Pharmacological evaluation of phenylcarbamic acid derivatives on cardiovascular functions in rats

Four phenylcarbamic acid derivatives, 1 (1-(4-fluorophenyl)-4-[3-(4-methoxyphenylcarbamoyloxy)-2-hydroxypropyl]piperazinium chloride, 2 (1-(2-methylphenyl)-4-[3-(4-methoxyphenylcarbamoyloxy)-2-hydroxypropyl]piperazinium chloride), 3 (1-(2-methylphenyl)-4-[3-(4-ethoxyphenylcarbamoyloxy)-2-hydroxypropyl]piperazinium chloride) and 4 (1-(3-trifluoromethylphenyl)-4-[3-(4-methoxyphenylcarbamoyloxy)-2-hydroxypropyl]piperazinium chloride) were investigated for their ability to affect various cardiovascular functions and to establish their chemical structure-biological activity relationship. The compounds were evaluated for their antiarrhythmic efficacy using ouabain-induced rhythm disturbances and the ability to inhibit the positive chronotropic effect of isoproterenol in isolated atria of Wistar rats. Electrocardiogram (ECG) parameters in isolated hearts of spontaneously hypertensive rats (SHR) perfused according to the Langendorff method and ability to decrease phenylephrine-induced contraction of the aortic strips after repeated administration of the compounds were also analyzed. Only compound 3 delayed significantly the evaluated parameter of arrhythmogenicity and was able to antagonize the isoproterenol-induced positive chronotropic effect in normotensive rats’ atria. Similarly, in SHR rats, only compound 3 was able to decrease heart frequency significantly without influencing the duration of QT (time between the start of the Q wave and the end of the T wave) and QTc (frequency corrected QT) intervals. The evaluated endothelial function was improved after administration of compound 2. Fluorine-containing structures (1 and 4) were less effective compared to 2´-methylphenylpiperazine derivatives (2 and 3). The latter two compounds showed suitable efficacy, which supported their use for futher pharmacological research

Investigating the activity spectrum for Ring-Substituted 8-Hydroxyquinolines

In this study, a series of fourteen ring-substituted 8-hydroxyquinoline derivatives were prepared. The synthesis procedures are presented. The compounds were analyzed using RP-HPLC to determine lipophilicity. They were tested for their activity related to inhibition of photosynthetic electron transport (PET) in spinach (Spinacia olerácea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial strains and against eight fungal strains. Several compounds showed biological activity comparable with or higher than the standards isoniazid or fluconazole. For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds are discussed

The impact of diagnosis on the psychosocial and spiritual needs of the patients

Introduction: Holistic care focuses on the relationship between the body, mind, and spirit. Spiritual needs are among the basic needs of the individual. From the physical and spiritual dimension and the interaction of these two dimensions, the spiritual needs of the person are developed. Aim:The aim of our study was to analyze if the patient's knowledge regarding their diagnosis and possible proximity of death have significant impact on satisfaction of psychological and spiritual needs. Material and Methods:In our study we used standardized questionnaire The Spiritual Needs Assessment for Patient – SNAP constructed by Sharma Rashmi, applied for 113 respondents and processed by SPSS statistical program. Results:Reliability of questionnaire is given by Cronbach's Alpha 0.945 for the total SNAP. A statistically significant difference at the level p < 0.01 has been confirmed in all questions among respondents with fatal diagnosis and respondents with not life-threatening diagnosis. In domain of psychosocial needs, significant difference was not confirmed regarding to gender, age, education, income, religion and place of residency. In domain of spiritual needs, significant difference was partially confirmed regarding religion in 4 questions from 13. Conclusion:Faced with chronic or fatal diseases, many patients rely on dealing with spiritual and religious issues. In fact, spirituality/religiosity can be considered an important source of support and management of severe chronic diseases. It is possible to identify the four basic dimensions of spiritual need: interconnection, peace, meaning/purpose, and transcendence. Patients often have the problem addressing their needs for related psychosocial and physical problems such as physical disability, fatigue, sleep disorders, side effects of treatment, etc. Importance of satisfaction of psychosocial and spiritual needs is increased in time of threat, fatal diagnosis

Coping with death and awareness of mortality in patients and their relatives

The aim of our study was to analyze the attitudes of people – patients and their relatives in proximity of death and dying. End-stage of human life is often associated with changes in the scale of values and needs of the individual. Particular attention was paid to the needs and values that are associated with recognition of limitations concerning to earthly life, but also with the hope of eternal life. Generally, people think that the feelings and coping with death and dying are same in patients and their relatives. The truth is that coping with death and mortality is individual to each person. The problems related to the dying should be coped with by all: dying patients, their relatives and friends. Dying is not letting cold those who are in the presence of dying. In our study we used Acceptation of Dying and Coping with Mortality Questionnaire – 20 Items (ADCMQ20). Research sample consisted of 275 respondents: 95 dying patients and 180 their relatives. All data were processed by SPSS 24 statistical program

Rapid Drop in Coronary Heart Disease Mortality in Czech Male Population—What Was Actually behind It?

The high mortality of coronary heart disease (CHD) among Czech men—one of the highest worldwide—began to decline in 1991 soon after the abolition of government subsidies to all foodstuffs rich in animal fat. As participants in the WHO MONICA Project, we were able to analyze the CHD risk factors just before and after this major economic change. We had previously documented that the originally subsidized prices decreased animal fat consumption and consequently non-HDL cholesterol concentrations in the population. By the early 1990s, no progress had been made in the treatment of acute myocardial infarction, statins were unavailable as was not the currently more effective antihypertensive therapy. Our recent research proved a close relationship between cholesterolemia and proinflammatory macrophages in adipose tissue and accelerated macrophage polarization with increased palmitate and palmitoleate contents in cell membrane phospholipids. By contrast, the proportion of proinflammatory macrophages decreases with increasing presence of n-3 fatty acids in the cell membrane. The combination of non-HDL cholesterol drop and a decreased proportion of proinflammatory macrophages due to replacement of alimentary fat decreased CHD mortality immediately

Bragg concentrators for hard (> 10 keV) X-ray astronomy: Status report

The use of focusing telescopes in hard X-ray (E > 10 keV) astronomy will provide better flux sensitivity and imaging perfomances with respect to the directviewing detectors, utilized until now. We present recent results obtained from our Group regarding the possible use of Bragg-diffraction technique to design hard X-ray focusing telescopes

Pharmacological Evaluation of the Effects of Phenylcarbamic Acid Derivatives on Cardiovascular Functions in Rats

Four phenylcarbamic acid derivatives, (1-(4-fluorophenyl)- 4-[3-(4-methoxyphenylcarbamoyloxy)-2-hydroxypropyl]piperazinium chloride (1), (1-(2-methylphenyl)-4-[3-(4-methoxyphenylcarbamoyloxy)- 2-hydroxypropyl]piperazinium chloride) (2), (1-(2-methylphenyl)-4-[3-(4-ethoxyphenylcarbamoyloxy)- 2-hydroxypropyl]piperazinium chloride) (3) and (1-(3-trifluoromethylphenyl)-4-[3-(4-methoxyphenylcarbamoyloxy)- 2-hydroxypropyl]piperazinium chloride) (4) were investigated for their ability to affect various cardiovascular functions and to establish their chemical structure-biological activity relationship. The compounds were evaluated for their antiarrhythmic efficacy using ouabain-induced rhythm disturbances and the ability to inhibit the positive chronotropic effect of isoproterenol in isolated atria of Wistar rats. Electrocardiogram (ECG) parameters in isolated hearts of spontaneously hypertensive rats (SHR) perfused according to the Langendorff method and ability to decrease phenylephrine- -induced contraction of the aortic strips after repeated administration of the compounds were also analyzed. Only compound 3 delayed significantly the evaluated parameter of arrhythmogenicity and was able to antagonize the isoproterenol- induced positive chronotropic effect in normotensive rats’ atria. Similarly, in SHR rats, only compound 3 was able to decrease heart frequency significantly without influencing the duration of QT (time between the start of the Q wave and the end of the T wave) and QTc (frequency corrected QT) intervals. The evaluated endothelial function was improved after administration of compound 2. Fluorine-containing structures (1 and 4) were less effective compared to 2´-methylphenylpiperazine derivatives (2 and 3). The latter two compounds showed suitable efficacy, which supported their use for futher pharmacological research