[Influence of copper (II) complex on the activity of selected oxidative enzymes]. / Wplyw kompleksu miedzi (LL) na aktywnosc wybranych enzymów antyoksydacyjnych.

UNLABELLED: Coxarthrosis results in physical limitations (hypokinesis) and a necessity to change one's life style to the one that does not require much movement. Physical inactivity leads rapidly to metabolic processes inhibition. The processes of protein, carbohydrate and lipid catabolism intensify. Abnormal metabolism of polyunsaturated fatty acids occurs, which consequently leads to the development of reactive oxygen species (ROS) and to the acceleration of lipid peroxidation. Therefore, it is well-founded to seek for a new group of compounds demonstrating interesting biochemical properties. Among such already known compounds are chromone, azole and flavone derivatives, known for their oxidative properties. The aim of the study was to assess the antioxidant enzymes: catalase (CAT) and glutathione peroxidase (GPX) in erythrocytes in 25 patients suffering from coxarthrosis in comparison with healthy persons. MATERIALS AND METHODS: The activity of catalase was determined in erythrocytes using the method of Beers and Sizer at 240 nm on the Beckman spectrophotometer. The activity of glutathione peroxidase was estimated using the method of Little and O'Brien at 412 nm on the Beckman spectrophotometer. The research was conducted with the permit of the Bioethics Committee No RNN/260/08/KB dated 20.05.2008. Blood for the tests was taken from periulnar vein to anticoagulant tubes (EDTA). The group consisted of 25 patients hospitalized in the Trauma and Orthopaedic Ward of the Hospital in Lódz. RESULTS: The results of the tests on erythrocytes in the patients with physical limitations reveal the increase of glutathione peroxidase and catalase activity by about 50% in all patients, who were administered the dichlorobis (N1-dichloromethyl-3,5-dimethylpyrazole, copper (II) compound in comparison to the control group, where the foregoing compound was not used. CONCLUSION: The research results significantly emphasise that adding of new chemical compounds to blood in investigation of oxidative properties has a considerable influence on the activity of the selected enzymes (catalase and glutathione peroxidase) in comparison to the control group. The research reveals an increase of the activity of all antioxidant enzymes, where newly synthesized chemical compounds were used. The results of antioxidative capacity tests confirmed that complex compounds with Cu (II) ions have a significant influence on the antioxidative status. The studies on the foregoing enzymes also indicate that overproduced free radicals participate in the whole course of the coxarthrosis.

[Etiology of colorectal cancer and antioxidant barrier of the organism]. / Etiologia raka jelita grubego oraz bariera antyoksydacyjna ustroju.

Colorectal cancer is a serious medical and economic problem in Poland, as the detection and results of its treatment are very low. Due to this fact, medical research is still conducted in order to find out the symptoms of this tumor and proper preventive measures. According to one hypothesis of carcinogenesis, the process of creating the tumor begins and develops when the balance between the production of reactive oxygen species (ROS) and their deactivation by the "antioxidant protective barrier of the organism" is disturbed. As a result of this theory, it has been decided to examine the plasma concentration of the dietary minerals which work as antioxidants. The results entailed conclusions which prove the free radicals theory of carcinogenesis. They also confirm the part which the antioxidant protective barrier plays in the defence against ROS and their carcinogenic consequences.

[The search for new antitumor medicines]. / Poszukiwanie nowych leków przeciwnowotworowych.

Tumor illnesses belong to the major problems of contemporary medicine. A crucial group of medicines used in the antitumor therapy are complexes of platinum (II). The first medicine introduced into the treatment of various tumors was cis-platinum. This compound was first used at the beginning of the 1970s. It is used up to now in the treatment of ovary, esophagus, testicle and neck tumors. The second medicine used in chemotherapy was carboplatin. The medicines mentioned above have a similar method of activity but they differ in toxicity. The main area of research of contemporary medicine is the constant search for new antitumor medicines which would be characterized by a better therapeutic index in comparison with cis-platinum.

[Tumour illnesses and nutrition]. / Choroby nowotworowe a ywienie.

It is very important for contemporary medicine to create new effective cytotoxic compounds of platinum with better clinical tolerance. Harmful elements which exist in food delivered to a human organism may either get inactive or activate complex processes which may to lead to illnesses such as tumors. One of these elements are. Undoubtedly, free radicals. They destroy, among other things, the DNA, causing changes in the genetic code and its mutations. More recently came the publication of speaking a lot about the capabilities of the organism to defend against the above-mentioned factors. Eating adequate amounts of fruits and vegetables contain antioxidants in its composition contributes positively to our body and reduces the risk of cancer.

[Activity of selected antioxidant enzymes examination in people with colorectal cancer]. / Badanie aktywnosci wybranych enzymów antyoksydacyjnych u chorych na raka jelita grubego.

UNLABELLED: Colorectal cancer is a serious medical problem. According to one hypothesis of carcinogenesis, tumour creation process begins and develops when the balance between the production of reactive oxygen species (ROS) and their disactivation by the antioxidant protective barrier of the organism is disturbed. THE AIM OF THE STUDY was, following this theory, to examine the plasma concentration of the dietary minerals with antioxidant properties. MATERIAL AND METHODS: The research material was the blood of 8 people, taken to vacuum test tubes with an anticoagulant - 4 ml of sodium heparin. The activity of catalase was marked following Beers method, while the activity of superoxide dismutase according to H.P. Misra and J. Fridovich method. RESULTS: The results show that the copper complex added, i.e. dichlorine(3,4,5-trimethyl-N1 - pyrazol-1yl) Cu(II) from derivatives of azoles, has a large impact on the activity of selected enzymes. After adding it, their activity increased by ca 67% in comparison with the control group. It proves the efficacy of this compound. CONCLUSIONS: The results prove the free radicals theory of carcinogenesis. They also confirm the part which the antioxidant protective barrier plays in the defense against ROS and their carcinogenic consequences.

[In vitro biological activity of new platinum(II) and palladium(II) complex compounds]. / Aktywnoss biologiczna--in vitro nowych zwiazków koordynacyjnych platyny(II) i palladu(II).

UNLABELLED: A nitrogen ring is present in many biological molecules, which play an important part in cell division as well as in genetic information transfer. It is also a part of the purine system, which builds DNA and has potential places/spots of platinum drug co-ordination. Therefore, it may be hoped, that platinum(II) complexes with diazol ligands will have considerable affinity for DNA binding sites. The work was aimed at assessment of biological activity and especially of cytotoxic activity, of new complex connections of the selected diazols with Pt(II) and Pd(II) ions. MATERIALS AND METHODS: The MTT test is aimed at the assessment of cytotoxicity of chemical compounds. It consists in the colorimetric determination of a product--farmazon, formed after adding MTT (bromide 3[4,5-dimetylo-2-ilo]-2,5-difenylotetrazolu) to the culture suspension in the presence of the compound subject to the test. All the tested Pt(II) complexes before adding to the cell cultures were dilluted in DMF. MTT tests for individual complexes were conducted on two cell lines L1210 and P388. RESULTS: Compounds 13, 21 and 25 on P388 neoplastic cell revealed about three times smaller in-vitro cytotoxicity, whereas platinum(II) and palladium(II) complexes 13, 21, 25, 43, 46, revealed cytotoxicity being about 3-4 times smaller than the reference cisplatin. Complex 45 revealed eight times smaller activity and complex 44 revealed significantly small, about two hundred smaller activity. CONCLUSION: Based on the MTT tests it may be concluded that compounds 13, 21 and 25 reveal selective cytotoxicity to P388 neoplastic cells.

[Testing antineoplastic activity of new platinum(II) and palladium(II) complex compounds]. / Badanie aktywnosci przeciwnowotworowej nowych zwiazków koordynacyjnych platyny(II) i palladu(II).

UNLABELLED: A pyrazole system is incorporated in many biological molecules which play an important part in genetic processes. It seems that co-ordinating biological molecules, which would serve as carriers, should contribute to minimising the toxic effects of the potential platinic drugs. AIM OF THE STUDY: Assessment of in vivo biological activity, and in particular of antineoplastic activity of new platinum(II) and palladium(II) complexes. MATERIAL AND METHODS: The assessment of toxicity of the compounds was made with the Deichmann and Le Blanck method. The antineoplastic activity of the new complex compounds--pyrazole derivatives with Pt(II) and Pd(II) ions was tested on mouse L1210 leukemia cell culture and on lymphatic leukemia P388. BDF1 or CDF1 mice divided into groups of 5-9 animals were subject to the tests. RESULTS: Complexes 13, 21, 25, 16, 24 and 28 did not reveal any antineoplastic activity to the mouse L1210 leukemia, whereas complexes 13, 21 and 25 revealed in-vivo antineoplastic activity to the P388 leukemia, extending the mouse's survival time by about 50%. The control group consisted of mice which were administered a 14% methylcellulose solution. CONCLUSIONS: As a result of the tests conducted to asses the in-vivo antineoplastic activity it was found that the 25 complex demonstrates the strongest activity to the P388 leukemia. It may be presumed that it is caused by trans configuration of the complex predisposing to the creation of interstrand cross-links. It may be also caused by the presence of the chloromethyl substituents, located on N1 nitrogen atom of the ligand, which increases the capacity of nitrogen N7 guanine alkylation in DNA.

[Influence of complex compounds on the activity of antioxidant enzymes in neoplastic diseases of the digestive tract]. / Wplyw zwiazków koordynacyjnych na aktywnosé enzymów antyoksydacyjnych w chorobach nowotworowych przewodu pokarmowego.

UNLABELLED: Chemotherapy is an important field of clinical medicine and pharmacology Chemotherapy is the main method of treating the neoplasm. It involves treating the neoplastic disease with the use of natural or synthetic anticancer drugs commonly known as the cytostatics. The cancer therapy involving the cytostatics is a difficult and not always effective process, which requires taking into consideration the mechanisms of action, pharmacokinetics and the dosage schemas. The complexity of the chemotherapy is influenced by: still incomplete knowledge of causes of neoplasm formation, slight biological differences between the cancer cells and the regular cells, very small selectivity of cytostatics' action, narrow therapeutic index of the anticancer drugs, high toxicity for healthy cells and unsatisfactory anticancer activity. The aim of the study was to obtain the complex compounds of copper (II), and especially of dinitrate (V) di (3,4, 5-trimethyl-N1-pyrazol-kappaN2) copper (II), and its subsequent testing for pro- and antioxidative activity in people suffering from neoplastic diseases of the digestive tract (colorectal and gastric carcinoma). Material and methods. The activity of catalase was determined in erythrocytes patients suffering from colorectal and gastric carcinoma and in control group (hernia, chronic gastric ulcer disease and haemorrhoids) using the method of Beers and Sizer at 240 nm on the Beckman spectrophotometer. RESULTS: The results of the test on catalase in patients suffering from colorectal and gastric carcinoma indicate that the addition to the blood of the complex compound of Cu(II) significantly influences the activity of the enzyme in comparison with the control group in which the substance tested was not used. In the tests a marked statistical difference was observed between the studied and the control group. CONCLUSION: The results reveal that chemical compounds, that is, dinitrate (V) di (3,4,5-trimethyl-N1-pyrazol-kappaN2) copper (II), has a significant influence on the activity of catalase, the antioxidant enzyme.

Application of thin-layer chromatographic data in quantitative structure-activity relationship assay of thiazole and benzothiazole derivatives with H1-antihistamine activity. II.

Quantitative structure-activity relationship (QSAR) analysis of H1-antihistamine activity was carried out and chromatographic data of 2-[2-(phenylamino)thiazol-4-yl]ethanamine, 2-(2-benzyl-4-thiazolyl)ethanamine, 2-(2-benzhydrylthiazol-4-yl)ethylamine derivative, and 2-(1-piperazinyl- and 2-(hexahydro-1H-1,4-diazepin-1-yl)benzothiazole derivatives were obtained. Normal-phase (NP) TLC plates (silica gel 60F254), impregnated with solutions of selected amino acid mixtures (L-Asp, L-Asn, L-Thr and L-Lys) were used in two developing solvents as human histamine H1-receptor (hH1R) antagonistic interaction models. The lipophilicity data of the examined compounds were obtained and used in the QSAR assay. Using regression analysis, relationships between chromatographic and biological activity data were found. The correlations obtained in the present experiment with NP-TLC are more significant that those obtained in the experiment with RP2 TLC, because of the optimal fitting of the chromatographic system conditions to the lipophilicity of solutes. All proposed chromatographic models should facilitate pre-selection of the new drug candidates. The correlations of calculated pA2(H1) values of the tested compounds predicted by the use of the best equations versus their pA2(H1) obtained from the biological tests were significant (R2 = 0.91-0.94).

Colorectal cancer mortality in Poland - analysis of regional variation.

INTRODUCTION: In 1999 in Poland 7,139 people died of colon cancer, while in 2008 this number rose to 9,915. Among malignant tumours, colorectal cancer is the second most commonly occurring one, frequently leading to death. The main reason for this is the fact that in 50% of patients with this cancer the illness is diagnosed at an advanced stage already. The risk increases significantly after 60 years of age. The aim of study was analysing the mortality of patients with colorectal cancer over 10 years in Poland (1999-2008), in both men and women from all provinces in the country. MATERIAL AND METHODS: The basis for the study was the number of deaths caused by colorectal cancer taking into account sex. Statistical data were drawn from the National Cancer Registry. RESULTS: In 1999 in Poland 3,706 men and 3,433 women died of colorectal cancer, while in 2008 the number of deaths stood at 5,385 and 4,530 respectively. In the years 1999-2008, colorectal cancer mortality rates among men were approximately 1.5 times higher than among women, and the majority of provinces demonstrate an upward trend. Among women the differences in the values of the coefficients are less clear. CONCLUSIONS: Early detection of cancer could significantly reduce mortality among patients with colon cancer. Screening for colorectal cancer and colonoscopy are tests that should permanently become a part of preventive measures aimed at detecting disease and teaching risk factors, particularly in males and people over 60 years of age.

Colorectal cancer morbidity in Poland and Japan in the years 1999-2006 - a comparison.

INTRODUCTION: The frequency of colorectal cancer (CRC) is dependent on sex and age. The illness more often affects men than women, and a considerable increase in morbidity is noted after 65 years of age. The aim of the study was to assess the influence of various risk factors on CRC morbidity, statistical data from countries varied in cultural, socioeconomic and biological terms need to be studied. Poland and Japan can serve as examples of such contrasts. MATERIAL AND METHODS: The basis for the analysis of CRC morbidity was statistical data from Poland and Japan gathered in the period 1999-2006. They were expressed in absolute numbers and were related to the total morbidity, as well as morbidity according to sex and age. RESULTS: In the years 1999-2006, the total morbidity in Japan was on average 2.3 times higher than in Poland. The value was 2.5 times higher among men and 2.1 times among women when compared to Poland. In both countries morbidity is closely related to age and it reaches a peak between 65 and 74 years of age. Although the change in morbidity over the period was the same for Poland and Japan, there are considerable differences concerning the sex of the patients. CONCLUSIONS: There is a substantial increase in CRC morbidity in both countries, especially among elderly people, which may point to the predominant influence of environmental factors and population aging in both countries. The much higher increase in morbidity among Polish men when compared to Polish women, not observed in the Japanese population, requires further study.

Incidence of colorectal cancer in Poland in 1999-2008.

INTRODUCTION: Malignant neoplasm of the colon is one of the most common gastrointestinal cancers and takes the second place in terms of incidence in the world. In Asian countries compared with Western countries the incidence is a bit lower. In recent years in Poland there has been a disturbing increase in the incidence of this cancer, particularly in the voivodships Mazowieckie, Slaskie, and Wielkopolskie. MATERIAL AND METHODS: Statistical data from the National Cancer Registry on the incidence of colorectal cancer in Poland in 1999-2008, including the provinces which are grouped into provinces of Eastern, Western and Central Poland. We analysed data on both men and women, with the division of colon cancer, rectal folds esico and rectum. The analysis took into account the recognized incidence in absolute numbers and age-standardized incidence rates. RESULTS: The incidence of colon cancer in 1999 was 3438 cases among men and 3476 women, while in 2008 this number increased in both men and women and for men was 4763, and 4340 for women. In all Polish provinces, in 1999, 2165 men and 1719 women, and in 2008, 3188 men and 2150 women suffered from rectal cancer. CONCLUSIONS: In the years 1999-2008 there was an increase in incidence of cancer of the colon. In Poland, there are territorial differences in the incidence of colorectal cancer described by the standardized incidence ratio. The incidence in Western and Central Poland is generally higher than for Eastern Poland. Probably, these differences have multiple bases.