Dihydroquinoline derivative as a potential anticancer agent: synthesis, crystal structure, and molecular modeling studies.

Cancer is one of the leading causes of death worldwide and requires intense and growing research investments from the public and private sectors. This is expected to lead to the development of new medicines. A determining factor in this process is the structural understanding of molecules with potential anticancer properties. Since the major compounds used in cancer therapies fail to encompass every spectrum of this disease, there is a clear need to research new molecules for this purpose. As it follows, we have studied the class of quinolinones that seem effective for such therapy. This paper describes the structural elucidation of a novel dihydroquinoline by single-crystal X-ray diffraction and spectroscopy characterization. Topology studies were carried through Hirshfeld surfaces analysis and molecular electrostatic potential map; electronic stability was evaluated from the calculated energy of frontier molecular orbitals. Additionally, in silico studies by molecular docking indicated that this dihydroquinoline could act as an anticancer agent due to their higher binding affinity with human aldehyde dehydrogenase 1A1 (ALDH 1A1). Tests in vitro were performed for VERO (normal human skin keratinocytes), B16F10 (mouse melanoma), and MDA-MB-231 (metastatic breast adenocarcinoma), and the results certified that compound as a potential anticancer agent. A Dihydroquinoline derivative was tested against three cancer cell lines and the results attest that compound as potential anticancer agent.

Echocardiographic parameters in dogs treated with acepromazine and fentanyl / Parâmetros ecocardiográficos em cães tratados com acepromazina e fentanil

Considering that the use of tranquillizers could optimize the performance of the echocardiogram, this study aimed to evaluate the effect of protocols with acepromazine and fentanyl on the echocardiographic parameters of healthy dogs, besides their effect in systolic blood pressure (SBP), respiratory rate (RR), heart rate (HR), time spent for examination and sedation scale. Ten adult dogs were submitted to different tranquilizing protocols 20 minutes before the echocardiographic examination, totalling five treatments for each pair, performed at seven-day intervals between evaluations. The treatments were CT (control treatment), IAT (intramuscular acepromazine), OAT (oral acepromazine), FT (fentanyl) and AFT (acepromazine associated with fentanyl). In addition to the echocardiographic evaluation, SBP, degree of reassurance, duration of the exam, HR and RR in the different protocols were evaluated. There was a significant decrease of SBP in OAT. There was a significant reduction in left ventricular diameter during systole and diastole and mitral annular movement in IAT, OAT and AFT, compared with CT. There was a decrease in tricuspid annular plane systolic excursion and increase in mitral E/mitral A ratio in IAT and OAT when compared with CT. All the tranquillizer protocols studied were found to significantly reduce HR, that facilitated the echocardiographic examination.(AU)

Considerando que o uso de tranquilizantes poderia otimizar a realização do ecocardiograma, objetivou-se com este estudo avaliar o efeito da tranquilização com acepromazina e fentanil sobre os parâmetros ecocardiográficos em cães saudáveis, bem como o efeito na pressão arterial sistólica (PAS), na frequência respiratória (FR), na frequência cardíaca (FC), no tempo gasto para a realização do exame e na escala de sedação. Dez cães adultos foram submetidos a diferentes protocolos tranquilizantes, 20 minutos antes da avaliação ecocardiográfica, totalizando cinco tratamentos para cada dupla, realizados com intervalos de sete dias entre as avaliações. Os tratamentos foram: TC (tratamento controle), TAI (acepromazina intramuscular), TAO (acepromazina oral), TF (fentanil) e TAF (acepromazina associada ao fentanil). Além dos parâmetros ecocardiográficos, foram avaliados a PAS, o grau de tranquilização, o tempo de duração do exame e a FC e a FR nos diferentes protocolos. Houve diminuição significativa da PAS no TAO. Observou-se redução significativa do diâmetro do ventrículo esquerdo em sístole e diástole e do movimento anular de mitral nos protocolos TAI, TAO e TAF, comparados com o TC. Observou-se também uma redução da excursão sistólica do plano anular tricúspide e aumento da relação mitral E/mitral A nos protocolos TAI e TAO quando comparados ao TC. Todos os protocolos de tranquilização reduziram significativamente a FC, o que facilitou a realização do exame.(AU)

Parâmetros ecocardiográficos em cães saudáveis tratados com acepromazina, meperidina e sua associação / Echocardiographic parameters in healthy dogs treated with acepromazine, meperidine and their association

Objetivou-se avaliar os efeitos da tranquilização com meperidina, acepromazina e de sua associação sobre os parâmetros ecocardiográficos em cães. Foram utilizados 12 cães adultos, da raça Rottweiler, submetidos ao exame ecocardiográfico sem utilização de sedação (controle - TC) e a três protocolos de tratamento, utilizando-se meperidina (TM), acepromazina (TA) e a associação dos medicamentos (TMA). As variáveis foram analisadas pelo teste de Tukey (P<0,05). Observou-se que as médias obtidas na onda A do fluxo mitral em TA e TMA diminuíram significativamente com relação ao TM, que não diferiu do TC. Houve uma diminuição significativa no valor de movimento anular mitral (MAM) e excursão sistólica do plano anular tricúspide (ESPAT) no TA. Não houve diferença significativa para os valores de fração de encurtamento (FE) entre TA e os demais tratamentos. Entretanto, observou-se que 57,3% dos cães apresentaram valores de FE abaixo da normalidade. As alterações encontradas podem ser decorrentes dos efeitos hipotensores da acepromazina utilizada de forma isolada. Conclui-se que a meperidina ou sua associação com acepromazina não alteram os parâmetros ecocardiográficos em cães saudáveis e que a acepromazina, utilizada isoladamente, causa alteração nos parâmetros de função sistólica dos cães, não sendo recomendada para a contenção química dos cães submetidos ao ecocardiograma, o que poderia levar à má interpretação do exame.(AU)

The aim of this study was to evaluate the effects of sedation with meperidine, acepromazine and its association on the echocardiographic parameters in dogs. Twelve adult Rottweilers were used and subjected to the echocardiography examination without the use of sedation (control - CT) and subjected to three treatment protocols using meperidine (MT), acepromazine (AT), and the combination of drugs (MAT). Variables were analyzed by Tukey test (p<0,05). The averages obtained in A-wave of mitral inflow in AT and MAT decreased significantly compared to MT, which did not differ from CT. There was a significant decrease in the measurement of mitral annulus motion (MAM) and tricuspid annular plane systolic excursion (TAPSE) at TA. There was no significant difference in shortening fraction (SF) values between TA and other treatments. However, it was observed that 57.3% of the dogs showed SF values below the normal range for the species. All changes found may be due to the hypotensive effects of acepromazine used in isolation. In conclusion, meperidine or its association with acepromazine does not alter echocardiographic parameters in healthy dogs and acepromazine, used alone, causes changes in the parameters of systolic function and is not recommended for sedation of dogs submitted to echocardiogram, since it could cause a misinterpretation of the exam.(AU)

Pectus carinatum in a dog / Pectus carinatum em um cão

Descreve-se o atendimento de um cão macho de cinco meses de idade, apresentando diversas malformações congênitas, incluindo uma protrusão ventral da parte distal do externo, que foi diagnosticada como Pectus carinatum tendo por base os achados clínicos e radiográficos.