labile antitumor enediyne: Topics by WorldWideScience.org

A rationale for stabilization of oxygen-labile enzymes: application to a clostridial hydrogenase.

... The anti-tumor drugs used for these studies were: busulfan, cyclophosphamide, metho- trexate, vinblastine and 6-mercaptopurine. ...

1968-01-01

Relationship between the lability of sediment-bound metals (Cd, Cu, Zn) and their bioaccumulation in benthic invertebrates

A general procedure for stabilization of O2-labile enzymes exploiting "salting out" of oxygen from the microenvironment in the molecular layers immediately adjacent to charged surfaces of polyionic...Full Text Available

1978-08-01

British Library Electronic Table of Contents (United Kingdom)

The present study has investigated metal contamination at nine sites (10 sampling stations) from the English Channel to the Mediterranean Sea, including low level and highly contaminated sediments. Both total and labile concentrations of metals were determined in superficial sediments. The influence of different pHs was tested and metal lability at pHs encountered in the gut of invertebrates (the ragworm Nereis diversicolor, the blue mussel Mytilus edulis, the Japanese oyster Crassostrea gigas) was compared with the distribution of metals in various operationally defined geochemical fractions. Cd showed the highest lability and Cu the lowest, whereas Zn lability was intermediate. Metal concentrations were determined in bivalves at six sites and in worms at three sites. Cd in living organis...

2007-01-01

Overview of the activity of a Brucella abortus preparation, Bru-Pel.

Antitumor Activity of Noscapine in Combination with Doxorubicin in Triple Negative Breast Cancer

The properties of a nonviable, aqueous ether-extracted Brucela abortus preparation, Bru-Pel, are described. In addition to inducing a "virus-type" interferon response and protecting mice against challenge with otherwise lethal doses of Semliki Forest virus, Bru-Pel is demonstrated to have potent antitumor properties in mice. These antitumor effects appear to be mediated by an increase in nonspecific resistance similar to that seen with other experimental antitumor agents. PMID:728911

1978-11-01

Induction of an abortive and futile DNA repair process in E. coli by the antitumor DNA bifunctional intercalator, ditercalinium: role in polA in death induction.

BackgroundThe aim of this study was to investigate the anticancer activity and mechanism of action of Noscapine alone and in combination with Doxorubicin against triple negative...Full Text Available

Some properties of beta-toxin produced by Clostridium perfringens type C.

Ditercalinium, an antitumor bifunctional intercalator which forms a high affinity reversible complex with DNA, was found to be specifically cytotoxic for polA and lig7 E. coli strains. In the polA strain,...Full Text Available

1988-02-11

Dynamics of ligand substitution in labile cobalt complexes resolved by ultrafast T-jump

Purified beta-toxin from Clostridium perfringens type C was found to be a single polypeptide chain protein with a molecular weight of approximately 30,000. The toxin was heat labile, with 75% of its...Full Text Available

1978-08-01

Vitamin A Enhances Antitumor Effect of a Green Tea Polyphenol on Melanoma by Upregulating the Polyphenol Sensing Molecule 67-kDa Laminin Receptor

Ligand exchange of hydrated metal complexes is common in chemical and biological systems. Using the ultrafast T-jump, we examined this process, specifically the transformation of aqua cobalt (II) complexes...Full Text Available

2008-09-02

Treatment with LL-37 Peptide Enhances Antitumor Effects Induced by CpG Oligodeoxynucleotides Against Ovarian Cancer

BackgroundGreen tea consumption has been shown to have cancer preventive qualities. Among the constituents of green tea, (-)-Epigallocatechin-3-O-gallate (EGCG)...Full Text Available

Introduction of the CIITA gene into tumor cells produces exosomes with enhanced anti-tumor effects

AbstractThere is an urgent need for innovative therapies against ovarian cancer, one of the leading causes of death from gynecological cancers in the United States. Immunotherapy employing...Full Text Available

2009-04-01

CDC45 and DPB11 are required for processive DNA replication and resistance to DNA topoisomerase I-mediated DNA damage

Exosomes are small membrane vesicles secreted from various types of cells. Tumor-derived exosomes contain MHC class I molecules and tumor-specific antigens, receiving attention as a potential cancer...Full Text Available

2011-05-31

ANTITUMOR ACTIVITY OF HYALURONIC ACID SYNTHESIS INHIBITOR 4-METHYLUMBELLIFERONE IN PROSTATE CANCER CELLS

The antitumor agent camptothecin targets DNA topoisomerase I by reversibly stabilizing a covalent enzyme-DNA intermediate. The subsequent collision of DNA replication forks with these drug-enzyme-DNA...Full Text Available

1999-09-28

Shifts in soil organic matter composition following treatment with sodium hypochlorite and hydrofluoric acid

4-methylumbelliferone (4-MU) is a hyaluronic acid (HA) synthesis inhibitor with anticancer properties; the mechanism of its anticancer effects is unknown. We evaluated the effects of 4-MU on...Full Text Available

2010-04-01

British Library Electronic Table of Contents (United Kingdom)

A renewed interest in chemical fractionation of soil organic matter (SOM) originates from the premise that it enables to isolate labile SOM from SOM protected through mineral binding and recalcitrant SOM. Both selective removal of labile non-bound SOM through oxidation or hydrolysis as well as selective removal of minerals and attached SOM are often applied. Molecular-level SOM characterization by means of temperature resolved Pyrolysis-Field Ionization Mass Spectroscopy analysis (Py-FIMS) was used here as an approach to obtain insight into the fate of SOM upon wet chemical treatment with regard to composition and thermal stability. The applied sequential chemical treatment with 6% NaOCl and 10% HF yielded similar sizes in stable SOM fractions between sandy semi-native heathland and cultiv...

2009-01-01

Quantification of Free and Bound Fractions of Nickel in Natural Waters by Solvent Extraction with 1,2-Cyclohexanedione Bis-Benzoyl-Hydrazone

British Library Electronic Table of Contents (United Kingdom)

An hydrazone derivative, 1,2-cyclohexanedione bis-benzoyl-hydrazone (1,2-CHBBH), has been used as a selective reagent for an advanced environmental application consisting of separating the different species of nickel in natural waters by solvent extraction. The effects of pH and reagent concentration on the extraction process were studied, as well as the influence of both organic (humic acids) and inorganic ligands (Cl-). Under natural conditions, organic and inorganic nickel species presented different extraction behaviors, and the variations in extraction yields could be correlated with the concentrations of organic complexes in the samples, allowing the separation of labile and non-labile nickel species in both fresh and marine waters.

2010-01-01

1 2 3 4

Distribution of Indole-3-Acetic Acid and the Occurrence of Its Alkali-Labile Conjugates in the Extraxylary Region of Pinus sylvestris Stems ¹

Cesium ion desorption ionization with Fourier transform mass spectrometry

Free and conjugated indole-3-acetic acid (IAA) were measured by quantitative gas chromatography-selected ion monitoringmass spectrometry in the extraxylary region of the stem of large Pinus...Full Text Available

1990-08-01

Preferential antitumor effect of the Src inhibitor dasatinib associated with a decreased proportion of aldehyde dehydrogenase 1-positive cells in breast cancer cells of the basal B subtype

Cesium ions (Cs"+) are used for the production of the feed ions necessary to obtain Fourier transform mass spectra (FTMS). The molecule chosen for the initial study of this Cs"+ desorption ionization (DI-FTMS) was vitamin B-12 because of its nonvolatile, thermally labile character. 21 references.

Interferon-? Targets Cancer Cells and Osteoclasts to Prevent Tumor-associated Bone Loss and Bone Metastases*S?

BackgroundRecent studies have suggested that the Src inhibitor dasatinib preferentially inhibits the growth of breast cancer cells of the basal-like subtype. To clarify this finding...Full Text Available

Enhanced anti-tumor effects of combined MDR1 RNA interference and human sodium/iodide symporter (NIS) radioiodine gene therapy using an adenoviral system in a colon cancer model

Interferon-γ (IFN-γ) has been shown to enhance anti-tumor immunity and inhibit the formation of bone-resorbing osteoclasts. We evaluated the role of IFN-γ in bone metastases,...Full Text Available

2009-02-13

Decreased 7,12-dimethylbenz[a]anthracene-induced carcinogenesis coincides with the induction of antitumor immunities in adult female B6C3F1 mice pretreated with genistein

Using an adenoviral system as a delivery mediator of therapeutic gene, we investigated the therapeutic effects of the use of combined MDR1 shRNA and human NIS (hNIS)...Full Text Available

2010-07-01

Genome lability in radiation-induced transformants of C3H 10T1/2 mouse fibroblasts

The objective of this study was to determine if genistein (GEN) modulation of the immune responses might contribute to the increased host resistances to tumors. A time-course study was performed...Full Text Available

2007-12-01

Uptake of atmospheric tritium by market foods

We have been investigating radiation-induced neoplastic transformants of C3H 10T1/2 mouse fibroblasts for evidence of heritable changes. C3H 10T1/2 cells were treated with 8 Gy X rays. After approximately 8 weeks of culture, type II/III foci were isolated from the monolayer using cloning rings. Cell lines developed from these foci, and clones established from these cell lines, were examined for DNA content. The isolated focus-derived populations and derived clones often display aneuploidy and/or polyploidization. In one instance a clone (derived from a single cell) displayed multiple polyploidies. During passage the ploidy of many of the anomalous populations gradually reverted to the ploidy of the non-neoplastically transformed state. The morphological features associated with the neoplastic transformation event were nevertheless retained. The results demonstrate that exposure to radiation can induce, in association with morphological neoplastic transformation, a heritable, ...

1994-04-01

Thermally cleavable surfactants

In this paper uptake of tritium by market foods from tritiated water vapor in the air is investigated using cereals and beans purchased in Deep River, Canada. The concentrations of tissue free water tritium (TFWT) and organically bound tritium (OBT) range from 12 to 79% and from 10 to 38% respectively, of that estimated for atmospheric water vapor of the sampling month. The specific activity ratios of OBT to TFWT were constant for cereals, but variable for beans. The elevated OBT was shown to be the result of isotopic exchange of labile hydrogen by the fact that washing the foods with tritium free-water reduced their tritium contents to levels characteristic of their production sites.

1992-03-01

Thermally cleavable surfactants

Two new surfactant molecules are reported which contain thermally labile Diels-Alder adducts connecting the polar and non-polar sections of each molecule. The two surfactants possess identical non-polar dodecyl tail segments but exhibit different polar headgroups. The surfactants become soluble in water when anionic salts are formed through the deprotonation of the surfactant headgroups by the addition of potassium hydroxide. When either surfactant is exposed to temperature above about 60.degree. C., the retro Diels-Alder reaction occurs, yielding hydrophilic and hydrophobic fragments or the aqueous solutions of the surfactants subsequently exhibit loss of all surface-active behavior.

2009-09-29

Thermally cleavable surfactants

2009-11-24

Status of bismuth and lead for radioimmunoimaging and therapy

Two new surfactant molecules are reported which contain thermally labile Diels-Alder adducts connecting the polar and non-polar sections of each molecule. The two surfactants possess identical non-polar dodecyl tail segments but exhibit different polar headgroups. The surfactants become soluble in water when anionic salts are formed through the deprotonation of the surfactant headgroups by the addition of potassium hydroxide. When either surfactant is exposed to temperature above about 60.degree. C., the retro Diels-Alder reaction occurs, yielding hydrophilic and hydrophobic fragments and the aqueous solutions of the surfactants subsequently exhibit loss of all surface-active behavior.

2006-04-04

Radioiodinated 2-nitrobenzyl carbamates as bioreductive alkylating agents for tissue hypoxia

Of the radionuclides with physical properties most suited for use with monoclonal antibody for tumor imaging or therapy, few are more available or desirable than Pb-203, 212 and Bi-212. Yet no clinical studies have as yet been possible solely due to the lability in vivo of known complexes. We now report that bismuth complexes of the ligands p-SCN-Bz-DOTA and p-SCN-Bz-trans-cyclohexylDTPA are effective at protecting Bi-206 from release when linked to immunoproteins. Practicable, efficient ligand syntheses will be reported. Initial studies reveal that antibody is labeled efficiently with radiolead DOTA complexes. Preliminary studies indicate stability in vivo.

1990-08-26

British Library Electronic Table of Contents (United Kingdom)

Three N-methylcarbamates of iodonitrobenzyl alcohols (4-iodo-2-nitrobenzyl alcohol 2, 5-iodo-2-nitrobenzyl alcohol 3 and 4-iodo-2,6-dinitrobenzyl alcohol 4) bearing [[sup 125]I] have been prepared and characterized for their lipophilicity, their reduction potentials and the in vivo lability of the radioiodine in healthy mice. Based upon these results, 2 and 4 were tested in tumor-bearing mice showing limited uptake of radioactivity in tumours and a tumor-to-blood ratio of less than 1. Consequently these particular carbamates are not satisfactory as hypoxia imaging agents. (author).

1993-05-01

Cleavable surfactants

The review covers the development within the field of cleavable surfactants since 2003. Cleavable surfactants are amphiphiles in which a weak linkage has been deliberately inserted, normally, but not always, between the hydrophobic tail and the polar headgroup. Alkali labile linkages that have been used for the purpose include normal ester bonds, betaine esters, and carbonates. Ketals and ortho esters are example of bonds that are susceptible to acid hydrolysis. Several investigations deal with cationic ester-containing surfactants, both monomeric and dimeric species, the latter being gemini surfactants. Ester, amide and carbonate containing surfactants have been investigated with respect to enzyme catalyzed hydrolysis. The main incentive for the development of novel cleavable surfactants ...

2007-01-01

Stereospecific ligands and their complexes. Part VII. Synthesis, characterization and in vitro antitumoral activity of platinum(II) complexes with O,Oprime-dialkyl esters of (S,S)-ethylenediamine-N,Nprime-di-2-(4-methyl)pentanoic acid

British Library Electronic Table of Contents (United Kingdom)

Platinum(II) complexes (1-4) with bidentate N,Nprime-ligands, O,Oprime-dialkyl esters (alkyl = ethyl, n-propyl, n-butyl and n-pentyl), of (S,S)-ethylenediamine-N,Nprime-di-2-(4-methyl)pentanoic acid were synthesized and characterized by IR, 1H NMR and 13C NMR spectroscopy and elemental analysis. DFT calculations were performed for the complexes and it was found that only one diastereoisomer could be formed. Cytotoxic activity of complexes 1-4 was determined against chronic lymphocytic leukemia cells (CLL) and compared to the activity of ligand precursors L12HCl-L42HCl and corresponding palladium(II) complexes, [PdCl2L] (L = L1-L4). The complexes were found to exhibit significantly higher antitumor activities than cisplatin on CLL cells. Cytotoxic effect of platinum(II) complexes on CLL cel...

2011-01-01

Biophysical analysis of DNA modified by 1,2-diaminocyclohexane platinum(II) complexes

GC-MS investigation and toxicological evaluation of alkaloids from Leptadenia pyrotechnica

Modification of DNA and double-stranded deoxyoligonucleotides with antitumor 1,2-diamino-cyclohexanedinitroplatinum(II) (Pt-dach) complexes was investigated with the aid of physico-chemical methods and chemical probes of nucleic acid conformation. The three Pt-dach complexes were used which differed in isomeric forms of the dach non-leaving ligand-Pt(1R,2R-dach), Pt(1S,2S-dach) and Pt(1R,2S-dach) complexes. The latter complex has lower antitumor activity than the other two Pt-dach complexes. Pt(1R,2S-dach) complex exhibits the slowest kinetics of its binding to DNA and of the conversion of monofunctional binding to bifunctional lesions. The anomalously slow electrophoretic mobility of multimers of the platinated and ligated oligomers suggests that bifunctional binding of Pt-dach complexes to a d(GG) site within double-stranded oligonucleotides induces bending of the oligomer. It is proposed that different effects of the Pt-dach complexes on DNA ...

1992-01-25

British Library Electronic Table of Contents (United Kingdom)

GC-MS analysis of isolated alkaloids from aerial parts of Leptadenia pyrotechnica (Forsk.) Decne (Asclepiadaceae) was performed. Twenty-four alkaloids and six simple amines were detected for the first time in this plant. Almost all of the alkaloids belonged to pyridine, pyrrole, pyrazine, and indole types. The acute LC50 of the total alkaloids and alcohol extracts estimated by means of brine shrimp toxicity test were 63.09 and 11.89 ppm, respectively. The antitumor activities of these extracts, using potato disc screen, showed good activity represented by -33.6% and -49.3%, respectively.

2009-01-01

Theoretical study on antitumor activity of palladium(II) and platinum(II) complexes with isoxazole and its derivatives

Improved therapeutic efficacy against murine carcinoma by combining honokiol with gene therapy of PNAS-4, a novel pro-apoptotic gene.

The palladium(II) and platinum(II)complexes(where, (M(L){sub 2}X{sub 2}), M=Pd(II), Pt(II); L=isoxazole (isox), 3, 5-dimethylisoxazole(3, 5-diMeisox), 3-methyl, 5-phenylisoxazole(3-Me, 5-Ph-isox), and 4-amino-3, 5-di-methylisoxazole (4-ADI); X=Cl, Br) with isoxazole and its derivatives were investigated on antitumor activity by MM2 and EHMO calculation. Because for all the complexes the {sigma}MO energy level (E{sub {sigma}}{sub (M-X)} between d{sub x}{sup 2}{sub -y}{sup 2} orbital of central metal and p{sub x} orbital of halogen atom is less than {sigma}MO energy level E{sub {sigma}}{sub (M-N)} between d{sub x}{sup 2}{sub -y}{sup 2} orbital of central metal and p{sub x} orbital of N atom, without exception. And judging, from the lower E{sub {sigma}}{sub (M-X)} value in trans, the bonding strength was found to be weaker in trans isomer than in cis. For the Pd(II) and Pt(II) complexes which have planar ligands, it was shown that for all the complexes dissociation of ...

1998-02-01

Antitumor activity of platinum(II) complexes with histamine and radioiodinated histamine in a transplantable murine adenocarcinoma model

PNAS-4, a novel pro-apoptotic gene activated during the early response to DNA damage, can inhibit proliferation via apoptosis when overexpressed in some tumor cells. Recent studies have indicated that honokiol can induce apoptosis, inhibit angiogenesis, and suppress tumor growth. In the present study, we investigated whether mouse PNAS-4 (mPNAS-4) could augment the apoptosis of tumor cells induced by honokiol in vitro, and whether the antiangiogenic activity of honokiol and induction of apoptosis by mPNAS-4 could work cooperatively to improve the antitumor efficacy in vivo. In vitro, mPNAS-4 inhibited proliferation of murine colorectal carcinoma CT26 and Lewis lung carcinoma LL2 cells through induction of apoptosis, and significantly augmented the apoptosis of CT26 and LL2 cells induced by honokiol. Compared with treatment with mPNAS-4 or honokiol alone, in vivo systemic administration of an expression plasmid encoding mPNAS-4 and low-dose honokiol significantly ...

2009-06-04

The utilization of polysaccharides by heterotrophic bacterioplankton in the Bay of Biscay (North Atlantic Ocean)

Purpose: Antitumor activity of the dichloroplatinum(II)-histamine complexes labeled with I-125 or I-131 was investigated in a transplantable murine adenocarcinoma (MA) model. Methods: The tumor model was obtained in C3H/W female mice after subcutaneous inoculation of the tumor cells derived from the mice bearing a mammary tumor of spontaneous origin. Antitumor activities of the platinum-histamine complexes were investigated in three independent experiments, which differed in applied doses of preparations (PtCl{sub 2}Hist, PtCl{sub 2}[{sup 125}I]Hist, PtCl{sub 2}[{sup 131}I]Hist, PtCl{sub 2}Hist/PtCl{sub 2}[{sup 125}I]Hist and PtCl{sub 2}Hist/PtCl{sub 2}[{sup 131}I]Hist), treatment schedules as well as stages of the disease progress in the animals used. Experiment 1 included long-term, multidose treatment with low single doses (treatment duration 31-32 days; 8-10 doses of ca. 0.25{center_dot}MTD{sub Pt} each). Experiment 2 included short-term, ...

2008-07-15

1 2 3 4

British Library Electronic Table of Contents (United Kingdom)

This study investigates the turnover of polysaccharides by heterotrophic bacterioplankton in the northern Bay of Biscay, a productive marine system on the continental margin of the temperate Atlantic Ocean. Bacterial biomass production (BBP) near the surface ranged from 0.5 to 25.7 nmol C L?1 h?1 during small phytoplankton blooms in May and June that occurred after the main spring bloom. A direct relationship between BBP and total polysaccharides strongly suggests the dependence of bacterial growth on the availability of semi-labile organic matter. Concentrations of combined glucose as well as rate constants of extracellular glucosidase activity and glucose uptake were determined to estimate the actual carbon fluxes from bacterial polysaccharide turnover. Results reveal that ...

2011-01-01

Synthetic enantiopure aziridinomitosenes: preparation, reactivity, and DNA alkylation studies.

Empirical tests of life-history evolution theory using phylogenetic analysis of plant demography

An enantiocontrolled route to aziridinomitosenes had been developed from l-serine methyl ester hydrochloride. The tetracyclic target ring system was assembled by an internal azomethine ylide cycloaddition reaction based on silver ion-assisted intramolecular oxazole alkylation and cyanide-induced ylide generation via a labile oxazoline intermediate (62 to 66). Other key steps include reductive detritylation of 26, methylation of the N-H aziridine 56, oxidation of the sensitive cyclohexenedione 68 to quinone 70, and carbamoylation using Fmoc-NCO. Although the aziridinomitosene tetracycle is sensitive, a range of protecting group manipulations and redox chemistry can be performed if suitable precautions are taken. A study of DNA alkylation by the first C-6,C-7-unsubstituted aziridinomitosene 11a has been carried out, and evidence for DNA cross-link formation involving nucleophilic addition to the quinone subunit is described. PMID:14677970

2003-12-24

British Library Electronic Table of Contents (United Kingdom)

Summary 1. A primary goal of evolutionary ecology is to understand factors selecting for the diversity of life histories. Life-history components, such as time-to-reproduction, adult survivorship and fecundity, might differ among species because of variation in direct and indirect benefits of these life histories in different environments or might have lower-than-expected variability because of phylogenetic constraints. Here, we present a phylogenetic examination of demography and life histories using a data base of 204 terrestrial plant species. 2. Overall, statistical models without phylogeny were preferred to models with phylogeny for vital rates and elasticities, suggesting that they lacked phylogenetic signal and are evolutionarily labile. However, the effect of phylogeny was signific...

2010-01-01

Fate of corrosion products released from stainless steel in marine sediments and seawater. Part 3. Calcareous ooze

Vitiligo during Treatment of Crohn's Disease with Adalimumab: Adverse Effect or Co-Occurrence?

The physicochemical forms and partitioning of corrosion products released from stainless steel upon exposure to selected environmental conditions is the subject of this investigation. This report describes the influence of calcareous sediment on the rate of release and fate of corrosion products produced when neutron-activated stainless steel specimens were exposed to a Globigerina ooze taken from the Northeast Pacific Ocean. The calcareous ooze used in this study consists largely of planktonic formanifera tests and was found to be about 90% CaCO_3. The trace metal content of this sediment was typical of average deep-sea carbonate sediments, and the ratios of trace elements to Ti were not remarkably different from a coastal clayey silt or a Northeast Pacific pelagic red clay. Most (>80%) of the trace metals extracted by sequential chemical treatment were associated with reductant-soluble materials, i.e., amorphous Mn and Fe oxides, or were incorporated in the carbonate substrate. ...

British Library Electronic Table of Contents (United Kingdom)

Abstract Adalimumab is a fully human monoclonal anti-tumor necrosis factor-a agent that is approved for the treatment of Crohn's disease. It has a good safety profile, injection site reactions being the most common adverse effect. We report a case of a 54-year-old woman with a 30-year history of Crohn's disease who developed achromic patches on the trunk and upper extremities after initiating treatment with adalimumab. Cutaneous biopsy confirmed diagnosis of vitiligo and laboratory testing ruled out thyroid disease. Concomitant occurrence of vitiligo and inflammatory bowel disease, although rare, has been described. A common autoimmune basis could explain this fact. Moreover, multiple cutaneous adverse effects have been described in the literature secondary to biologic treatments, includin...

2011-01-01

Proteomic analysis of apoptosis induction in human lung cancer cells by recombinant MVL

British Library Electronic Table of Contents (United Kingdom)

Lung cancer is still difficult to treat by current chemotherapeutic procedures. We recently found that MVL, an anti-HIV lectin from blue-green algae Microcystis viridis, also has antitumor activity. The objective of this study was to investigate apoptosis-inducing activity of recombinant MVL (R-MVL) and proteomic changes in A549 cells, and to identify the molecular pathways responsible for the anti-cancer action of R-MVL. We found that R-MVL induces A549 cells apoptosis in a dose-dependent manner by using MTT assay, fluorescent microscope (FM) and flow cytometry (FCM), and the IC50 was calculated to be 24.12??g/ml. Subsequently, 7 altered proteins in R-MVL-treated A549 cells were identified, including upregulated aldehyde dehydrogenase 1 and ?-actin, and five downregulated proteins: heat s...

2011-01-01

Possible association of lower rate of postherpetic neuralgia in patients on anti-tumor necrosis factor-

British Library Electronic Table of Contents (United Kingdom)

Abstract Recently, a study of patients with rheumatoid arthritis who developed herpes zoster while taking a tumor necrosis factor (TNF)- inhibitor reported a decreased incidence of postherpetic neuralgia. The objective of this study was to investigate whether patients on TNF- inhibitors who developed herpes zoster have a lower incidence of subsequent development of postherpetic neuralgia. A retrospective review of herpes zoster patients on TNF- inhibitors (infliximab, etanercept, or adalimumab) was conducted in 12 dermatology clinics. Medical records of such patients were reviewed thoroughly to confirm herpes zoster and TNF- inhibitors and any subsequent development of postherpetic neuralgia (pain score -3 out of 10 after 90 days of shingles onset) was noted. A total of 206 cases were revi...

2011-01-01

Ligand Tuning in Asymmetric Hydrovinylation of 1,3-Dienes. A Stereoselective Route to either Steroid-C20 (S) or -C20 (R) Derivatives

Correlation of Multislice CT and Histomorphology in HCC Following TACE: Predictors of Outcome

1,3-Dienes derived from steroidal D-ring C17-ketones undergo Ni(II)-catalyzed hydrovinylation to give 1,2- or 1,4-addition of ethylene. Using finely tuned phosphoramidite ligands it is possible to synthesize either the C20 (R)- or the C20 (S)-derivatives without mutual contamination. The proportion of the 1,4-adduct, which is also formed stereoselectively, can be minimized by optimizing the reaction conditions. Since the two alkenes in the resultant dienes have differing steric demands for many potential reactions, and are ideally juxtaposed for further D-ring functionalization, these intermediates could be useful for the preparation of biologically important compounds such as vitamin D analogs and various antitumor steroidal glycosides.

2008-06-21

Antitumor and Antiviral Activity of Colombian Medicinal Plant Extracts

The purpose of this study was to correlate histopathological with CT findings in patients suffering from hepatocellular carcinoma (HCC) eligible for orthotopic liver transplantation (OLT), with a special focus on the antitumoral effect of transarterial chemoembolization (TACE) therapy. A total of 42 consecutive patients suffering from HCC had been treated prior to OLT by means of TACE. TACE was carried out with a mixture of Lipiodol (10-20 ml) and mitomycin C (max. dosage, 10 mg). TACE was performed at 6- to 8-week intervals. Follow-up investigation included contrast-enhanced multislice CT controls and laboratory control. Liver explants were evaluated macroscopically and microscopically to determine the number and size of the tumor lesions as well as the degree of tumor necrosis. Necrosis was investigated in H and E-stained sections. The degree of necrosis was classified as follows: 0-25%, 26-50%, 51-75%, 75-99%, and complete necrosis. Two hundred thirty-one TACE ...

2008-07-15

Scientific Electronic Library Online (English)

Abstract in english Extracts of nine species of plants traditionally used in Colombia for the treatment of a variety of diseases were tested in vitro for their potential antitumor (cytotoxicity) and antiherpetic activity. MTT (Tetrazolium blue) and Neutral Red colorimetric assays were used to evaluate the reduction of viability of cell cultures in presence and absence of the extracts. MTT was also used to evaluate the effects of the extracts on the lytic activity of herpes simplex virus type (more) 2 (HSV-2). The 50% cytotoxic concentration (CC50) and the 50% inhibitory concentration of the viral effect (EC50) for each extract were calculated by linear regression analysis. Extracts from Annona muricata, A. cherimolia and Rollinia membranacea, known for their cytotoxicity were used as positive controls. Likewise, acyclovir and heparin were used as positive controls of antiherpetic activity. Methanolic extract from Annona sp. on HEp-2 cells presented a CC50 value at ...

1999-07-01

Synthesis of alkylated deoxyno irimycin and 1,5-dideoxy-1,5-iminoxylitol analogues: : Polar side-chain modification, sulfonium and selenonium heteroatom variants, conformational analysis, and evaluation as glycosidase inhibitors

DEFF Research Database (Denmark)

The syntheses of N-alkylated deoxynojirimycin and 1,5-dideoxy-1,5-iminoxylitol derivatives having either a D- or an L-erythritol-3-sulfate functionalized N-substituent are reported. The alkylating agent used was a cyclic sulfate derivative, whereby selective attack of the nitrogen atom at the least hindered primary center afforded the desired ammonium salt. In aqueous solution, these salts were configurationally labile at the ammonium center. Sulfonium and/or selenonium analogues of the ammonium salts were prepared by analogous reactions. The chalcogen salts were obtained as mixtures of diastereomers, separable in some cases, differing only in the stereochemistry at the configurationally stable sulfur or selenium atoms. Proof of configuration and conformation of each compound was obtained by detailed NMR experiments. The compounds are six-membered ring analogues of salacinol, a known sulfonium-salt glucosidase inhibitor. Evaluation of the target compounds for ...

2004-01-01

Monitoring of the insecticide trichlorfon by phosphorus-31 nuclear magnetic resonance ({sup 31}P NMR) spectroscopy

Epigenomic disruption: the effects of early developmental exposures.

Trichlorfon is an organophosphorus insecticide, which is extensively being used for protection of fruit crops. Trichlorfon is a thermal labile compound, which cannot be easily determined by gas chromatography (GC) and has no suitable group for sensitive detection by high performance liquid chromatography (HPLC). In this study, a {sup 31}P nuclear magnetic resonance ({sup 31}P NMR) has been described for monitoring of trichlorfon without any separation step. The quantitative works of {sup 31}P NMR spectroscopy has been performed in the presence of an internal standard (hexamethylphosphoramide). Limit of detection (LOD) for this method has been found to be 55 mg L{sup -1}, without any sample preparation, and the linear working range was 150-5500 mg L{sup -1}. Relative standard deviation (R.S.D.%) of the method for three replicates within and between days was obtained {<=}9%. The average recovery efficiency was approximately 99-112%. This method was applied for ...

2006-08-25

Synthesis, characterization and antitumor activity study of some cyclometalated organoplatinum(II) complexes containing aromatic N-donor ligands

Through DNA methylation, histone modifications, and small regulatory RNAs the epigenome systematically controls gene expression during development, both in utero and throughout life. The epigenome is also a very reactive system; its labile nature allows it to sense and respond to environmental perturbations to ensure survival during fetal growth. This pliability can lead to aberrant epigenetic modifications that persist into later life and induce numerous disease states. Endocrine-disrupting compounds (EDCs) are ubiquitous chemicals that interfere with growth and development. Several EDCs also interfere with epigenetic programming. The investigation of the epigenotoxic effects of bisphenol A (BPA), an EDC used in the production of plastics and resins, has further raised concern over the impact of EDCs on the epigenome. Using the Agouti viable yellow (A(vy)) mouse model, dietary BPA exposure was shown to hypomethylate both the A(vy) and the Cabp(IAP) metastable ...

2010-10-01

British Library Electronic Table of Contents (United Kingdom)

A general approach has been designed to synthesize some mononuclear and binuclear cyclometalated platinum(II) complexes, containing aromatic N-donor ligands with the presence of one Cl- trans to carbon. In this way, cyclometalated platinum(II) complex [Pt(C^N)Cl(dmso)], 1, C^N = N(1),C(2prime)-chelated, deprotonated 2-phenylpyridine and dmso = dimethylsulfoxide, was used as a precursor to react with imidazole derivatives (1-methylimidazole, 2a, imidazole, 2b,), monodentate pyridine derivatives (4-methylpyridine, 2c, pyridine, 2d,) and bidentate pyridine derivative (4,4prime-bipyridine, 3 and 4,). Synthesized complexes were fully characterized by using multinuclear NMR spectroscopy (1H, 13C{1H} and 195Pt), correlation NMR spectroscopy (1H-1H COSY, 13C{1H}-1H Heteronuclear Multiple Quantum C...

2011-01-01

Synthesis and characterization of diastereomeric (substituted iminodiacetato)(1,2-diaminocyclohexane)platinum(II) complexes

Structure-activity-relationships (SAR) in pyrimidine nucleoside transport

Novel complexes of the type (Pt(DACH)(N-R-iminodiacetate)), wherein DACH represents (R,S)- and (R,R)-1,2 diaminocyclohexane and R represents /minus/Me, /minus/EtOH, and /minus/CH/sub 2/Ph groups, have been prepared, purified, and characterized by spectroscopic techniques (/sup 1/H, /sup 13/C, and /sup 195/Pt NMR;MS(FAB);IR) and by the measurement of selected physical properties (pH, pK/sub a/, conductivity, and molecular weights). The data are consistent with the formation of two diastereomeric complexes in unequal proportions in which the N-R-iminodiacetate ligand appears to be bonded as a pseudofacial tridentate chelate. One are of the ligand forms a stable five-membered-ring O,N-chelate while the other arm appears to be involved in ion-pair formation (zwitterion-like) involving the carboxylate anion and the formally positive Pt(II) central metal atom. It has been demonstrated indirectly that an active impurity was present in predictably inactive bulk complexes of the type PtN/sub ...

1988-11-16

Structure determination and investigation on cytotoxicity of potassium dichlorido(l-prolinato)platinate(II) versus chlorido(dimethyl sulfoxide)(l-prolinato)platinum(II) complex -In vitro antitumor deactivation by Cl^-/dmso ligand exchange

Several series of pyrimidine nucleosides were evaluated as part of a larger program to develop non-invasive brain imaging agents. The interaction of these antitumor/antiviral nucleosides with an NBMPR-sensitive murine erythroctye nucleoside transporter was evaluated by determining their inhibitory effect (K_i) on zero-trans influx of thymidine. Within each series of compounds, which had F, Cl, Br or I as halogen substituents, an increase in size of the halogen atom or a decrease in electronegativity decreased affinity for the transporter. Partition coefficients (P) of these pyrimidine nucleosides were measured to determine their potential to diffuse across the blood-brain-barrier (BBB). Most of the pyrimidine nucleosides had lower P values (log P < 0.9), and were considered to be poor candidates for simple diffusion across the BBB, although an active BBB transport mechanism for some nucleosides could be operative. For a given series, it was found that log P ...

British Library Electronic Table of Contents (United Kingdom)

Potassium dichlorido(l-prolinato)platinate(II), K[PtCl"2(l-pro"?"H)] (1), and chlorido(dimethyl sulfoxide)(l-prolinato)platinum(II), [PtCl(l-pro"?"H)(dmso)] (2), were synthesized by ligand substitution reactions. Both complexes were characterized by ^1H, ^1^3C, and ^1^9^5Pt NMR spectroscopy, elemental analysis, and HR-ESI-MS. The molecular structures of 1 and 2 were determined by single crystal X-ray diffraction, proving bidentate coordinated l-prolinato ligand and SP-4-4 configuration of 2a. With the help of DFT calculations stability of possible isomers of 1 and 2 was studied. A considerable difference in the in vitro cytotoxicity of 1 versus 2a (exchange of one chlorido ligand by dmso) against four human cancer cell lines was found.

2011-01-01

Morusin induces apoptosis and suppresses NF-#kappa#B activity in human colorectal cancer HT-29 cells

Liposome encapsulation of lipophilic N-alkyl-propanediamine platinum complexes: impact on their cytotoxic activity and influence of the carbon chain length

Morusin is a pure compound isolated from root bark of Morusaustralis (Moraceae). In this study, we demonstrated that morusin significantly inhibited the growth and clonogenicity of human colorectal cancer HT-29 cells. Apoptosis induced by morusin was characterized by accumulation of cells at the sub-G_1 phase, fragmentation of DNA, and condensation of chromatin. Morusin also inhibited the phosphorylation of IKK-#alpha#, IKK-#beta# and I#kappa#B-#alpha#, increased expression of I#kappa#B-#alpha#, and suppressed nuclear translocation of NF-#kappa#B and its DNA binding activity. Dephosphorylation of NF-#kappa#B upstream regulators PI3K, Akt and PDK1 was also displayed. In addition, activation of caspase-8, change of mitochondrial membrane potential, release of cytochrome c and Smac/DIABLO, and activation of caspase-9 and -3 were observed at the early time point. Downregulation in the expression of Ku70 and XIAP was exhibited afterward. Caspase-8 or wide-ranging caspase inhibitor ...

2008-07-18

Honokiol and magnolol as multifunctional antioxidative molecules for dermatologic disorders.

Antitumor platinum(II) complexes derived from N-alkyl-propanediamine differing in the length of their carbon chain (C8, C10, C12 and C14) were incorporated in liposomes and the cytotoxic activity of these formulations was evaluated against tumor (A{sub 549}, MDA-MB-231, B16-F1 and B16-F10) and non-tumor (BHK-21 and CHO) cell lines. Stable and monodisperse liposome suspensions incorporating the platinum complexes were obtained from the lipid composition consisting of distearoyl-sn-glycero-3-phosphocholine, cholesterol and 1,2-distearoyl-sn-glycero- 3-phosphoethanolamine-N-(methoxy(polyethylene glycol)-2000) at 5:3:0.3 molar ratio. The entrapment efficiency (EE%) of the platinum complexes in liposomes increased with the carbon chain length. EE% was higher than 80% in C12- and C14-derivatives. The effect of liposome encapsulation on the cytotoxic activity of the complexes was found to depend on the carbon chain length. These data indicate that the highest drug ...

2010-07-01

A DC-81-indole conjugate agent suppresses melanoma A375 cell migration partially via interrupting VEGF production and stromal cell-derived factor-1a-mediated signaling

Chinese herbs have been and still are widely used as important remedies in Oriental medicine. Over the recent years, a variety of biologically active constituents have been isolated from these sources and confirmed to have multifunctional activity in experimental studies. Honokiol is a small-molecule polyphenol isolated from the genus Magnolia. It is accompanied by other related polyphenols, including magnolol, with which it shares certain biological properties. Recently, honokiol and magnolol have been found to have anti-oxidative, anti-inflammatory, anti-tumor, and anti-microbial properties in preclinical models, without appreciable toxicity. These findings have increased interest in bringing honokiol and magnolol to the clinic as novel therapeutic agents in dermatology. In this review, the findings concerning the major mechanisms of action of honokiol and magnolol are described. Knowledge of the multiple activities of honokiol and magnolol can assist with the ...

2010-09-16

1 2 3 4

British Library Electronic Table of Contents (United Kingdom)

Pyrrolo[2,1-c][1,4]benzodiazepine (PBD) chemicals are antitumor antibiotics inhibiting nucleic acid synthesis. An indole carboxylate-PBD hybrid with six-carbon spacer structure (IN6CPBD) has been previously demonstrated to induce melanoma cell apoptosis and reduce metastasis in mouse lungs. This study aimed at investigating the efficacy of the other hybrid compound with four-carbon spacer (IN4CPBD) and elucidating its anti-metastatic mechanism. Human melanoma A375 cells with IN4CPBD treatment underwent cytotoxicity and apoptosis-associated assays. Transwell migration assay, Western blotting, and ELISA were used for mechanistic study. IN4CPBD exhibited potent melanoma cytotoxicity through interrupting G1/S cell cycle progression, increasing DNA fragmentation and hypodipoidic DNA contents, a...

2011-01-01

The (--)(/sup 3/H)dihydroalprenolol binding to rat adipocyte membranes: an explanation of curvilinear Scatchard plots and implications for quantitation of beta-adrenergic sites

Synthesis, characterization, and evaluation of a novel bifunctional chelating agent for the lead isotopes {sup 203}Pb and {sup 212}Pb

In rat adipocyte membranes, both beta-adrenergic agonists and beta-adrenergic antagonists competed with (--)(/sup 3/H)dihydroalprenolol for high affinity (KD 2-4 nM) and low capacity binding sites. The antagonists but not the agonists competed with (--)(/sup 3/H)dihydroalprenolol for lower affinity and higher capacity sites. The present studies were performed in order to characterize the adipocyte beta-adrenergic receptor and distinguish it from low affinity, higher capacity sites which were heat-labile and not stereoselective. When isoproterenol was used to define the nonspecific binding, saturation studies showed a single binding site with a capacity of approximately 100 fmol/mg membrane protein (corresponding to approximately 50,000 sites/adipocyte). Binding was saturated by 10 nM (--)(/sup 3/H)dihydroalprenolol. Approximate KD's of 204 nM were observed. Kinetic analysis of (--)(/sup 3/H)dihydroalprenolol binding provided an independent measurement of ...

1982-09-01

Synthesis, characterization, and evaluation of a novel bifunctional chelating agent for the lead isotopes "2"0"3Pb and "2"1"2Pb

Radioisotopes of Pb(II) have been of some interest in radioimmunotherapy and radioimmunoimaging (RII). However, the absence of a kinetically stable bifunctional chelating agent for Pb(II) has hampered its use for these applications. {sup 203}Pb (T{sub 1/2}=52.02 h) has application potential in RII, with a {gamma}-emission that is ideal for single photon emission computerized tomography, whereas {sup 212}Pb (T{sub 1/2}=10 h) is a source of highly cytotoxic {alpha}-particles via its decay to its {sup 212}Bi (T{sub 1/2}=60 min) daughter. The synthesis of the novel bifunctional chelating agent 2-(4-isothiocyanotobenzyl)-1,4,7,10-tetraaza-1,4,7,10-tetra-(2-carbamoyl methyl)-cyclododecane (4-NCS-Bz-TCMC) is reported herein. The Pb[TCMC]{sup 2+} complex was less labile to metal ion release than Pb[DOTA]{sup 2-} at pH 3.5 and below in isotopic exchange experiments. In addition to increased stability to Pb{sup 2+} ion release at low pH, the bifunctional TCMC ligand was ...

2000-01-01

Radiation-induced damage to DNA; Les lesions radio-induites de l'ADN

Radioisotopes of Pb(II) have been of some interest in radioimmunotherapy and radioimmunoimaging (RII). However, the absence of a kinetically stable bifunctional chelating agent for Pb(II) has hampered its use for these applications. "2"0"3Pb (T_1_/_2=52.02 h) has application potential in RII, with a #gamma#-emission that is ideal for single photon emission computerized tomography, whereas "2"1"2Pb (T_1_/_2=10 h) is a source of highly cytotoxic #alpha#-particles via its decay to its "2"1"2Bi (T_1_/_2=60 min) daughter. The synthesis of the novel bifunctional chelating agent 2-(4-isothiocyanotobenzyl)-1,4,7,10-tetraaza-1,4,7,10-tetra-(2-carbamoyl methyl)-cyclododecane (4-NCS-Bz-TCMC) is reported herein. The Pb[TCMC]"2"+ complex was less labile to metal ion release than Pb[DOTA]"2"- at pH 3.5 and below in isotopic exchange experiments. In addition to increased stability to Pb"2"+ ion release at low pH, the bifunctional TCMC ligand was found to have many other ...

2000-01-01

New atomic energy law - international and national developments. Proceedings; Neues Atomenergierecht - internationale und nationale Entwicklungen. Tagungsbericht

This short survey focuses on the main radiation-induced base lesions that have been identified within cellular DNA. For this purpose, sensitive assays that are aimed at measuring a few modifications per 10{sup 7} normal bases were set-up. In that respect high performance liquid chromatography - tandem mass spectrometry (CLHP-MS/MS) was found to be able to single out the formation of 9 oxidized nucleosides and two modified nucleo-bases out of the 70 oxidative base lesions that have been identified in model systems. As a striking result, it was found that in the DNA of {gamma}-irradiated human monocytes, the formamide-pyrimidine derivative of guanine is produced in a higher yield than the ubiquitous 8-oxo-7,8-dihydro-guanine damage, both arising from the same radical precursor. However, relatively high doses of ionizing radiation (> 20 Gy) have to be applied in order to detect an increase in the level of the damage. This is due to the low efficiency for both low and high LET ...

2002-03-01

Isolation and characterization of a novel lectin from the mushroom Armillaria luteo-virens

Two of the working sessions of the meeting were devoted to aspects of international atomic energy law; the international character of the meeting was also reflected by the home countries of the members of the panel discussion concluding the working sessions. There was substantial reason to put emphasis on the international dimension of the topics discussed. In June 1994, the Nuclear Safety Convention had been signed in Vienna by diplomatic representatives of the signatory countries, and this Convention marks a signpost in the history of international atomic energy law. At the time the meeting was held, negotiations for improving the international nuclear lability law, which had been dragging on since 1989, had come to a stalemate. The meeting offered a suitable forum for taking a scientific approach to tackle the complex problems involved in reshaping the law on nuclear safety and nuclear liability. The third working session of the meeting has been discussing ...

1995-12-31

Development of a new radiolabel (lead-203) and new chelating agents for labeling monoclonal anntibodies for imaging

From the dried fruiting bodies of the mushroom Armillaria luteo-virens, a dimeric lectin with a molecular mass of 29.4 kDa has been isolated. The purification procedure involved (NH{sub 4}){sub 2}SO{sub 4} precipitation, ion exchange chromatography on DEAE-cellulose, CM-cellulose, and Q-Sepharose, and gel filtration by fast protein liquid chromatography on Superdex 75. The hemagglutinating activity of the lectin could not be inhibited by simple sugars but was inhibited by the polysaccharide inulin. The activity was stable up to 70 {sup o}C but was acid- and alkali-labile. Salts including FeCl{sub 3}, AlCl{sub 3}, and ZnCl{sub 2} inhibited the activity whereas MgCl{sub 2}, MnCl{sub 2}, and CaCl{sub 2} did not. The lectin stimulated mitogenic response of mouse splenocytes with the maximal response achieved by 1 {mu}M lectin. Proliferation of tumor cells including MBL2 cells, HeLa cells, and L1210 cells was inhibited by the lectin with an IC{sub 5} of 2.5, 5, and 10 ...

2006-07-14

DOC, Color and Disinfection By-Product Precursor Dynamics along an Urbanization Gradient, Croton Water Supply System, New York, USA

High liver uptake and slow body clearance presently limit the usefulness of "1"1"1In labeled antibodies for tumor imaging. We have investigated "2"0"3Pb as an alternate and better antibody label. The DTPA and cyclohexyl EDTA (CDTA) conjugates of an anticolon carcinoma antibody, 17-1A were labeled (bicyclic anhydride method) with "2"0"3Pb and "1"1"1In with 60 and 90% labeling yields, respectively. The biodistribution of "2"0"3Pb-17-1A conjugates was compared with the corresponding "1"1"1In-labeled preparations and with "2"0"3Pb-DTPA, "2"0"3Pb-nitrate and nonrelevant antibody controls in normal and human tumor (SW948) xenografted nude mice at 24, and 96 hr. Lead-203-labeled CDTA and DTPA antibody conjugates gave similar in vivo distributions. Even though the lead bound to these chelate-antibody conjugates was more labile in serum and in vivo, compared to indium, it cleared much faster from the liver and the whole body. A new series of chelating agents based on the ...

1988-05-22

An investigation of some Turkish herbal medicines in Salmonella typhimurium and in the COMET assay in human lymphocytes.

Hydrologic processes in suburban watersheds and their effects on water quality warrant investigation. Biweekly and storm samples were collected and analyzed for base cations, selected anions, and DOC over a one-year period at the outlet of three small (37 - 55 ha) watersheds (one forested, two with different degrees of suburban development) in the Croton Watershed, southeastern New York. Less frequent sampling for Pt/Co color and disinfection by-product precursors (DBPs) were also conducted. Median baseflow concentrations (>3 days since rainfall) of DOC were similar, ranging from 2.1 to 1.8 to 1.7 mg L -1 for the most urbanized to the forested watershed, respectively. On a unit area load basis (kg ha-1 yr-1), the range was from 8.9 to 6.4 to 5.1, again from most urbanized to forested watershed. All three watersheds showed similar storm responses, with evidence for a flushing mechanism in that DOC concentration increased with increasing discharge. Pt/Co color and DBPs (determined as ...

2005-05-01

Synthesis, structure, and antitumor activity of novel platinum(II) complexes involving asymmetric chiral diamines as carrier ligands

Medicinal plants play a major role in the life of Turkish people and of late medicinal plant usage has increased in many countries. Green plants in general contain mutagenic and carcinogenic substances, but there is little information about the biological activities of herbal medicine. In the present study, therefore, various Turkish medicinal herbs were investigated for their genotoxic potential in the Salmonella typhimurium microsomal activation assay and the alkaline single cell gel electrophoresis (COMET) assay. Extracts from these medicinal herbs and some fractions of these extracts were examined. The species investigated were Arctium minus, Ecballium elatterium, Momordica charantia, Plantago major, Urtica dioica, Viscum album, Salvia triloba, Euphorbia rigida, Stachys lavandulifolia, Acteoside, Abies nordmannia. They are used for various immune disorders and are applied either topically or taken orally as a herbal tea. Of the 19 samples of the extracts and fractions investigated, ...

1996-01-01

Structure-function studies on inhibitory activity of Bungarus multicinctus protease inhibitor-like protein on matrix metalloprotease-2, and invasion and migration of human neuroblastoma SK-N-SH cells.

New platinum(II) complexes with asymmetrically substituted chiral diamine ligands A{sub 2}PtX{sub 2}, (A{sub 2}=NH{sub 2}CH(CH{sub 3})CH{sub 2}NH(c-C{sub 5}H{sub 9}) (apcpa), NH{sub 2}CH(CH{sub 3})CH{sub 2}NH(c-C{sub 6}H{sub 11}) (apcha); X{sub 2}=2Cl, isopropylidenmalonate (IPM), 1,1'-cyclobutandicarboxylate (CBDCA) have been synthesized and characterized by means of elemental analyses, infrared and NMR spectroscopies, and X-ray crystallography. The crystal structures of (S-apcha)Pt[CBDCA]{center_dot}3H{sub 2}O (orthorhombic, P2{sub 1}2{sub 1}2(No. 18), a=6.926(3), b=15.243(3), c=19.319(4) A, V=2039.5(10) A{sup 3}, Z=4, R=0.072) and (S-apcha)Pt[IPM]{center_dot}2.5H{sub 2}O (monoclinic, P2/c(No. 13), a=9.882(1), b=18.502(1), c=22.056(1) A, V=4032.8(5) A{sup 3}, Z=8, R=0.093) exhibit that the platinum atoms achieve a typical square planar arrangement with two nitrogen atoms in cis position and with the chiral center retained. The spectroscopic data disclose that these platinum ...

1999-12-01

Risk of malignant lymphoma in patients with inflammatory bowel diseases: A Dutch nationwide study.

In view of the findings that several Kunitz-type protein inhibitors suppress tumor invasion and metastasis, the aim of the present study is to explore whether Bungarus multicinctus protease inhibitor-like protein-2 (PILP-2) and PILP-3 exhibit anti-tumor activity. Although approximately 28% of amino acid substitutions occurred between PILP-2 and PILP-3, molecular modeling suggested that PILP-2 and PILP-3 shared similar folded structures. Unlike PILP-2, PILP-3 showed a notable activity in abolishing migration and invasion of human neuroblastoma SK-N-SH cells. The ability of PILP-3 to inhibit matrix metalloprotease-2 (MMP-2) activity was higher than that of PILP-2. Pull-down assay revealed protein-protein interaction between PILP-3 and MMP-2. In contrast to mutation on N-terminal region, replacement of amino acids at C-terminus attenuated notably the ability of PILP-3 to inhibit cell invasion, cell migration and MMP-2 activity as well as the binding capability of ...

2009-08-23

Hyperfractionated radiation therapy for incompletely resected supratentorial low-grade glioma. A phase II study

BACKGROUND: Immune suppressant medications such as thiopurines and anti-tumor necrosis factor agents are important for maintaining disease control in most patients with inflammatory bowel diseases (IBDs); however, their use has been associated with the development of malignant lymphoma. The purpose of this Dutch nationwide study was to estimate the relative risk of malignant lymphoma in IBD patients. METHODS: IBD patients who developed a lymphoma between 1997 and 2004 were identified using the Dutch National Database of PALGA. Data from confirmed cases were collected from individual hospitals, including data on Epstein-Barr virus (EBV). The age-adjusted 8-year incidence of malignant lymphoma in the Netherlands was retrieved from the Central Bureau of Statistics. RESULTS: Forty-two hospitals were visited and 285 matches evaluated in the total cohort of 17,834 IBD patients. Forty-four lymphomas were observed, resulting in a relative risk of 1.27 (95% confidence ...

2010-12-22

Designed hybrid TPR peptide targeting Hsp90 as a novel anticancer agent

Background and purpose: In order to investigate the feasibility, toxicity and antitumor efficacy of hyperfractionated radiation therapy, 37 adult patients with incompletely resected supratentorial low-grade glioma were entered into a phase II study. Materials and methods: The radiation therapy dose was 55 Gy in 50 fractions in 25 treatment days over 5 weeks to the tumor plus a 2-cm margin, with an additional 17.6 Gy given in 16 fractions in 8 treatment days over 1.5 weeks to the tumor plus a 1-cm margin, using 1.1 Gy b.i.d. fractionation with a 6 h interfraction interval. The total tumor dose was 72.6 Gy in 66 fractions in 33 treatment days over 6.5 weeks. Results: The median survival time (MST) for all 37 patients has not yet been attained, while 5- and 7-year survival rates were 75% and 69%, respectively. The median time to tumor progression (MTP) has also not yet been attained, while 5- and 7-year progression-free survival (PFS) rates were both 70%. There was no ...

1998-10-01

A novel glioblastoma cancer gene therapy using AAV-mediated long-term expression of human TERT C-terminal polypeptide.

BackgroundDespite an ever-improving understanding of the molecular biology of cancer, the treatment of most cancers has not changed dramatically in the past three decades and drugs that do not discriminate between tumor cells and normal tissues remain the mainstays of anticancer therapy. Since Hsp90 is typically involved in cell proliferation and survival, this is thought to play a key role in cancer, and Hsp90 has attracted considerable interest in recent years as a potential therapeutic target.MethodsWe focused on the interaction of Hsp90 with its cofactor protein p60/Hop, and engineered a cell-permeable peptidomimetic, termed "hybrid Antp-TPR peptide", modeled on the binding interface between the molecular chaperone Hsp90 and the TPR2A domain of Hop.ResultsIt was demonstrated that this designed hybrid Antp-TPR peptide inhibited the interaction of Hsp90 with the TPR2A domain, inducing cell death of breast, pancreatic, renal, lung, prostate, and gastric cancer cell lines in vitro. In ...

2011-01-14

Study of the inorganic constituents in different species of Casearia medicinal plant collected in distinct regions of the Atlantic Forest, SP State, Brazil; Estudo sobre os constituintes inorganicos presentes em diferentes especies da planta medicinal do genero Casearia coletadas em regioes distintas da Mata Atlantica, SP

Glioblastoma multiforme is the most aggressive form of human brain tumor, which has no effective cure. Previously, we have demonstrated that overexpression of the C-terminal fragment of the human telomerase reverse transcriptase (hTERTC27) inhibits the growth and tumorigenicity of human cervical cancer HeLa cells. In this study, the therapeutic effect and molecular mechanisms of hTERTC27-mediated cancer gene therapy were further explored in vivo in established human glioblastoma xenografts in nude mice. We showed that intratumoral injection of adeno-associated virus carrying hTERTC27 (rAAV-hTERTC27) is highly effective in reducing the growth of the subcutaneously transplanted glioblastoma tumors. Histological analyses showed that rAAV-hTERTC27 treatment leads to profound necrosis, apoptosis, infiltration of polymorphonuclear neutrophils and reduced microvessel density in the tumor samples. To study the molecular mechanism of rAAV-hTERTC27-mediated antitumor ...

2007-03-23

Water-level variations and their effects on tree growth and mortality and on the biogeochemical system at the phytoremediation demonstration site in Fort Worth, Texas, 1996-2003

The use of medicinal plants in the treatment of diseases has increased significantly in the last years, as has research concerning chemical characterization of these plants. In this study, inorganic constituents were determined in leaves and in extracts from three medicinal plant species of the Casearia genus (C. sylvestris, C. decandra and C. obliqua) collected in distinct regions of the Atlantic Forest, SP. The elemental compositions of the soils in which these plants were grown were also determined. Traditionally, these plants are used due to their antiinflammatory, antiacid, antiseptic and cicatrizing properties. The antiulcer and the antitumor activities of the Casearia genus and its capacity to neutralize snake and bee venoms, have also been scientifically confirmed. The analytical methodology used was neutron activation analysis. Long and short irradiation periods of the samples and the standards were carried out at IPEN's IEA-R1 nuclear research ...

2006-07-01