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WOS: 000326852400015, PubMed ID: 24255582, Objective: To investigate the effects of E7080 and N-5-(1-iminoethyl)-L-ornithine dihydrochloride (L-NIO) on colorectal cancer alone and in combination. Methods: HT29 colorectal cancer cell line from Sap Institute was used. Real-time cell analysis (xCELLigence system) was performed to determine the effects of E7080 and L-NIO on colorectal cell proliferation. While apoptosis was determined with Annexin V staining, and the effect of agents on angiogenesis was determined with chorioallantoic membrane (CAM) model. Results: We found that E7080 has a strong antiproliferative effect with an half maximum inhibition of concentration (IC50) value of 5.60x10(-8) mol/L. Also it has been observed that E7080 showed antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. Antiangiogenic scores of E7080 were 1.2, 1.0 and 0.6 for 100, 10 and 1 nmol/L E7080 concentrations, respectively. Furthermore, apoptosis has been detected in 71% of HT29 colorectal cancer cells after administration of 100 nmol/L E7080 which may indicate strong apoptotic effect. Meanwhile administration of L-NIO alone did not show any effect, but the combination of E7080 with L-NIO increased the antiproliferative, antiangiogenic and apoptotic effects of E7080. Conclusions: Results of this study indicate that E7080 may be a good choice in treatment of colorectal tumors. Furthermore the increased effects of E7080 when combined with L-NIO raise the possibility to use a lower dose of E7080 and therefore avoid/minimize the side effects observed with E7080.

WOS: 000315167100021, Poly[(maleic anhydride)-co-(vinyl acetate)] (MAVA) copolymer was synthesized by free radical polymerization reaction, in methyl ethyl ketone at 80 degrees C, using benzoyl peroxide as the initiator. The copolymer was then modified with a biomolecule, noradrenaline (NA). The modification reaction was performed at 70 degrees C in dimethylformamide containing triethylamine as the catalyst. The modified polymer was named MAVA/NA. Structural characterization of the copolymer and the modified product was carried out by Fourier transform infrared (FTIR) and 1H NMR and 13C NMR spectroscopy. The FTIR, 1H NMR and 13C NMR spectra confirmed that NA was successfully covalently bound to the MAVA copolymer backbone. Surface morphology was visualized by atomic force microscopy. The cumulative release of NA from MAVA/NA was determined in phosphate buffered saline solution for 7 days at 37 degrees C and compared with MAVA. Cytotoxicity of the MAVA/NA was evaluated by using a mouse fibroblast cell line (L929). Results obtained indicated that MAVA/NA had almost no toxicity and no negative effect on cell viability at 250 mu g mL1 concentration. (c) 2012 Society of Chemical Industry, Science Research Projects Foundation of Cumhuriyet University [F258], This work was supported by the Science Research Projects Foundation of Cumhuriyet University (Project F258).

WOS: 000287819600002, Biomaterials are mostly polymers made by monomers, and are used in artificial organ production in contemporary medicine. They are prepared by the polimerization reaction of certain monomers. The aim of the present study was to investigate whether acrylamide, methacrylamide, N-isopropylacrylamid, acrylic acid, 2-hydroxyethyl methacrylat, 1-vinyl-2-pyrrolidone and ethylene glycol had cytotoxic effects and induce apoptosis or not in spinal cord. Immunolocalization of glial fibrillary acidic protein (GFAP) was also determined, and it was evaluated by using semi-quantitative morphometrical techniques. The cellular process of apoptosis is an important component of tissue and organ development as well as the natural response to disease and injury. Therefore the positive immunohistochemical staining for apoptosis was also examined by TUNEL staining technique. Following the intramuscular injection of aqueous monomer solutions that are prepared in certain concentration, appropriate tissue samples obtained at certain time intervals were fixed in 10% buffered neutral formaline. The cytotoxicity of monomers on cultured fibroblastic cell lines was examined in vitro. Acrylic acid had the most cytotoxic effect when compared to the methacrylamide and the ethylene glycol groups. GFAP immunoreactivity was found to be rather stronger in the methacrylamide than the other monomers application groups. TUNEL positive cell were observed in the methacrylamide, acrylic acid, N-vynil pyrrolidine, acrylamide, N-isopropylacrilamid and 2-hydroxyethyl metacrylad application groups than the other groups. In conclusion, while some monomers used in biomaterial production seemed not to affect the cell viability and GFAP immunoreactivity, some other monomers had adverse effects on those features. This in turn may contribute to the pathological changes associated to the monomer type.

WOS: 000457840400041, PubMed ID: 29210829, Purpose: To evaluate the factors affecting the adhesion of Acanthamoeba trophozoites to the surface of cosmetic contact lenses (CCLs). Methods: Acanthamoeba castellanii and A. hatchetti trophozoites were inoculated onto CCLs (hema copolymer [HM] [38.5% H2O], phemfilcon [PF] [55% H2O], polymacon [PM] [38% H2O], polyhema [PH] [% 42 H2O], and hema [HM55] [55% H2O]), and the number of trophozoites adhered to the lens surfaces was assessed over time, that is, at 15 min, 1, and 24 hr. In addition, scanning electron microscopy (SEM) analysis of the lens surfaces was performed to evaluate the effect of lens surface topology on adhesion. Results: The number of amoeba adhered to the contact lens surface was found lower with PF and PH production materials, than lenses with HM, PM, and HM55 production materials (P0.05). No significant difference was found on average amoeba adhesion between contact lenses with hema production material but with different water contents (45%, 55%), to see the effect of water content on amoebic adhesion (P, Scientific Research Project Fund of Cumhuriyet University [631], Supported by the Scientific Research Project Fund of Cumhuriyet University under the project number: 631.

WOS: 000319496400007, PubMed ID: 23713427, Poly(maleic anhydride-co-styrene) (MAST) was synthesized by a free-radical polymerization reaction. A bioactive molecule, procainamide hydrochloride (PH), was then conjugated to MAST. The conjugation product was named as MAST/PH. Structural characterization of MAST and MAST/PH was carried out by Fourier Transform Infrared and Nuclear Magnetic Resonance spectroscopy. Their molecular weights were determined by size-exclusion chromatography. A mechanism was then suggested for the conjugation reaction. The results of the cytotoxicity assay, employing a mouse fibroblast cell line (L929), indicated that MAST/PH had no cytotoxicity at concentrations 62gmL(1) (p>0.05). Antiproliferative activities of MAST/PH and PH were determined by the BrdU cell proliferation ELISA assay, using C6 and HeLa cell lines. In the experiment, two anticancer chemotherapy drugs, cisplatin and 5-fluorouracil, were included as positive control. Antiproliferative activity results demonstrated that MAST/PH yielded the highest suppression profile (approximately 42%) at 20g/ml, while free PH exerted the same activity at 100g/ml. Interestingly, both MAST/PH and PH suppressed the proliferation of only one of the cell lines, C6 cells. Both cisplatin and 5-fluorouracil yielded approximately 60% antiproliferative activity on C6 cells at 20 and 100g/ml concentrations. Antiangiogenic capacity of both MAST and MAST/PH was also investigated by using the chicken chorioallantoic membrane assay. Results obtained indicated that while MAST/PH could be included into the category of good antiangiogenic substances, the activity score of MAST was within the weak category., Sciences Research Projects Foundation of Cumhuriyet University [F258], This work was supported by Sciences Research Projects Foundation of Cumhuriyet University (Project No: F258). The structural characterizations were carried out at Technology Research and Developing Centre, Erciyes University, Kayseri, Turkey.

WOS: 000374972400021, PubMed ID: 27078662, Trichomonosis, caused by the protozoan parasite Trichomonas vaginalis, is a curable sexually transmitted disease that is most commonly encountered worldwide. Increasing importance of trichomoniasis and emerging of resistance against metronidazole lead to search for alternative drugs with different mode of activity. The purpose of this study was to determine in vitro activity of ceragenins (CSA-13, CSA-44, CSA-13, and CSA-138) against the metronidazole-susceptible (ATCC 30001) and metronidazole-resistant (ATCC 50138) strains of T. vaginalis. The effective concentrations were evaluated using two strains of T. vaginalis with different metronidazole susceptibilities (ATCC 30001 and ATCC 50138) in the presence of dilution series of ceragenins in 24-well microtitre assays. Overall, all the ceragenins killed the metronidazole-susceptible (ATCC 30001) and metronidazole-resistant (ATCC 50138) strains of T. vaginalis (p > 0.05). With regard to the their effects against the studied strains of T. vaginalis, in order of effectiveness, overall, the ceragenins ordered as CSA-13 (the most effective), CSA-131 and CSA-138 (effective similarly), and CSA-44 (the least effective) (p < 0.05). All of the ceragenins reduced the trophozoite numbers of both of studied strains of T. vaginalis with a time-and dose-dependent manner (p < 0.05). Although all of the study ceragenins, CSA-13, CSA-44, CSA-13, and CSA-138, killed the studied strains of T. vaginalis. CSA-13 is the leading ceragenin as the most effective anti-trichomonas compound, followed by CSA-131 and CSA-138. They have a potential to have a place in the armemantarium of gynecologic and urologic practice for the management of sexually transmitted diseases.

WOS: 000302264600008, PubMed ID: 22343683, Unfractionated heparin (UFH) and low molecular weight heparins have been used as anticoagulation agents in cardiovascular clinics for decades. However, these molecules also have potent antiangiogenic effects. Whereas, angiogenesis may be the most crucial determinant of the prognosis of cardiovascular diseases, and except some special situation, antiangiogenic effect is not desirable in the most of the cardiovascular disease. In this study, we aimed to compare the antiangiogenic potency of UFH, enoxaparin, and tinzaparin. The antiangiogenic efficacies of UFH, enoxaparin, and tinzaparin were examined in vivo by using the chick chorioallantoic membrane (CAM) model. Twenty fertilized eggs were used for each studied drug. Drug solutions were prepared in 10 and 1 IU/10 mu l concentrations. Decreases in the density of the capillaries were assessed and scored. All three drugs showed antiangiogenic effects on the chick CAM at the 10 IU/10 mu l concentration. However, the antiangiogenic score of the UFH was significantly higher than that of enoxaparin and tinzaparin at 1 and 10 IU/10 mu l concentrations. UFH had stronger and antiangiogenic potential than enoxaparin and tinzaparin. However, tinzaparin showed dose-dependent antiangiogenic effects. We think that an anticoagulant molecule with a less and dose-dependent antiangiogenic effect, as in the case of tinzaparin, may be more desirable in case of cardiovascular disease related with insufficient angiogenesis. Blood Coagul Fibrinolysis 23: 218-221 (C) 2012 Wolters Kluwer Health vertical bar Lippincott Williams & Wilkins.