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Cytostatic Activity (cytostatic + activity)
Selected AbstractsSynthesis and Cytostatic Activity of 4-Substituted Derivatives of Isoxazolyltriazenes.CHEMINFORM, Issue 49 2003E. Wagner Abstract For Abstract see ChemInform Abstract in Full Text. [source] Chemical composition and biological activities of the essential oils of Salvia canariensisFLAVOUR AND FRAGRANCE JOURNAL, Issue 1 2006M. C. García Vallejo Abstract Comparative studies of the chemical composition of steam-distilled essential oils from cultivated Salvia canariensis, collected at different seasons of the year, were studied. The essential oils were analysed by gas chomatography,mass spectrometry: the major components were bornyl acetate (17.8,28.6%), , -caryophyllene (12.7,30.2%), , -pinene (4.6,9.5%) and viridiflorol (13.9,17.3%) in all samples. The essential oils were evaluated for antimicrobial and cytostatic activities and enzymatic inhibitions of xanthine oxidase, , -glucosidase and , -glucuronidase. Concerning the antimicrobial and cytotoxic tests, the oils showed interesting activities towards different Gram-positive bacteria (MIC 45,35 µg[sol ]ml), but had no effect against eukaryotic cells. Copyright © 2005 John Wiley & Sons, Ltd. [source] Synthesis, Characterization and in Vitro Study of the Cytostatic and Antiviral Activity of New Polymeric Silver(I) Complexes with Ribbon Structures Derived from the Conjugated Heterocyclic Thioamide 2-Mercapto-3,4,5,6-tetra- hydropyrimidineEUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 7 2004Panagiotis C. Zachariadis Abstract Silver(I) bromide reacts with 2-mercapto-3,4,5,6-tetrahydropyrimidine (StpmH2, C4H8N2S) in DMSO with an excess of triethylamine to give a water-insoluble complex of formula [Ag6(,2 -Br)6(,2 -StpmH2)4(,3 -StpmH2)2]n (1), while the reaction of silver(I) nitrate with StpmH2 under the same conditions gives a water-insoluble complex of formula [{Ag4(,2 -StpmH2)6}(NO3)4]n (2). The products were characterized by elemental analyses, and FT-IR far-IR, UV/Vis, 1H and 13C NMR spectroscopy. Crystal structures of complexes 1 and 2 were determined by X-ray diffraction. Complex 1, C24H48Ag6N12S6, crystallizes in the triclinic system space group P , a = 8.041(1) Å, b = 12.838(4) Å, c = 13.281(2) Å, , = 68.40(1)°, , = 72.97(1)°, , = 87.80(2), Z = 2, forming a one-dimensional infinite ribbon structure by strong interatomic interactions of two ,2 -Br bonds with Ag(1). Complex 2, C24H48Ag4N16O12S6, crystallizes in the orthorhombic system, space group Cmc21, and a = 32.148(3) Å, b = 9.461(2) Å, c = 7.234(1) Å, , = , = , = 90°, Z = 8, forming infinite Ag,S,Ag chains which are bridged to each other by a sulfur atom of ,2 -StpmH2 ligands. Complexes 1 and 2 were studied for their cytostatic activity against murine leukemia (L1210) and human T-lymphocyte (Molt4/C8 and CEM) cells and for their antiviral activity against a wide variety of viruses. They are markedly cytostatic at 50% inhibitory concentration (IC50) values ranging from 3 to 17 ,g/mL. None of the compounds showed appreciable antiviral activity at subtoxic concentrations. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004) [source] Enhanced maturation and functional capacity of monocyte-derived immature dendritic cells by the synthetic immunomodulator MurabutideIMMUNOLOGY, Issue 4 2001Vincent Vidal Summary Murabutide is a safe synthetic immunomodulator derived from muramyl dipeptide, the smallest bioactive unit of bacterial peptidoglycan. Although it is well known that muramyl peptides modulate the functions of monocytes/macrophages, their activity on dendritic cells is poorly documented. We thus investigated the effects of Murabutide on immunophenotype, endocytosis, T-cell stimulatory capacity, and cytokine secretion of human monocyte-derived immature dendritic cells (iDCs). We found that Murabutide triggers immunophenotypic changes as upon treatment, iDCs up-regulate the surface expression of the major histocompatibility complex type II molecule human leucocyte antigen-DR, the co-stimulatory molecules CD80, CD86 and CD40 and the differentiation marker CD83, and down-regulate the expression of the mannose receptor. These phenotypic changes are also mirrored by changes in their biological activity. Subsequent to treatment with the synthetic immunomodulator, DC have a decreased endocytic capacity but exhibit enhanced stimulatory capacity for both allogeneic and autologous T cells. In addition, Murabutide-stimulated iDCs have a greater cytostatic activity toward the tumour cell line THP-1. Furthermore, in the presence of Murabutide, DCs transiently increased the release of macrophage inhibitory protein-1,, tumour necrosis factor-, and interleukin-10, whereas the enhanced production of macrophage-colony stimulating factor was sustained over the 3-day period analysed. In addition, Murabutide triggers the phosphorylation of the three classes of mitogen-activated protein kinases in iDCs. Altogether our results demonstrate that Murabutide triggers the maturation and activation of monocyte-derived iDCs. As this immunomodulator is approved for administration in humans, it could be a useful adjunct to boost the efficacy of DC-based vaccines designed against tumours or virus-infected cells. [source] Insecticidal activity of the pyrimidine nucleoside analogue (E)-5-(2-bromovinyl)-2,-deoxyuridine (BVDU)PEST MANAGEMENT SCIENCE (FORMERLY: PESTICIDE SCIENCE), Issue 8 2005Dr Michael Breuer Abstract The insecticidal activity of the antiherpetic agent (E)-5-(2-bromovinyl)-2,-deoxyuridine (BVDU) was assessed in in vivo assays against the fall armyworm, Spodoptera frugiperda (JE Smith) (Lepidoptera, Noctuidae). BVDU, mixed into an artificial diet, caused a variety of effects, depending on the concentration used. Compared with controls, food intake was lower, larval growth was retarded and larval development was prolonged. The treated larvae formed smaller pupae and the hatching moths often showed morphogenetic defects. A higher mortality could be found in larval and pupal stages and was generally caused by moult disruption. A choice assay showed that BVDU has very slight feeding-deterrent properties, which only partly explain the toxic effects. The agent most probably acts through its cytostatic activity that has been described previously using cell lines of different insect species. Copyright © 2005 Society of Chemical Industry [source] Docetaxel,ST1481 sequence exerts a potent cytotoxic activity on hormone-resistant prostate cancer cells by reducing drug resistance-related gene expressionTHE PROSTATE, Issue 2 2010Francesco Fabbri Abstract BACKGROUND The efficacy of current therapy for hormone-refractory prostate cancer is still unsatisfactory and new agents and therapeutic modalities are needed. The aims of the present work were to examine the in vitro activity and mechanisms of action of different antitumor drug combinations in hormone-resistant prostate cancer (HRPC) cell lines. METHODS The activity of docetaxel (Doc), cisplatin (Cis), oxaliplatin (Oxa), SN-38 and ST1481, singly or in combination, was assessed in different HRPC cell lines (PC3, parental DU145 and taxane-resistant DU145-R) by SRB test. Apoptosis was evaluated by TUNEL and ANN-V assays. Extrusion pump activity was studied by Hoechst 33342 assay, while gene expression related to drug efflux mechanisms and DNA damage repair was analyzed by RT-PCR. RESULTS Doc induced a high cytocidal effect in the HRPC cells, whereas Cis, Oxa, SN-38 and ST1481 exerted prevalently cytostatic activity. Doc followed by ST1481 proved to be the most effective drug sequence among those investigated, producing an important synergistic effect (R.I. from 2.0 to 5.2) in all the tested cell lines. Moreover, this sequence induced a significant downregulation of xenobiotic extrusion pump and DNA damage repair gene expression. ST1481 synergistically increased the cytocidal effect of Doc, probably through a downregulation of extrusion pump activity and DNA damage repair-related genes. CONCLUSIONS Our results show that the Doc,,,ST1481 sequence effectively reduces the cancer cell population and restores Doc activity in taxane-resistant HRPC, indicating its potential usefulness as first- or second-line treatment of hormone-refractory prostate cancer. Prostate 70: 219,227, 2010. ©2009 Wiley-Liss, Inc. [source] Possible involvement of phosphatidylinositol 3-kinase in the maintenance of metaphase II attest in porcine oocytes matured in vitroANIMAL SCIENCE JOURNAL, Issue 1 2010Junya ITO ABSTRACT It has been reported that phosphatidylinositol 3-kinase (PI3K)-protein kinase B (PKB) pathway plays a crucial role in the meiotic resumption and progression to the metaphase II (MII) stage of oocytes. However, the role of this pathway in meiotic arrest at the MII stage (cytostatic activity) is not well understood. In this study the effect of a PI3K inhibitor, LY294002, on the MAPK and p34cdc2 kinase activities of matured porcine oocytes was examined. After maturation culture, both the MAPK and p34cdc2 kinase activities in the oocytes were gradually decreased in a time-dependent manner. Although 25 µmol/L LY294002 did not affect either the MAPK or p34cdc2 kinase activities, 50 µmol/L LY294002 suppressed the PKB phosphorylation and slightly decreased MAPK activity, but not the p34cdc2 kinase activity. Therefore the effect of 10 µmol/L Ca2+ ionophore which was reported as inducing a transient decrease of p34cdc2 kinase but not MAPK activities, was also examined in LY294002-treated oocytes. By additional treatment with LY294002 after Ca2+ ionophore, both the MAPK and p34cdc2 kinase activities were decreased in a time-dependent manner, concomitantly with improvement of pronuclear formation. Therefore, we concluded that PI3K is involved in the maintenance of MAPK activity in matured porcine oocytes. [source] Synthesis, Antiviral and Cytostatic Evaluation of Unsaturated Exomethylene and Keto D -Lyxopyranonucleoside AnaloguesARCHIV DER PHARMAZIE, Issue 6 2009Niki Tzioumaki Abstract This report describes the synthesis of unsaturated exomethylene lyxopyranonucleoside analogues as potential biologically active agents. Commercially available 1,2,3,4-tetra- O -acetyl-,- D -lyxopyranose 1 was condensed with silylated thymine and uracil, respectively, deacetylated and acetalated to afford 1-(2,3- O -isopropylidene-,- D -lyxopyranosyl)thymine 4a and 1-(2,3- O -isopropylidene-,- D -lyxopyranosyl)uracil 4b. The new derivatives 1-(2,3,4-trideoxy-4-methylene-,-pent-2-enopyranosyl)thymine 8a and 1-(2,3,4-trideoxy-4-methylene-,-pent-2-enopyranosyl)uracil 8b were prepared via two different key intermediates, 7a, b and 13a, b in order to elucidate the influence of 2,,3,-unsaturation and to clarify the difference between the keto and exomethylene group on the biological activity of the target molecules. Compounds 7a, b, 8a, b, and 13a, b were evaluated for their antiviral and cytostatic activity using several virus strains and cell lines. Whereas no marked antiviral activity was noticed, 13a and 13b showed a cytostatic activity that ranged between 7 and 23 ,M for 13a and 26 and 38 ,M for 13b against murine leukemia L1210, human lymphocyte Molt4/C8 and CEM cells, and human breast carcinoma MCF7 cells. [source] | |||||||||||||