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PubMed2004

2-Phenyl-3-(quinolizidin-1-yl)-5-substituted indoles as platelet antiaggregating agents.

A set of ten 2-phenyl-3-(quinolizidin-1-yl)-5-substituted indoles was prepared through the Fischer cyclization of lupinyl- and epi-lupinylphenylketone 4-substituted phenylhydrazones. Compounds were tested for antiaggregating activity on human platelets activated by adenosine diphosphate (ADP), collagen and adrenaline. At 2.5 x 10(-4) M concentration most compounds strongly inhibited the aggregation induced by all the agonists considered and many of them still displayed good activity at 0.625 x 10(-4) M concentration. The least active (1c) and one of the most active (1d) compounds were also tested for antiaggregating activity on rabbit platelets activated by ADP, PAF and sodium arachidonate. Both the compounds were active against ADP and PAF, but only 1d inhibited the arachidonate-induced aggregation (100% at 8 x 10(-6) M concentration) and increased the bleeding time in mice. The same compounds were subjected to a general pharmacological screening and found to display several activities; of particular interest was the dose dependent reduction of serum cholesterol and heparin precipitating betalipoproteins in hypercholesterolemic mice exerted by 1c, which was still significant at the oral dose of 10 mg/kg.

Adenosine Diphosphate↗

PubMed2004

Quinoxaline chemistry. Part XVII. Methyl [4-(substituted 2-quinoxalinyloxy) phenyl] acetates and ethyl N-([4-(substituted 2-quinoxalinyloxy) phenyl] acetyl) glutamates analogs of methotrexate: synthesis and evaluation of in vitro anticancer activity.

Fourteen out of 21 quinoxaline derivatives described in the present paper were selected at NCI for evaluation of their in vitro anticancer activity. Preliminary screening showed that some derivatives exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10(-5) and 10(-4) M concentrations. Interesting selectivities were also recorded between 10(-8) and 10(-6) M for the compounds 9 and 13.

Antimetabolites, Antineoplastic↗

PubMed2004

Mutagenic activity of sweepings and pigments from a household-wax factory assayed with Salmonella typhimurium.

The mutagenic activity of garbage originating from a household wax industry was determined by the Salmonella/microsome assay, using the bacterial strains TA100, TA98 and YG1024. The garbage was obtained by sweeping the floor of the factory at the end of the work shift. Organic compounds were extracted by ultrasound for 30 min in dichloromethane or 70% ethanol. After evaporation of solvent, these extracts (HFS: household-wax factory sweepings) were dissolved in DMSO, and were tested for the mutagenic activity at varying concentrations (HFS-ET: 0.08-0.68 mg/plate, HFS-DCM: 0.60-7.31 mg/plate). The colouring agents (pigments) used in the production of the wax were also dissolved in DMSO and tested with the assay. The concentrations tested for each pigment were: Amaranth: 0.46-3.65 mg/plate, Auramine: 0.15-1.2 mg/plate and Rhodamine B: 0.22-1.82 mg/plate. Both ET and DCM organic extracts had mutagenic activity, especially in the YG1024 strain. The pigments behaved in a similar way, demonstrating that YG1024 was the most sensitive strain for the detection of mutagenicity, and that metabolization increased the activity. Human exposure (occupational and non-occupational) to industrial residues generated during the household-wax manufacturing and packaging process should be monitored, since this type of garbage is normally deposited in the environment without any control.

Animals↗

PubMed2005

Liriodenine inhibits the proliferation of human hepatoma cell lines by blocking cell cycle progression and nitric oxide-mediated activation of p53 expression.

Liriodenine was isolated from the leaves of Michelia compressa. This study was designed to assess cell cycle arrest, the production of nitric oxide (NO) and p53 expression in liriodenine-treated human hepatoma cell lines, including wild-type p53 (Hep G2 and SK-Hep-1). As evidenced by flowcytometric studies, liriodenine induced cell cycle G(1) arrest and inhibited DNA synthesis in Hep G2 and SK-Hep-1 cell lines. The p53, iNOS expression and intracellular NO level were markedly increased in Hep G2 cells after liriodenine treatment. A NO inhibitor, carboxy-PTIO inhibited the p53 expression induced by liriodenine. In addition, liriodenine could not induce obvious cytotoxicity in normal human IMR-90 cell line. These results demonstrate that NO production and p53 expression are critical factors in liriodenine-induced growth inhibition in human wild-type p53 hepatoma cells.

Antimetabolites↗

PubMed2006

A novel retinoid binding property of human annexin A6.

Vitamin A (all-trans retinol) and all-trans retinoid acid (ATRA) interacted with human annexin A6 (AnxA6) as evidenced by AnxA6-induced blue shift of retinoid absorption maxima, by AnxA6-Trp fluorescence quenching and by a fluorescence resonance energy transfer from a Trp residue of AnxA6 to retinol. In addition, both retinoids stimulated the calcium-dependent binding of AnxA6 to liposomes, accompanied by oligomerization of AnxA6. Up to our knowledge, it is a first report supporting the hypothesis of a direct implication of AnxA6 in vitamin A-dependent tissue mineralization.

Annexin A6↗

PubMed2006

Bismuth-norfloxacin complex: synthesis, physicochemical and antimicrobial evaluation.

Norfloxacin is a fluoroquinolone antibacterial agent which is active against various Gram-positive as well as Gram-negative microorganisms. Presence of metal ions considerably alters the activity of fluoroquinolones against potentially susceptible bacteria. As bismuth is known to possess a good antibacterial activity, bismuth complex of norfloxacin was prepared by reacting bismuth citrate with aqueous solution of norfloxacin. The structure of the bismuth-norfloxacin complex (BNC) was confirmed by spectral, chemical and elemental analysis. Antimicrobial studies were carried out using agar diffusion method against Escherichia coli (ATCC 25922), Klebsiella pneumoniae (NTCC 10320), Staphylococcus aureus (ATCC 29213), Bacillus pumilis (NTCC 8241) and Staphylococcus epidermidis (ATCC 12228). The results showed significant increase (p<0.05, Tukeys test) in antibacterial activity of BNC as compared with norfloxacin and physical mixture of norfloxacin and bismuth citrate. This increase in activity is being considered due to increased bioavailability of the metal drug complex. Thus, the use of the BNC may be preferable over norfloxacin alone.

Anti-Bacterial Agents↗

PubMed2004

Spectral analysis and fingerprinting for biomedia characterisation.

Classical culture media, as well as domestic and/or industrial wastewater treated by biological processes, have a complex composition. The on-line and/or in situ determination of some substances is possible, but expensive, as sample collection and pre-treatment are often necessary with strict rules of sterility. More global methods can be used to detect rapidly "accidents" such as the appearance of an undesirable by-product in a fermentation broth or of a toxic substance in wastewater. These methods combine a "hard" part, for sensing, and a "soft" part, for data treatment. Among potential "hard" candidates, spectroscopy can be the basis for non-invasive and non-destructive measuring systems. Some of them have been already tested in situ: ultra-violet-visible, infra-red (mid or near), fluorescence (mono-dimensional, two-dimensional or synchronous), dielectric, while others, more sophisticated, such as mass spectrometry, coupled or not to pyrolysis, nuclear magnetic resonance and Raman spectroscopy, have been proposed. All these methods provide spectra, i.e. large sets of data, from which meaningful information should be rapidly extracted, either for analysis or fingerprinting. The recourse to data-mining techniques (the "soft" part) such as principal components analysis, projection on latent structures or artificial neural networks, is a necessary step for that task. A review of techniques, mostly based on spectroscopy, with examples taken in the bioengineering field in general is proposed.

Biotechnology↗

PubMed2004

Preparative high-performance liquid chromatographic separation and analysis of the Maltacine complex - a family of cyclic peptide antibiotics from Bacillus subtilis.

Purification of secondary metabolites from fermentation broths can be a challenging task both due to the complexity of the medium, inherently unstable molecular structures or by the action of enzymes present in the fermentation broth leading to poor isolation yield and loss of antibiotic activity. A combination of different purification techniques has usually been used to arrive at acceptable purities for characterisation of the target molecules. Due to rapid decay of antimicrobial activity a rapid preparative high-performance liquid chromatography (HPLC) method was developed that provided separation and resolution of a family of 18 closely related cyclic peptides within 110 min with minimal loss of activity. Characterisation of the peptides with LC-MS, UV/IR spectroscopy and amino acid analysis disclosed 20 different peptides with cyclic structures (lactones) with molecular weights between 1447.7 and 1519.8 Da. No peptide antibiotics with identical molecular weights have previously been reported in the literature, which lead us to conclude that this peptide complex has not been discovered before. We have named them Maltacines.

Anti-Bacterial Agents↗

PubMed2007

Isolation and characterization of antioxidant and antibacterial compound from mango ginger (Curcuma amada Roxb.) rhizome.

The chloroform extract of mango ginger (Curcuma amada Roxb.) rhizome was subjected to antioxidant activity-guided purification by repeated silica gel column chromatography to obtain a pure antioxidant compound. The structure was deduced by analyzing UV, IR, liquid chromatography-mass spectrometry (LC-MS) and two-dimensional heteronuclear multiple quantum coherence transfer spectroscopy (2D-HMQCT) NMR spectral data, and named it as "Amadannulen", a novel compound. It exhibited DPPH radical scavenging activity, super oxide radical scavenging activity, lipid peroxidation inhibitory activity and metal chelating activity. Amadannulen also showed antibacterial activity against both Gram-positive and Gram-negative bacteria tested. It also exhibited bactericidal activity against M. luteus, B. cereus and B. subtilis.

Anti-Bacterial Agents↗

PubMed2004

Investigation of spherical oil agglomeration properties of celestite.

In this study, concentration of celestite particles was investigated by using oil agglomeration. For this purpose, effects of operating parameters were investigated, and zeta potential measurements and Fourier transform infrared spectrophotometry (FTIR) analyses have also been carried out. In the experiments, effects of operating parameters such as pH, stirring speed, amount of Na oleate as a anionic type collector and kerosene as a bridging liquid, solid ratio, agglomeration time, collector stirring time, conditioning time, and amount of EDTA were investigated to obtain optimum conditions. Zeta potential measurements were carried out for various pH values and amounts of Na oleate. FTIR analyses were investigated to determine the adsorption type of Na oleate on celestite surface. By evaluation of the experimental results, optimum oil agglomeration conditions of celestite were determined as follows: pH 7, stirring speed 1500 rpm, amount of kerosene 100 l/t, amount of Na oleate 10 kg/t, solid ratio 5 wt%, conditioning time 5 min, collector stirring time 1 min, agglomeration time 5 min, and amount of EDTA 1.0 kg/t. In the optimum conditions, celestite was concentrated with recovery of 89.47 wt%.

Journal Article↗

PubMed2005

The sorption behavior of a nickel-insolubilized humic acid system in a column arrangement.

The sorption characteristics of insolubilized humic acid (IHA) were investigated for Ni (II) in a column arrangement. The sodium form of the IHA (INaA) was used as a solid phase. Column operations were performed with five steps and all of them were monitored continuously by a flowthrough cell-adapted UV-Vis spectrophotometer. Thus, all solid-phase extraction (SPE) steps were visualized by breakthrough curves and analyses progress were evaluated. However, all calculations and evaluations were focused on the atomic absorption spectrophotometric (AAS) analyses of the solutions collected during the stripping steps. There was a high correlation (r(2), 0.972) between peak area and AAS data of stripping steps. The effect of concentration and pH of the loading solution onto sorption of Ni (II) by INaA was investigated. Sorption characteristics were evaluated by using Freundlich, Langmuir, and Dubinin-Radushkevich (D-R) adsorption isotherms, as well as by Scatchard plot analysis. Multilayer sorption was found to be agreeable for Ni (II). From the D-R isotherm the mean free energy of sorption (E) was calculated (6.65 kJ mol(-1)) and attributed to the multilayer sorption. Finally, the sorption characteristic of the INaA-Ni (II) system was compared with that of the INaA-Cu (II) system, and possible separation of two ions in a binary mixture system is discussed.

Adsorption↗

PubMed2005

Designing of the centers for adsorption of bile acids on a silica surface.

Silicas chemically modified with attached aminopropyl, imidazolyl, and trimethylsilyl groups, with adsorptive and coordinative grafted hemin were synthesized. Adsorption of some bile acids on the surface of hydroxylated silica, synthesized siliceous adsorbents and cholestyramine has been studied. It was found that the main contribution to the total adsorption is caused by electrostatic attraction between anions of bile acids and positively charged sites of the surface of modified silica and also by dispersion interactions between steroid skeleton of bile acids and functional groups of modified silicon dioxides. It was established that the kinetic parameters of adsorption and adsorptive capacity for all investigated siliceous adsorbents exceed similar characteristics for cholestyramine. The best of synthesized adsorbents is hemin-containing adsorbent IX, and the sequence of increase in its adsorptive capacity in relation to bile acids corresponds to the following series: I < III < II, IV < VI < V < VIII < VII < IX.

Adsorption↗

PubMed2005

Poly(sebacic acid-co-ricinoleic acid) biodegradable carrier for paclitaxel--effect of additives.

Injectable polymeric formulation for paclitaxel was studied. Poly ricinoleic acid and sebacic acid were synthesized. The effect of additives on the viscosity of polymer, paclitaxel release, and polymer degradation was investigated both in vitro and in vivo. Additives that were used in this study were ricinoleic acid, phospholipid, PEG 400, and PEG 2000. Addition of 20% ricinoleic acid to P(SA:RA)3:7 liquefied the formulation and allowed injection of the formulation containing paclitaxel via a 22-G needle at room temperature with no effect on paclitaxel release rate. Addition of PEG 400, PEG 2000, and phospholipid to the formulation did not affect the paclitaxel release from the formulation. The degradation of modified formulations with paclitaxel and additives was examined in vitro and by subcutaneous injection of liquid formulations to the backspace via a 22-G needle into seven groups of four C3H mice. In vivo formulations with additives (20% ricinoleic acid and PEG or phospholipid) and 5% paclitaxel content degraded faster than the formulation with only 20% ricinoleic acid and the same paclitaxel content: 51% and 54% versus 43%. The slowest degradation (26% in 1 week) was of the formulation containing 10% paclitaxel. The release rate in vivo was affected by the paclitaxel content; the higher the content, the slower was the release. By using additives, we could adjust the physical characteristics of the surgical paste while maintaining a desirable system for sustained paclitaxel release.

Animals↗

PubMed2005

Cytotoxicity of plants from Malaysia and Thailand used traditionally to treat cancer.

The SRB cytotoxicity assay was used to screen extracts and isolated constituents of some traditional medicinal plants from Malaysia and Thailand against two human cancer cell lines, COR L23 lung cancer cell line and MCF7 breast cancer cell line and the non-cancer MCF5 cell line. Five out of the seven species tested, i.e. Thai Alpinia galanga, Alpinia officinarum, Cayratia japonica, Physalis minima, Tabernaemontana divaricata, exhibited interesting cytotoxicity activity and this is the first report of cytotoxicity from any Cayratia species. Following bioassay-guided fractionation, 1'-acetoxychavicol acetate (48h exposure against COR L23 cells, IC(50) 7.8 microM against MCF7 cells, IC(50) 23.9 microM) was isolated as the major cytotoxic component of the Alpinia species, physalin F as the major cytotoxic component of Physalis minima (48 h exposure against COR L23 cells IC(50) 0.4 microM against MCF7 cells, IC(50) 0.59 microM). The Malaysian Alpinia galanga showed weak activity compared with the Thai sample and this was shown to be due to the relatively high amounts of 1'-acetoxychavicol acetate present in the Thai sample.

Antineoplastic Agents, Phytogenic↗

PubMed2006

Effects of Astilbe thunbergii rhizomes on wound healing Part 1. Isolation of promotional effectors from Astilbe thunbergii rhizomes on burn wound healing.

The dried rhizomes of Astilbe thunbergii (Sieb. et Zucc) Miq (Saxifragaceae) have been traditionally used for the treatments of a sword cut, wound bitten by animals, frost-bite, burn, suppurative dermatitis or skin inflammatory diseases from the Tang period (about 8th century) in China. The physiological actions, especially the wound-healing effects of this drug are not yet well understood. In this study, we examined the effects of an ethanol extract of Astilbe thunbergii rhizomes on burn wound healing in mice. The topical application at a dose of 100mg ointment per wound of 70% ethanol extract (0.5 or 1.0% (w/w) ointment) of this drug promoted the burn wound healing. The ethanol extract was divided into two fractions (ethyl acetate-soluble and -insoluble fractions), and it was found that the topical application at a dose of 100mg ointment per wound of the ethyl acetate-soluble fraction (0.5 and 1.0% ointment) promoted the burn wound healing. Based on this finding, we attempted to isolate the active substance(s) from the ethyl acetate-soluble fraction. Three active substances 1, 2 and 3, were obtained from A. thunbergii rhizomes as promotional effectors of burn wound healing in mice. Based on the analysis of (1)H and (13)C NMR spectra, compounds 1, 2 and 3 were identified as eucryphin (1), bergenin (2) and astilbin (3), respectively. The effective dose (ED(50)) of compounds 1, 2 and 3 on burn wound healing were 4, 190 and 64 microg/wound, respectively. Among these three compounds, eucryphin (1) promoted the burn wound healing most strongly.

Acetates↗

PubMed2006

Chelating adsorption properties of PEI/SiO(2) for plumbum ion.

In this paper, a novel adsorption material PEI/SiO(2) with strong adsorption ability towards heavy-metal ions was prepared. In preparation of PEI/SiO(2), functional macromolecule polyethyleneimine (PEI) was grafted onto the surfaces of silica gel particles via the coupling effect of gamma-chloropropyl trimethoxysilane (CP). The adsorption properties of PEI/SiO(2) for Pb(2+) ion were studied by both static and dynamic methods. The experimental results show that PEI/SiO(2) possesses very strong adsorption ability for Pb(2+) ion, the saturated adsorption amount could reach to 17.5mgg(-1), and the empirical Langmuir isotherm was found to describe well the equilibrium adsorption data. The pH and grafting amount of PEI have great influence on the adsorption amount. The Pb(2+) ions adsorbed on PEI/SiO(2) are eluted easily by diluted hydrochloric acid solution.

Adsorption↗

PubMed2004

Solution, solid state and biological characterization of ruthenium(III)-DMSO complexes with purine base derivatives.

Two new complexes of Ru(III) with purine base derivatives, [mer-RuCl(3)(acv)(DMSO-S)(C(2)H(5)OH)].C(2)H(5)OH (1) (acv=acyclovir, DMSO=dimethyl sulfoxide) and [trans-RuCl(4)(guaH)(DMSO-S)].2H(2)O (2) (guaH=protonated molecule of guanine), were prepared from the same Ru(III) precursor, [trans-RuCl(4)(DMSO-S)(2)](-), by substitution of one DMSO-S. Coordination of acv induced also replacement of one chloride by an ethanol molecule. This reactivity difference was explained by striking contrasts in the hydrogen bonding schemes of the two complexes, evidenced in their X-ray crystal structures. In 1 the guanine derivative acyclovir is coordinated to ruthenium through the N(7) atom, while in 2 the protonated guanine molecule is bound through the N(9) atom. Both complexes were also characterized by various physico-chemical methods in the solid state and in the solution. In vitro, the biological activity of 2 and of the previously described complexes [mer-RuCl(3)(acv)(DMSO-S)(CH(3)OH)].0.5CH(3)OH (3) and [mer-RuCl(3)(acv)(DMSO-S)(H(2)O)].H(2)O (4) on tumour cells appear to be very similar to that of NAMI-A (NAMI-A=[ImH][trans-RuCl(4)(DMSO-S)Im]). All compounds are only weakly active on tumour cell proliferation but show an interesting proadhesive effect that suggest possible activity on tumour malignancy.

Adenocarcinoma↗

PubMed2005

Nickel (II) complexes of naphthaquinone thiosemicarbazone and semicarbazone: synthesis, structure, spectroscopy, and biological activity.

Ni(II) complexes of ortho-naphthaquinone thiosemicarbazone and semicarbazone were synthesized and spectroscopically characterized. The X-ray crystal structure of both the complexes describe a distorted octahedral coordination with two tridentate mono-deprotonated ligands. In vitro anticancer studies on MCF-7 human breast cancer cells reveal that the semicarbazone derivative along with its nickel complex is more active in the inhibition of cell proliferation than the thiosemicarbazone analogue.

Antineoplastic Agents↗