α, β amyrin (ABAM) is a natural mixture of pentacyclic triterpenes that has a wide range of biological activities. ABAM is isolated from the species of the Burseraceae family, in which the species Protium is commonly found in the Amazon region of Brazil. The aim of this work was to develop inclusion complexes (ICs) of ABAM and β-cyclodextrin (βCD) and hydroxypropyl-β-cyclodextrin (HPβCD) by physical mixing (PM) and kneading (KN) methods. Interactions between ABAM and the CD’s as well as the formation of ICs were confirmed by physicochemical characterization in the solid state by Fourier transform infrared (FTIR), scanning electron microscopy (SEM), X-ray diffraction (XRD), thermogravimetry (TG) and differential scanning calorimetry (DSC). Physicochemical characterization indicated the formation of ICs with both βCD and HPβCD. Such ICs were able to induce changes in the physicochemical properties of ABAM. In addition, the formation of ICs with cyclodextrins showed to be an effective and promising alternative to enhance the anti-inflammatory activity and safety of ABAM.
Using readily available preallylated aldehydes, we report a simple and divergent synthesis of cyclic (alkyl)(amino)carbene (CAAC) iminium precursors. Using a combination of crystallographic data and steric maps, we further elaborate on the specific steric properties of CAAC ligands with respect to state-of-the-art phosphine and carbene ligands.
α,β-amyrenone (ABAME) is a triterpene derivative with many biological activities; however, its potential pharmacological use is hindered by its low solubility in water. In this context, the present work aimed to develop inclusion complexes (ICs) of ABAME with γ- and β-cyclodextrins (CD), which were systematically characterized through molecular modeling studies as well as FTIR, XRD, DSC, TGA, and SEM analyses. In vitro analyses of lipase activity were performed to evaluate possible anti-obesity properties. Molecular modeling studies indicated that the CD:ABAME ICs prepared at a 2:1 molar ratio would be more stable to the complexation process than those prepared at a 1:1 molar ratio. The physicochemical characterization showed strong evidence that corroborates with the in silico results, and the formation of ICs with CD was capable of inducing changes in ABAME physicochemical properties. ICs was shown to be a stronger inhibitor of lipase activity than Orlistat and to potentiate the inhibitory effects of ABAME on porcine pancreatic enzymes. In conclusion, a new pharmaceutical preparation with potentially improved physicochemical characteristics and inhibitory activity toward lipases was developed in this study, which could prove to be a promising ingredient for future formulations.
Background In remote islands lack of specialized medical facilities, long distance transfer and emergency medical system organization remains a challenge and fibrinolysis is necessary to achieve revascularization in optimal timing in ST-elevation myocardial infarction (STEMI) patients. Our angioplasty center is the only one located in an archipelago composed of nine islands, six of which do not have hospital facilities and only have small family health care units. Purpose To evaluate the reality and outcomes of our interventional angioplasty center and compare cardiovascular outcomes between STEMI patients from the main island and remote islands. Methods We retrospectively evaluated 103 patients with STEMI admitted to our center between 2018 and 2019. Patients from the main island where the center is located underwent primary percutaneous coronary intervention (PCI) (group 1, n=55) and patients from remote islands underwent fibrinolytic therapy followed by transference to our center with facilitated or rescue PCI (group 2, n=48). A subanalysis of the far remote islands without hospital facilities was also performed. Primary outcome was defined as cardiovascular death or re-infarction at two years and secondary outcome as intrahospital haemorrhagic complications. Results Mean age was 58,15±12,6 years, 85,4% were males and follow up period was 30,30±6,46 months. Seventy-eight patients (75,7%) had history of smoking, 45 (43,7%) dyslipidemia, 20 (19,4%) previous acute coronary syndrome, 18 (17,5%) diabetes and 17 (15,5%) were obese. Troponin I peak was 117,42±129,06 ug/L and 14 (13,6%) were in Killip Class III/IV. Infarct-related artery was the left anterior descending artery in 45 (45,5%) and multivessel disease was present in 38 (38,0%). In group 1 reperfusion after PCI was obtained in 91,5%. In group 2, 73,5% met criteria for reperfusion after fibrinolysis and 23,6% after rescue PCI. Mean time from fibrinolysis to PCI was 558±349 minutes. Rates of successful revascularization did not differ between groups, as well as complete patency of the culprit-vessel defined as thrombolysis in myocardial infarction (TIMI) flow 3 (91,5% vs. 97,2% and 90,0% vs. 93,0% respectively for group 1 and 2). Cardiovascular death at two years occurred in 4 (3,9%) patients and re-infarction in 11 (10,7%) and were similar between groups (3 (5,5%) vs. 1 (2,1%) and 8 (14,5%) vs. 3 (6,3%) respectively) as well as haemorrhagic complications (1 (1,8%) vs. 5 (10,4%) respectively). Nineteen (18,4%) patients were from far remote islands without hospital facilities and when comparing these patients with the others there was also no difference in primary outcome. Conclusion Even in remote islands, an organized STEMI network with attempted fibrinolytic treatment and coordinated transference of patients for facilitated or rescue PCI can provide successful revascularization with cardiovascular outcomes similar to those submitted to primary PCI. FUNDunding Acknowledgement Type of funding sources: None.
IntroduçãoA estenose ou oclusão de veia central é um problema comum nos pacientes com insuficiência renal crônica e geralmente está relacionada ao uso prévio de cateteres 1 . A incidência do problema tem sido relatada na literatura como presente em 25 a 40% dos pacientes em hemodiálise 2 . Essas lesões comumente são muito rígidas e de difícil recanalização quando ocluídas, de forma que quando se tornam sintomáticas podem levar a edema do membro homolateral ao acesso arteriovenoso ou edema da face 1 . Opções terapêuticas disponíveis são: ligadura da fístula arteriovenosa, intervenção cirúrgica com criação de uma ponte veno-venosa ou abordagem endovascular com angioplastia transluminal percutânea da lesão estenótica com ou sem a colocação de stent 1 . Apesar de não existirem estudos na literatura que indiquem a superioridade do stent em relação à angioplastia com balão, há claramente um grupo de pacientes que não é responsivo somente a este tipo de angioplastia, necessitando ResumoA estenose de veia central é uma das situações mais frequentes em pacientes com insuficiência renal crônica em hemodiálise. A angioplastia com o uso de stent-graft tem obtido bons resultados nestes casos. O sistema de liberação dos stents é de calibre maior, podendo dificultar sua navegabilidade em áreas de estenose ou tortuosidade acentuadas. A técnica do varal é comumente utilizada para o tratamento endovascular do aneurisma de aorta, permitindo atingir bom mecanismo de estiramento e facilitando a navegação do sistema de entrega da endoprótese. Descrevemos o caso de uma angioplastia de veia central com stent-graft na qual foi utilizada a técnica do varal para permitir a transposição da área de estenose.Palavras-chave: derivação arteriovenosa cirúrgica; angioplastia; diálise renal. AbstractThe central vein stenosis is one of the most common conditions in patients with chronic kidney failure in a hemodialysis program. In these cases, angioplasty using stent-grafts has obtained good results. The stent-graft delivery system is generally of large diameter what can hinder its navigability in very severe stenosis or tortuosities. The through-and-through technique is commonly used for endovascular treatment of aortic aneurysms, making possible to achieve a good mechanism of stretch and easy navigation of the endograft delivery system. We report a case of a central venous stenosis in wich a stent-graft was inserted using the through-and-through technique in order to cross the lesion.
We present a case of a patient with Crawford type IV aortic thoracoabdominal aneurysm. The patient underwent hybrid repair in two stages. Initially a Dacron graft was implanted surgically with revascularization of all visceral branches from the left external iliac artery (debranching). On a later date, the second stage of treatment was with an endovascular technique with bi aorto-iliac endoprosthesis. After 2 years the patient remains asymptomatic and in full working activity.Keywords: aortic aneurysm; surgery; aorta; aneurysm. ResumoApresentamos o caso de um paciente com aneurisma aórtico tóraco-abdominal tipo IV de Crawford submetido à correção híbrida em dois estágios. Inicialmente submetido a implante cirúrgico de prótese de Dacron com revascularização de todos os ramos viscerais a partir da ilíaca externa esquerda (debranching) e, posteriormente, tratado pela técnica endovascular com endoprótese aorto bi-ilíaca. Após dois anos, o paciente permanece assintomático e em plena atividade laborativa.
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