Template synthesis of N,N′-bis(4-acetyl-5-methylpyrazole-3-yl)formamidine (ampf) was performed starting from 4-acetyl-3-amino-5-methylpyrazole (aamp) and CH(OC2H5)3 in methanol in the presence of CuCl2, Cu(NO3)2, or Ni(NO3)2. The ligand was isolated in coordinated form as [Cu(ampf)Cl2], [Cu(ampf)(MeOH)(NO3)2]MeOH, and [Ni(ampf)(MeOH)2(NO3)]NO3 correspondingly. The compounds were characterized by elemental analysis, Fourier-transform IR and electronic spectroscopy, thermal analysis, single-crystal X-ray diffraction, and quantum chemical (density functional theory) calculations. The density functional theory calculations provided information on the metal–ligand interactions in the complexes and assisted the assignment of the FT-IR spectra. The antiproliferative activity of the complexes and the ligand precursor, aamp, was tested against human myelogenous leukaemia K562, colon adenocarcinoma HT29, and cervix carcinoma HeLa.
Starting from the D-glucose derivative (I), a total synthesis of (+)-crassalactone B (VI) and a new synthesis of (+)-crassalactone C (VII) is presented.
Department of Chemistry, Faculty of Sciences, University of Kragujevac, 34000 Kragujevac, Serbia Institute of Oncology Sremska Kamenica, Institutski put 4, 21204 Sremska Kamenica, Serbia Department of Chemistry, Faculty of Sciences, University of Novi Sad, 21000 Novi Sad, Serbia Faculty of Chemistry, University of Belgrade, 11000 Belgrade, Serbia *E-mail: mjoksovic@kg.ac.rs Received October 19, 2009 DOI 10.1002/jhet.400 Published online 8 June 2010 in Wiley InterScience (www.interscience.wiley.com).
INTRODUCTION In the last 15 years, the introduction of molecular biology methods and techniques for identifying mutations and measuring gene expression levels of mutated genes since recently, have enabled precise molecular diagnostics, classification and assessment of prognosis and therapeutic response of malignant disease to specific therapies. The increased knowledge of the cancer genome and the introduction of multiple new technologies in cancer research have significantly improved the drug discovery process, leading to key success in targeted cancer therapeutics, including tyrosine kinase inhibitors. Tyrosine kinase inhibitors are the molecular targeted neoadjuvant and adjuvant therapy of various malignancies. Many more results which are expected from ongoing trials are necessary to specify the appropriate dosages, stages at which to start the treatment, and which therapeutic combinations to apply.
In this study we investigated antioxidative and antiproliferative activity of different horsetail (Equisetum arvense L.) extracts. The antioxidative activity was measured by the electron spin resonance (ESR) spectroscopy-spin trapping method. The influence of different horsetail extracts during lipid peroxidation of (1) sunflower oil induced by the lipophilic azo-initiator 4,4'-azobis(4-cyanovaleric acid) and (2) soybean phosphatidylcholine liposomes induced by the hydrophilic azo-initiator 2,2'-azobis(2-amidinopropane) dihydrochloride was studied. Antiproliferative activity was measured using the sulforhodamine B colorimetric assay on the human cancer cell lines HeLa, HT-29, and MCF7. The results of ESR analysis confirmed that the extracts investigated suppressed the formation of lipid peroxyl radicals in both systems investigated in a dose-dependent manner. The results indicate that n-butanol, methanol, ethyl acetate, and water extracts had significant peroxyl radical scavenging activity. Extracts inhibited cell growth that was dependent on cell line, type of extract, and extract concentration. Ethyl acetate extract exhibited the most prominent antiproliferative effect, without inducing any cell growth stimulation on human tumor cell lines. The results obtained suggest that the horsetail extracts could be used as an easily accessible source of natural antioxidants and as potential phytochemicals.
UNLABELLED Each birth which has happened before gestation period of 37 weeks of gestation and which is not related to a degree of birth difficulty is called premature birth. Different researches pointed out that C-reactive protein (CRP) can be used as a possible marker of idiopathic preterm delivery. RESEARCH GOALS WERE To examine reliability of CRP in mothers serum as a marker of premature birth among pregnant women who had no of the known risks for premature birth. To determine critical value of CRP in pregnancies this ended up as a premature birth. To determine connection between value of CRP and low birth weight of the newborn. The research is done in a form of prospective study on 200 pregnant women. Research included pregnant women without known risks factors for premature birth with condition that those women had suitable antenatal protection. All pregnant women were divided in into two groups, experimental and control group. Experimental group is consisted of 150 pregnant women who were regularly controlled in ambulance. Control group consisted of 50 pregnant women who were hospitalized at the Department for Pathology of pregnancy due to threatening miscarriage symptoms of condition that tocolytic index were less than 4. The value of CRP in serum of all pregnant women was determined in period from 20 to 24th week of gestation. In further course of pregnancy we followed those pregnant women with more often premature birth and if premature birth occurred more often in pregnant women with increased value of CRP in relation to women who had normal values. As a critical value for CRP was taken > 2 median value. Besides descriptive statistic methods in evaluating data processing were used (see text for symbols) test, student's t-test, Fishers test and Mann-Whitney test. RESULTS Mean value of CRP in experimental group was 3.913 and in control group 14.92 (t = 4.72, p < 0.0001). Mean value of CRP was 18.17 in group of prematurely births and in women who gave birth on time 3.87 (t = 5.72, p < 0.0001). Value of CRP > 2 had 33 women who gave birth prematurely (16.5%). CONCLUSIONS CRP can be used as a reliable marker of idiopathic premature birth. CRP value which is connected with development of premature birth is 4 mg/l. There is connection between the value of CRP > 2 and low birth weight of the newborn.
In this study we performed the dynamic and static scintigraphy of the domestic dog, using the newly synthesized radiopharmaceutical, [ 99m Tc(CO)3(H2O)3]-C60(OH)22-24. In the current study, an advanced one-step method for the functionalization of fullerenol by 99m Tc is described. Optical properties of as-prepared samples and the mechanism responsible for the functionalization were investigated using UV–VIS and FTIR spectroscopy, respectively. Also, the presence of the Tc complex on fullerenol was confirmed by using the energy dispersive X-ray spectroscopy, HPLC and MALDI TOF techniques.This simple and effective method of producing a new radiopharmaceutical is of interest not only for its application in various areas of technology and biology, but also for investigating its potential use in radiation technology for nanoengineering of materials. With dynamic scintigraphy, performed during 30 minutes (120 frames, 15 sec per frame), we obtained ratios of heart, liver and spleen counts: 222/249/168; 178/320/217; 120/348/239 respectively. By static scintigraphy after 1 hour, we detected the activity in heart, liver, spleen and intestines. After 4 hours, the radiopharmaceutical activity was detected in salivary glands. The detection after 21 hours showed the activity in kidneys and urinary bladder, while the activity in intestines was absent. After 24 hours, we detected the activity in liver, spleen, kidneys and urinary bladder. Pharmacokinetic investigations performed in this study are of key interest for the further fullerenol in vivo research.
Nema pronađenih rezultata, molimo da izmjenite uslove pretrage i pokušate ponovo!
Ova stranica koristi kolačiće da bi vam pružila najbolje iskustvo
Saznaj više