harvested in 2012/2014 respectively from North East of Scotland) and their ethanol/water (95:5) Soxhlet extracts were carried out. Soxhlet extraction of the RSP (petroleum ether followed by 95% ethanol) gave a solid extract. LC-MS/MS data of the extracts revealed several secondary metabolites, with Sinapic acid being the most abundant. Strong antioxidant activities of the Soxhlet extracts were confirmed from the results obtained in the FRAP, DPPH and ORAC assays. Furthermore, for the very first time, RSP extracts (13.9µg/ml) provided complete DNA protection, from oxidative stress induced by AAPH (3.5mM). Therefore the strong antioxidant and DNA protecting properties demonstrated by the RSP extracts in this study warrants further investigation for their revalorisation and potential use as reliable source of antioxidants in different food applications.Gary Duncan for the LC-MS/MS analysis and financial support from Tenovus Scotland – Grampian.info:eu-repo/semantics/publishedVersio

    Direct observation of two base-pairing modes of a cytosine-thymine analogue with guanine in a DNA z-form duplex: significance for base analogue mutagenesis. [Dataset]

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    The pyrimidine nucleobase analogue 6H,8H-3,4-dihydropyrimido[4,5-c]-[1,2]oxazin-7-one (P) is a mimic both of cytosine and thymine, since it can form stable hydrogen-bonded base-pairs with either guanine or adenine. To investigate the geometric properties of pairing with guanine in a DNA double helix, the structure of d(CGCGPG)2 has been determined by single crystal X-ray analysis. The oligonucleotide crystallised as a left-handed Z-DNA duplex in the orthorhombic space group P212121 with cell dimensions a = 18.23 Å, b = 30.63 Å, c = 43.78 Å. Refinement using NUCLSQ with 51 water molecules included in the final model converged at R = 0.179 (Rw = 0.159) for 2798 reflections (F > 2s(F)) in the range 8 Å to 1.7 Å. Remarkably, the two P·G pairs in the hexamer duplex are different: UK Watson-Crick and wobble types separately illustrate both cytosine-like and thymine-like behaviour. The result suggests that mutagenesis experiments involving P and other analogues which display pronounced base-pairing ambivalence can be used to examine the structural basis of substrate discrimination by polymerases that is essential to accurate genetic replication. The data for this output can be found at : https://doi.org/10.2210/pdb223d/pdb
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