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OBJECTIVES: This study focuses on analyzing the impact of innovative human resource management practices (IHRMP) on knowledge worker burnout, and how organizational support and employee effort help explain this relationship in the context of the business services sector. To explore the problem, investigated whether IHRMP have a significant negative impact on employee burnout, and organizational support and employee effort mediate the negative impact of IHRMP on employee burnout. MATERIAL AND METHODS: A survey was conducted, collected using the computer assisted web interview method on 1000 knowledge workers employed at business services sector (BSS) organizations in Poland. The quantitative results obtained were analyzed using AMOS software to test the main statistical relationships and through structural equation modeling. RESULTS: The study outlines direct and indirect mechanisms to counteract perceived burnout among knowledge workers. The article contributes to the understanding of how IHRMP reduce burnout among knowledge workers and highlights the central importance of organizational support and employee effort as mediating factors against burnout in the context of high-skill, high-intensity work. CONCLUSIONS: The expected results in terms of application provide a proposal of measures for managers' consideration that can be implemented in the organization with a view to counteracting the incidence of burnout among BSS employees. Int J Occup Med Environ Health. 2024;37(2):220-33.
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Esgotamento Profissional , Humanos , Polônia , Esgotamento Profissional/psicologia , Esgotamento Profissional/epidemiologia , Esgotamento Profissional/prevenção & controle , Masculino , Feminino , Adulto , Inquéritos e Questionários , Pessoa de Meia-Idade , Cultura Organizacional , Comércio , Satisfação no EmpregoRESUMO
BACKGROUND: There are many current scientific reports on the synthesis of various derivatives modelled on the structure of known small-molecular and natural bioactive compounds. Curcuminoid chalcones are an innovative class of compounds with significant therapeutic potential against various diseases and they perfectly fit into the current trends in the search for new biologically active substances. AIM: The aim of this study was to design and synthesise a series of curcuminoid chalcones. OBJECTIVE: The objective of this scientific paper was to synthesise twelve curcuminoid chalcones and confirm their structures using spectral methods. Additionally, the biological activity of three of the synthesised compounds was evaluated using various assays, and their anticancer properties and toxicity were studied. METHODS: The proposed derivatives were obtained via the Claisen-Schmidt reaction of selected acetophenones and aldehydes in various conditions using both classical methods: the solutions and solvent-free microwave (MW) or ultrasound (US) variants. The most optimal synthetic method for the selected curcuminoid chalcones was the classical Claisen-Schmidt condensation in an alkaline (NaOH) medium. Spectral methods were used to confirm the structures of the compounds. The resazurin reduction assay, caspase-3 activity assay, and RT-qPCR method were performed, followed by measurements of the intracellular reactive oxygen species (ROS) level and the lactate dehydrogenase (LDH) release level. RESULTS: Twelve designed curcuminoid chalcones were successfully synthesized and structurally confirmed by NMR, MS, and IR spectroscopy. Examination of the anticancer activity was carried out for the three most interesting chalcone products. CONCLUSION: The results suggested that compound 3a increased the metabolism and/or proliferation of the human colon carcinoma (Caco-2) cell line, while compounds 3b and 3f showed significant toxicity against the Caco-2 cell line. Overall, the preliminary results suggested that compound 3b exhibited the most favorable anticancer activity.
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The COVID-19 pandemic provoked a global health crisis and highlighted the need for new therapeutic strategies. In this study, we explore the potential of the molecular consortia of cannabidiol (CBD) and non-steroidal anti-inflammatory drugs (NSAIDs) as novel antiviral dual-target agents against SARS-CoV-2/COVID-19. CBD is a natural compound with a wide range of therapeutic activities, including antiviral and anti-inflammatory properties, while NSAIDs are commonly used to mitigate the symptoms of viral infections. Chemical modifications of CBD with NSAIDs were performed to obtain dual-target agents with enhanced activity against SARS-CoV-2. The synthesised compounds were characterised using spectroscopic techniques. The biological activity of three molecular consortia (CBD-ibuprofen, CBD-ketoprofen, and CBD-naproxen) was evaluated in cell lines transduced with vesicular stomatitis virus-based pseudotypes bearing the SARS-CoV-1 or SARS-CoV-2 spike proteins or infected with influenza virus A/Puerto Rico/8/34. The results showed that some CBD-NSAID molecular consortia have superior antiviral activity against SARS-CoV-1 and SARS-CoV-2, but not against the influenza A virus. This may suggest a potential therapeutic role for these compounds in the treatment of emerging coronavirus infections. Further studies are needed to investigate the efficacy of these compounds in vivo, and their potential use in clinical settings. Our findings provide a promising new approach to combatting current and future viral emergencies.
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Sonodynamic therapy (SDT) is a non-invasive therapeutic modality in cancer treatment that combines low-intensity ultrasound (US) and sonosensitizers. Tumor cells are destroyed through the synergistic effects of ultrasound and a chemical sonosensitizer. This study focused on the synthesis and in vitro evaluation of the sonodynamic effect of natural curcumin, triterpene oleanolic acid, and their semi-synthetic derivatives on tongue cancer SCC-25 and hypopharyngeal FaDu cell lines. The combination of the tested compounds with sonication showed a synergistic increase in cytotoxicity. In the group of oleanolic acid derivatives, oleanoyl hydrogen succinate (6) showed the strongest cytotoxic effect both in the SCC-25 and FaDu cell lines. Comparing curcumin (4) and its pyrazole derivative (5), curcumin showed a better cytotoxic effect on SCC-25 cells, while curcumin pyrazole was more potent on FaDu cells. The highest sonotherapeutic activity, compared to its individual components, was demonstrated by a structural linker mode hybrid containing both curcumin pyrazole-oleanoyl hydrogen succinate units within one complex molecule (7). This study can be beneficial in the context of new perspectives in the search for effective sonosensitizers among derivatives of natural organic compounds.
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Curcumin and oleanolic acid are natural compounds with high potential in medicinal chemistry. These products have been widely studied for their pharmacological properties and have been structurally modified to improve their bioavailability and therapeutic value. In the present study, we discuss how these compounds are utilized to develop bioactive hybrid compounds that are intended to target cancer cells. Using a bifunctional linker, succinic acid, to combine curcumin and triterpenoic oleanolic acid, several hybrid compounds were prepared. Their cytotoxicity against different cancer cell lines was evaluated and compared with the activity of curcumin (the IC50 value (24 h), for MCF7, HeLaWT and HT-29 cancer cells for KS5, KS6 and KS8 compounds was in the range of 20.6-94.4 µM, in comparison to curcumin 15.6-57.2 µM). Additionally, in silico studies were also performed. The computations determined the activity of the tested compounds towards proteins selected due to their similar binding modes and the nature of hydrogen bonds formed within the cavity of ligand-protein complexes. Overall, the curcumin-triterpene hybrids represent an important class of compounds for the development of effective anticancer agents also without the diketone moiety in the curcumin molecule. Moreover, some structural modifications in keto-enol moiety have led to obtaining more information about different chemical and biological activities. Results obtained may be of interest for further research into combinations of curcumin and oleanolic acid derivatives.
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The aim of this article is to identify the relationship between the fulfilment of relational and transactional psychological contracts and work results, taking into account the mediation effect expressed in organisational identification. The empirical research was conducted on a group of 402 HR professionals responsible for designing and implementing HR practices in one of the leading companies of the Polish energy sector. Hypotheses were tested using the partial least squares structural equation modelling technique (PLS-SEM). Based on our research, we found that the implementation of both relational and transactional psychological contracts positively influenced the results achieved by HR professionals, both directly and indirectly, through the mediating role of organisational identification. The results indicate that the relationship between the psychological contract and work results is stronger when mediated by organisational identification. It plays an important role, especially in relation to the transactional contract. The collected results lead to the conclusion that organisations, wishing to increase the level of work results achieved by HR professionals, should as much as possible fulfil the expectations of employees and meet the commitments made to them within the framework of the established psychological contract. The study makes an important contribution to the understanding of the "priority" importance of organisational identification in enhancing the efforts of HR professionals to deliver work results that benefit both employees and the organisation.
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Contratos , Satisfação Pessoal , OrganizaçõesRESUMO
An increasing proportion of new medicinal substances are poorly soluble in water. Adsorption on mesoporous silicas increases their bioavailability when administered orally. Loading method determines adsorption either on the surface in crystalline state or inside the mesopores in amorphus form. The aim of this study was to compare two methods (adsorption equilibrium and solvent evaporation) of lornoxicam adsorption on SBA-15 and APTES-modified SBA-15 in terms of drug adsorption site. Additionally, we investigated the drug release profiles at different pH and cytotoxicity of the analysed mesoporous materials. The materials were characterized by a number of physicochemical techniques including X-ray diffraction, nitrogen adsorption/desorption techniques, differential scanning calorimetry, thermogravimetric analysis, scanning and transmission electron microscopy, infrared spectroscopy and 1H NMR. Lornoxicam was loaded on the studied materials and released in the media (HCl pH 1.2, phosphate buffers pH 6.8 and 7.4). The cytotoxicity assays of APTES-modified SBA-15 were performed on CaCo-2 human colon cancer cell line. We proved that adsorption equilibrium method is a more advantageous method of loading. It ensures drug adsorption in an amorphous state inside the mesopores. The solvent evaporation method, despite a greater amount of loaded drug, results in drug adsorption in a crystalline state on the silica surface. In drug release studies a greater amount of lornoxicam is released from modified materials compared to crystalline lornoxicam. Cytotoxicity study proved the safety of APTES-modified silica. We concluded that APTES-modified SBA-15 is applicable as an effective and non-toxic carrier for the poorly soluble drug lornoxicam. The adsorption equilibrium method should be the preferred loading method. It enables the adsorption of sparingly soluble substances inside the mesoproes and enhances bioavailability of oral pharmaceutical forms.
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Portadores de Fármacos , Dióxido de Silício , Adsorção , Células CACO-2 , Portadores de Fármacos/química , Humanos , Piroxicam/análogos & derivados , Porosidade , Dióxido de Silício/química , Solubilidade , Difração de Raios XRESUMO
Triterpenes are a wide and important group of compounds that have several promising pharmacological properties, such as hepatoprotective, anti-inflammatory, anti-HIV, antioxidant, or anticancer activities. Such potent substances can be successfully incorporated in more complex chemical systems e.g. codrugs or pro-drugs that have a better pharmacological profile. The codrug is connected with a drug formation pathway to chemically cohere at least two drug molecules to improve positive therapeutic efficiency or decrease side effects. The codrug can be cleaved in the organism to generate effective compounds previously used as substrates. This article presents an overview of codrugs that consist of pentacyclic triterpene moiety that is chosen as a basic codrug moiety due to their wide range of vital activities and another drug molecule fragment. It was found that triterpenoid codrugs are characterized by a wide range of biological activities. However, most of them have anticancer potency.
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Triterpenos Pentacíclicos/farmacologia , Animais , Humanos , Triterpenos Pentacíclicos/metabolismo , Pró-Fármacos/metabolismoRESUMO
At the end of 2019, a novel virus causing severe acute respiratory syndrome to spread globally. There are currently no effective drugs targeting SARS-CoV-2. In this study, based on the analysis of numerous references and selected methods of computational chemistry, the strategy of integrative structural modification of small molecules with antiviral activity into potential active complex molecules has been presented. Proposed molecules have been designed based on the structure of triterpene oleanolic acid and complemented by structures characteristic of selected anti-COVID therapy assisted drugs. Their pharmaceutical molecular parameters and the preliminary bioactivity were calculated and predicted. The results of the above analyses show that among the designed complex substances there are potential antiviral agents directed mainly on SARS-CoV-2.
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Antivirais/farmacologia , Betacoronavirus/efeitos dos fármacos , Infecções por Coronavirus/tratamento farmacológico , Reposicionamento de Medicamentos , Pneumonia Viral/tratamento farmacológico , Antivirais/química , COVID-19 , Fármacos Cardiovasculares/química , Fármacos Cardiovasculares/farmacologia , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Ácido Oleanólico/química , Ácido Oleanólico/farmacologia , Pandemias , SARS-CoV-2RESUMO
Increasingly stringent regulations aimed at protection of the natural environment have stimulated the search for new synthetic methodologies in organic and medicinal chemistry having no or minimum harmful effect. An interesting approach is the use of alternative activation factors, microwaves (MW) or ultrasounds (US) and also their cross-combination, which has been tested in the fast and efficient creation of new structures. At present, an easy and green hybrid strategy ("Lego" chemistry) is generally recommended for the design of new substances from different chemistry building blocks. Often, selected biologically active components with specific chemical reactivities are integrated by a suitably designed homo- or heterodifunctional linker that modifies the functionality of the starting structure, allowing easy covalent linkage to another molecule. In this study, a fast introduction of heterodifunctional halogenoacidic linker to selected mono-, di- and triphenolic active substances, allowing their functionalization, was investigated. Nucleophilic substitution reaction was chosen to produce final ethers with the reactive carboxylic group from phenols. The functionalization was performed using various green factors initiating and supporting the chemical reactions (MW, US, MW-US). The benefits of the three green supporting methods and different conditions of reactions were analyzed and compared with the results of the reaction performed by conventional methods.
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Preparações Farmacêuticas/síntese química , Fenóis/química , Química Farmacêutica , Química Verde , Micro-Ondas , Preparações Farmacêuticas/química , UltrassomRESUMO
The design and discovery of novel drug candidates are the initial and most probably the crucial steps in the drug development process. One of the tasks of medicinal chemistry is to produce new molecules that have a desired biological effect. However, even today the search for new pharmaceuticals is a very complicated process that is hard to rationalize. Literature provides many scientific reports on future prospects of design of potentially useful drugs. Many trends have been proposed for the design of new drugs containing different structures (dimers, heterodimers, heteromers, adducts, associates, complexes, biooligomers, dendrimers, dual-, bivalent-, multifunction drugs and codrugs, identical or non-identical twin drugs, mixed or combo drugs, supramolecular particles and various nanoindividuals. Recently much attention has been paid to different strategies of molecular hybridization. In this paper, various molecular combinations were described e.g., drug-drug or drug-non-drug combinations which are expressed in a schematic multi-factor form called a molecular matrix, consisting of four factors: association mode, connection method, and the number of elements and linkers. One of the most popular trends is to create small-small molecule combinations such as different hybrids, codrugs, drug-drug conjugates (DDCs) and small-large molecule combinations such as antibody-drug conjugates (ADCs), polymer-drug conjugates (PDCs) or different prodrugs and macromolecular therapeutics. A review of the structural possibilities of active framework combinations indicates that a wide range of potentially effective novel-type compounds can be formed. What is particularly important is that new therapeutics can be obtained in fast, efficient, and selective methods using current trends in chemical synthesis and the design of drugs such as the "Lego" concept or rational green approach.
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Química Click/métodos , Técnicas de Química Combinatória/métodos , Descoberta de Drogas/métodos , Pró-Fármacos/síntese química , Pró-Fármacos/químicaRESUMO
BACKGROUND: The influence of subjective perception of occupational stress and its individual factors on the overall level of job satisfaction was analyzed. The respondents were also asked to answer the question of the potential differences in terms of variables in managers and non-managers, and in various demographic factors. MATERIAL AND METHODS: This article presents the results of a study conducted among 5930 people employed in 3 units of the examined public sector institution. The research was conducted using computer-assisted web interview method. The parameters of the polynomial model of ordered categories were estimated. RESULTS: The results showed a statistically significant effect between the variables and the differences between the groups of subjects. Analyzes showed slight differences between men and women. Employees with a low level of stress and high job satisfaction were noted in the oldest group, aged over 55 years, and in managers. Low levels of stress and job satisfaction were observed in young employees with the shortest period of employment. Among those least satisfied with the work and experiencing high levels of stress there were respondents with 6-15 years of employment in non-managerial positions. While the highest levels of stress and high satisfaction were found in people aged 46-55 years, with more than 20 years of work experience. CONCLUSIONS: The results of the estimation of the polynomial model parameters of ordered categories indicate that the level of perceived stress is related to the level of job satisfaction. The lower the level of stress and stressors in the workplace, the greater the job satisfaction in the surveyed unit. Med Pr 2018;69(3):301-315.
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Emprego/psicologia , Satisfação no Emprego , Estresse Ocupacional/psicologia , Setor Público , Local de Trabalho/psicologia , Adulto , Fatores Etários , Emprego/estatística & dados numéricos , Feminino , Humanos , Relações Interpessoais , Masculino , Pessoa de Meia-Idade , Estresse Ocupacional/epidemiologia , Satisfação Pessoal , Polônia , Apoio Social , Local de Trabalho/estatística & dados numéricos , Adulto JovemRESUMO
The reactivity of 1,2-benzoxathiin-4(3H)-one 2,2-dioxide was studied in multicomponent type reactions for the first time, namely, in a three-component interaction with active methylene nitriles and aromatic aldehydes in order to construct condensed 2-amino-4H-pyran derivatives. The reaction outcome strongly depended on the nature of an active methylene nitrile and an arenecarbaldehyde. Application of malononitrile resulted in novel 2-amino-4-aryl-4H-pyrano[3,2-c][1,2]benzoxathiine-3-carbonitrile 5,5-dioxides in most cases, whereas the utilization of ethyl cyanoacetate resulted in a complex mixture of products. In the last case, three different products were isolated depending on the arenecarbaldehyde used, namely ethyl 2-amino-4-aryl-4H-pyrano[3,2-c][1,2]benzoxathiine-3-carboxylate 5,5-dioxides, ethyl 2-cyano-3-arylacrylates, and salts of 3,3'-(arylmethylene)bis(4-hydroxybenzo[e][1,2]oxathiine 2,2-dioxides). Attempts to obtain separately ethyl 2-amino-4-aryl-4H-pyrano[3,2-c][1,2]benzoxathiine-3-carboxylate 5,5-dioxides enabled us to propose reaction pathways leading to these products. The salts were obtained for the first time. The preparative method for the synthesis of triethylammonium salts of 3,3'-(arylmethylene)bis(4-hydroxybenzo[e][1,2]oxathiine 2,2-dioxides) was proposed by the direct interaction of 1,2-benzoxathiin-4(3H)-one 2,2-dioxide with arenecarbaldehydes. The application of ammonium acetate as a catalyst allowed us to synthesize 7-aryl-7,14-dihydrobenzo[5,6][1,2]oxathiino[4,3-b]benzo[5,6][1,2]oxathiino[3,4-e]pyridine 6,6,8,8-tetraoxides containing a novel heterocyclic system. These facts, combined with our past investigations, allowed us to assert that the reactivity of enol nucleophiles that include the COCH2SO2X fragment has not been reported previously.
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The current study focuses on the synthesis of several hybrid individuals combining a natural oleanolic acid skeleton and synthetic nonsteroidal anti-inflammatory drug moieties (NSAIDs). It studied structural modifications of the oleanolic acid structure by use of the direct reactivity of hydroxyl or hydroxyimino groups at position C-3 of the triterpenoid skeleton with the carboxylic function of anti-inflammatory drugs leading to new perspective compounds with high potential pharmacological activities. Novel ester- and iminoester-type derivatives of oleanolic unit with the different NSAIDs, such as ibuprofen, aspirin, naproxen, and ketoprofen, were obtained and characterized. Moreover, preliminary research of compounds obtaining structure stability under acidic conditions was examined and the PASS method of prediction of activity spectra for substances was used to estimate the potential biological activity of these compounds.
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Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios/química , Inflamação/tratamento farmacológico , Ácido Oleanólico/química , Anti-Inflamatórios/síntese química , Anti-Inflamatórios não Esteroides/síntese química , Aspirina/química , Aspirina/uso terapêutico , Humanos , Ibuprofeno/química , Ibuprofeno/uso terapêutico , Cetoprofeno/química , Cetoprofeno/uso terapêutico , Estrutura Molecular , Naproxeno/química , Naproxeno/uso terapêutico , Ácido Oleanólico/síntese químicaRESUMO
Taking the rising interest in jasmone structure based fragrant compounds into account it has been decided to take up an attempt to synthesize the new heterocyclic derivatives of this 2,3-disubstituted cyclopentenone, which could be characterized by the ability of interaction with the same receptors with which jasmone affects. Obtained structures of unsaturated heterocyclic derivatives are based on pyrrolidinone, oxazolidinone, pyrazolidinone, pyrazolone and thiazolidinone systems with 2-double or 2-triple unsaturated five-carbon side chain. The rapid, highly yielding and ecofriendly microwave assisted organic syntheses (MAOS) have been used to obtain compounds mentioned above. Odor evaluation and relationships between their structure and osmic properties for all synthesized fragrant compounds have been studied. It has been shown that the majority of the obtained compounds have exhibited interesting, very intensive and fixative fragrant properties.
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Ciclopentanos/síntese química , Compostos Heterocíclicos/química , Micro-Ondas , Oxilipinas/síntese química , Perfumes/síntese química , Ciclopentanos/química , Temperatura Alta , Cinética , Odorantes/análise , Oxilipinas/química , Perfumes/químicaRESUMO
The authors describe a case of 21-years old woman with idiopathic pulmonary arterial hypertension with atypical clinical consequences of massive internal bleeding. Despite significant hypovolemia clinical and laboratory presentation was one of RV failure with dilatation of right heart ventricle and increased plasma level of markers of myocardial stretch and injury (NT-proBNP and troponin, respectively). This is attributed to impaired right ventricular coronary perfusion and hypoxia. Intensive treatment restored baseline RV conditions and at 15 months follow-up no persistent right heart impairment was observed. This case demonstrates that bleeding should be also considered in differential diagnosis of exacerbation of right ventricular failure in patients with pulmonary arterial hypertension.
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Insuficiência Cardíaca/diagnóstico , Insuficiência Cardíaca/etiologia , Hipertensão Pulmonar/complicações , Hipertrofia Ventricular Direita/etiologia , Disfunção Ventricular Direita/etiologia , Adulto , Biomarcadores/sangue , Feminino , Insuficiência Cardíaca/sangue , Hemoperitônio/diagnóstico , Hemoperitônio/etiologia , Humanos , Hipertrofia Ventricular Direita/sangue , Hipertrofia Ventricular Direita/diagnóstico , Peptídeo Natriurético Encefálico/sangue , Fragmentos de Peptídeos/sangue , Troponina T/sangue , Disfunção Ventricular Direita/sangue , Disfunção Ventricular Direita/diagnósticoRESUMO
cis-Jasmone, from jasmonoid group, is an important jasmine odor fragrance compound. The syntheses of new heterocyclic analogues of jasmone were described. Five analogues of this compound were prepared under microwave irradiation and the results of the microwave assisted syntheses were compared with classical, thermally initiated reactions in solvent. Microwave reactions were carried out successfully, and reaction times were significantly reduced to a few minutes. Three of five obtained analogues, pyrrolidinone, oxazolidinone and thiazolidinone demonstrated an interesting, specific odor which was compared with floral, typical jasmine odor of jasmone.
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Ciclopentanos/química , Ciclopentanos/síntese química , Micro-Ondas , Ciclização , Ciclopentanos/farmacologia , Humanos , Estrutura Molecular , Odorantes , OxilipinasRESUMO
A case of 63-years old man suffering from CTEPH and chronic renal failure due to diabetic nephropathy is presented. First diagnosis of pulmonary hypertension was made at the beginning of 2000. Then the secondary anticoagulant prophylaxis were introduced. Despite such treatment there was no improvement and level of pulmonary hypertension increased. Finally, the pulmonary thrombectomy was considered because of proximal location of thromboembolic obstruction in pulmonary artery. Before surgery, the hemodialysis was started. Pulmonary thrombendarterectomy along with right coronary artery bypass grafting were performed in November 2001. The procedure was conducted successfully. The patient's condition improved and pulmonary pressure dropped substantially. During follow-up anticoagulant prophylaxis and hemodialysis are continued. It might be conducted that pulmonary thrombendarterectomy can be successfully performed also in patients with complex coexisting conditions.