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Moderate Cytotoxicity (moderate + cytotoxicity)
Selected AbstractsSynthesis and anticancer activity of chalcogenide derivatives and platinum(II) and palladium(II) complexes derived from a polar ferrocene phosphanyl,carboxamideAPPLIED ORGANOMETALLIC CHEMISTRY, Issue 5 2010í Schulz Abstract The polar phosphanyl-carboxamide, 1,-(diphenylphosphanyl)-1-[N -(2-hydroxyethyl)carbamoyl]ferrocene (1), reacts readily with hydrogen peroxide and elemental sulfur to give the corresponding phosphane-oxide and phosphane-sulfide, respectively, and with platinum(II) and palladium(II) precursors to afford various bis(phosphane) complexes [MCl2(1 -,P)2] (M = trans -Pd, trans -Pt and cis -Pt). The anticancer activity of the compounds was evaluated in vitro with the complexes showing moderate cytotoxicities towards human ovarian cancer cells. Moreover, the biological activity was found to be strongly influenced by the stereochemistry, with trans -[PtCl2(1 -,P)2] being an order of magnitude more active than the corresponding cis isomer. Copyright © 2010 John Wiley & Sons, Ltd. [source] Cytotoxic Prenylated Phenolic Compounds from the Twig Bark of Garcinia xanthochymusCHEMISTRY & BIODIVERSITY, Issue 5 2007Quan-Bin Han Abstract Three new hydroxylated xanthones with prenyl or geranyl substituents, compounds 1,3, were isolated from the twig bark of Garcinia xanthochymus, along with the four known compounds 1,4,5,6-tetrahydroxy-7,8-diprenylxanthone (4), 1,3,5,6-tetrahydroxy-4,7,8-triprenylxanthone (5), garciniaxanthone E (6), and 6-prenylapigenin (7). Their structures were elucidated by extensive spectroscopic analysis, including 1D- and 2D-NMR as well as HR-MS experiments. All compounds showed moderate cytotoxicities against breast cancer (MDA-MB-435S) and lung adenocarcinoma (A549) cell lines, but lacked antifungal activity against Candida albicans. [source] Characterization by NMR Spectroscopy, X-ray Analysis and Cytotoxic Activity of the Ruthenium(II) Compounds [RuL3](PF6)2(L = 2-Phenylazopyridine or o -Tolylazopyridine) and [RuL'2L"](PF6)2(L', L" = 2-Phenylazopyridine, 2,2'-Bipyridine)EUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 13 2005Anna C. G. Hotze Abstract Tris(ligand) complexes [RuL3](PF6)2 (L = 2-phenylazopyridine or o -tolylazopyridine) and mixed ligand [RuL'2L"](PF6)2 (L' and L" are 2-phenylazopyridine or 2,2'-bipyridine) have been synthesized, structurally characterized and investigated for cytotoxic activity. These complexes are important to study the hypothesis that the compound ,-[Ru(azpy)2Cl2] (azpy = 2-phenylazopyridine) exhibits a high cytotoxicity due to its two cis chloride ligands, which might be exchanged for biological targets as DNA. Molecular structures of mer -[Ru(azpy)3](PF6)2 (1) and mer -[Ru(tazpy)3](PF6)2 (5) (tazpy = o -tolylazopyridine) have been determined by X-ray diffraction. Series of complexes [RuL3](PF6)2 and [RuL'2L"](PF6)2 show interesting NMR spectroscopic data; e.g. the spectrum of mer -[Ru(azpy)3](PF6)2 (1) shows extremely broadened resonances at room temp. but sharpened resonances at low temperature. In the 1H NMR spectra of compounds [Ru(azpy)2(bpy)]2+ and [Ru(bpy)2(azpy)]2+ (bpy = 2,2-bipyridine), respectively, less broadened (room temp.) or completely sharp resonances (room temp.) occur in comparison to 1 (under same conditions). By selecting the right temperature and/or concentration, NMR spectra of these series of compounds have been resolved using 2D COSY and NOESY NMR spectroscopy. Remarkably, the cytotoxicity data against a series of human tumor cell lines (A498, EVSA-T, H226, IGROV, M19, MCF-7 and WIDR) show a moderate cytotoxicity for these series of tris(ligand) complexes. So, even though no chloride ligands are present in these tris(ligand) complexes, a considerable cytotoxic activity is observed. This would imply that the 2-phenylazopyridine ruthenium(II) complexes act by a completely different mechanism than the well-known cisplatin. This finding is important, because an anticancer compound acting via a different mechanism is a prerequisite in designing new anticancer drugs. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005) [source] A New Triterpene and New Sesquiterpenes from the Roots of Ligularia sagittaHELVETICA CHIMICA ACTA, Issue 9 2008Ping-Lin Li Abstract One new triterpene and seven new eremophilane-type sesquiterpenes were isolated from the roots of Ligularia sagitta, among them 1a, an O -acetylated oleanane type triterpene, 2a and 3a, two 11-nor eremophilane-type sesquiterpenes, 4a, 5, and 6, three standard eremophilane-type sesquiterpenes, and 7 and 8, two tri-nor eremophilane-type sesquiterpenes. Their structures were established by extensive spectral analyses (1D, 2D-NMR, IR, and MS). Compound 1a showed moderate cytotoxicity against two tumor cell lines. [source] Microparticle-mediated gene delivery for the enhanced expression of a 19-kDa fragment of merozoite surface protein 1 of Plasmodium falciparumBIOTECHNOLOGY PROGRESS, Issue 1 2010Shan Liu Abstract The 19 kDa carboxyl-terminal fragment of merozoite surface protein 1 (MSP119) is a major component of the invasion-inhibitory response in individual immunity to malaria. A novel ultrasonic atomization approach for the formulation of biodegradable poly(lactic- co -glycolic acid) (PLGA) microparticles of malaria DNA vaccines encoding MSP119 is presented here. After condensing the plasmid DNA (pDNA) molecules with a cationic polymer polyethylenimine (PEI), a 40 kHz ultrasonic atomization frequency was used to formulate PLGA microparticles at a flow rate of 18 mL h,1. High levels of gene expression and moderate cytotoxicity in COS-7 cells were achieved with the condensed pDNA at a nitrogen to phosphate (N/P) ratio of 20, thus demonstrating enhanced cellular uptake and expression of the transgene. The ability of the microparticles to convey pDNA was examined by characterizing the formulated microparticles. The microparticles displayed Z-average hydrodynamic diameters of 1.50,2.10 ,m and zeta potentials of 17.8,23.2 mV. The encapsulation efficiencies were between 78 and 83%, and 76 and 85% of the embedded malaria pDNA molecules were released under physiological conditions in vitro. These results indicate that PLGA-mediated microparticles can be employed as potential gene delivery systems to antigen-presenting cells in the prevention of malaria. © 2009 American Institute of Chemical Engineers Biotechnol. Prog., 2010 [source] Antimicrobial and Cytotoxic Activities of Neolignans from Magnolia officinalisCHEMISTRY & BIODIVERSITY, Issue 3 2004Wan-Jr Syu In the light of the steady increase of infections related to vancomycin-resistant enterococci (VRE) and methicillin-resistant Staphylococcus aureus (MRSA), the medicinal plant Magnolia officinalis was subjected to bioassay-directed fractionation, which led to the isolation of the known neolignans piperitylmagnolol (1), magnolol (2), and honokiol (3) from the MeOH extract. In broth-microdilution assays, 1,3 exhibited antibacterial activities against VRE and MRSA at minimum-inhibitory concentrations (MIC) in the range of 6.25,25,,g/ml, compound 1 being the most-potent antibiotic. The ratio of MBC/MIC (MBC=minimum bactericidal concentration) was ,2 for all compounds. The kinetics of the antibacterial action of 1 and 3 were studied by means of time-kill assays; both compounds were bactericidal against VRE and MRSA, their actions being time dependent, or both time and concentration dependent. Magnolol (2) was acetylated to magnolol monoacetate (4) and magnolol diacetate (5) (partial or full masking of the phenolic OH functions). The cytotoxic properties of 1,5 against human OVCAR-3 (ovarian adenocarcinoma), HepG2 (hepatocellular carcinoma), and HeLa (cervical epitheloid carcinoma) cell lines were evaluated. The CD50 values for compounds 1,3 were in the range of 3.3,13.3,,g/ml, derivatives 4 and 5 being much less potent. This study indicates that piperitylmagnolol (=3-[(1S,6S)-6-isopropyl-3-methylcyclohex-2-enyl]-5,5,-di(prop-2-enyl)[1,1,-biphenyl]-2,2,-diol; 1) possesses both significant anti-VRE activity and moderate cytotoxicity against the above cancer cell lines. [source] | ||||||||||