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Anticancer Drug Candidate (anticancer + drug_candidate)
Selected AbstractsReal-time monitoring of intracellular calcium dynamic mobilization of a single cardiomyocyte in a microfluidic chip pertaining to drug discoveryELECTROPHORESIS, Issue 24 2007Xiujun Li Abstract A microfluidic method for real-time quantitative measurement of cellular response pertaining to drug discovery is reported. This method is capable of multiple-step liquid delivery for measuring the drug response of a single cardiomyocyte, due to the improved cell retention by a newly designed chip. The chip, which consists of a cell-retention chamber with a weir structure, was fabricated just by a one-photomask microfabrication procedure followed by on-chip etching. This method differs from the conventional method, which uses two-mask photolithography to fabricate the microchannel (deep etch) and the weir structure (shallow etch). The dimensions of the weir structure have been predicted by a mathematical model, and confirmed by confocal microscopy. Using this microfluidic method, the dynamic [Ca2+]i mobilization in a single cardiomyocyte during its spontaneous contraction was quantified. Furthermore, we measured the cellular response of a cardiomyocyte on (i) a known cardiotonic agent (caffeine), (ii) a cardiotoxic chemotherapeutic drug (daunorubicin), and (iii) an herbal anticancer drug candidate , isoliquiritigenin (IQ) based on the fluorescent calcium measurement. It was found that IQ had produced a less pronounced effect on calcium mobilization of the cardiomyocytes whereas caffeine and daunorubicin had much stronger effects on the cells. These three experiments on cardiomyocytes pertaining to drug discovery were only possible after the improved cell retention provided by the new chip design (MV2) required for multiple-step real-time cellular analysis on a microchip, as compared with our old chip design (MV1). [source] New Insights into the Chemistry of the Antineoplastic Lanthanum Complex Tris(1,10-phenanthroline)tris(thiocyanato-,N)lanthanum(III) (KP772) and Its Interaction with BiomoleculesEUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 28 2009Florian Biba Abstract The lanthanide complex tris(1,10-phenanthroline)tris(thiocyanato-,N)lanthanum(III) [La(phen)3(NCS)3] (KP772) is a promising anticancer drug candidate, capable of overcoming resistance of tumors to established chemotherapeutics. The compound was characterized by elemental analysis, IR, 1H NMR spectroscopy, TG/DTA measurements, mass spectrometry and X-ray diffraction analysis. The results indicate that KP772 is a neutral, nine-coordinate complex. In addition the behavior in water, important for the application as a chemotherapeutic drug, and the binding to biomolecules was investigated by capillary electrophoresis and ICP-MS.(© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009) [source] Interactions of the "piano-stool" [ruthenium(II) (,6 -arene)(en)CL]+ complexes with water and nucleobases; ab initio and DFT studyJOURNAL OF COMPUTATIONAL CHEMISTRY, Issue 12 2009k Futera Abstract Piano stool ruthenium complexes of the composition [Ru(II)(,6 -arene)(en)Cl]+/2+ (en = ethylenediamine) represent an emerging class of cisplatin-analogue anticancer drug candidates. In this study, we use computational quantum chemistry to characterize the structure, stability and reactivity of these compounds. All these structures were optimized at DFT(B3LYP)/6-31G(d) level and their single point properties were determined by the MP2/6-31++G(2df,2pd) method. Thermodynamic parameters and rate constants were determined for the aquation process, as a replacement of the initial chloro ligand by water and subsequent exchange reaction of aqua ligand by nucleobases. The computations were carried out at several levels of DFT and ab initio theories (B3LYP, MP2 and CCSD) utilizing a range of bases sets (from 6-31G(d) to aug-cc-pVQZ). Excellent agreement with experimental results for aquation process was obtained at the CCSD level and reasonable match was achieved also with the B3LYP/6-31++G(2df,2pd) method. This level was used also for nucleobase-water exchange reaction where a smaller rate constant for guanine exchange was found in comparison with adenine. Although adenine follows a simple replacement mechanism, guanine complex passes by a two-step mechanism. At first, Ru-O6(G) adduct is formed, which is transformed through a chelate TS2 to the Ru-N7(G) final complex. In case of guanine, the exchange reaction is more favorable thermodynamically (releasing in total by about 8 kcal/mol) but according to our results, the rate constant for guanine substitution is slightly smaller than the analogous constant in adenine case when reaction course from local minimum is considered. © 2008 Wiley Periodicals, Inc. J Comput Chem, 2009 [source] Antimicrobial and cytotoxic activities of Malaysian endophytesPHYTOTHERAPY RESEARCH, Issue 5 2010Kalavathy Ramasamy Abstract Endophytes, which are receiving increasing attention, have been found to be potential sources of bioactive metabolites following the discovery of paclitaxel producing endophytic fungi. In the present study, a total of 348 endophytes were isolated from different parts of 24 Malaysian medicinal plants. Three selected endophytes (HAB10R12, HAB11R3 and HAB21F25) were investigated for their antimicrobial and cytotoxic activities. For antimicrobial activity, HAB10R12 and HAB11R3 were found to be most active against bacteria and fungi, respectively. Their antimicrobial effects were comparable to, if not better than, a number of current commercial antibacterial and antifungal agents. Both HAB10R12 and HAB21F25 were found to be potential anticancer drug candidates, having potent activity against MCF-7 and HCT116 cell lines and warrant further investigation. Copyright © 2009 John Wiley & Sons, Ltd. [source] | ||||||||||