C-6α- vs C-7α-Substituted Steroidal Aromatase Inhibitors: Which Is Better? Synthesis, Biochemical Evaluation, Docking Studies, and Structure-Activity Relationships

C-6α and C-7α androstanes were studied to disclose which position among them is more convenient to functionalize to reach superior aromatase inhibition. In the first series, the study of C-6 versus C-7 methyl derivatives led to the very active compound 9 with IC50 of 0.06 μM and Ki = 0.025 μM (competitive inhibition). In the second series, the study of C-6 versus C-7 allyl derivatives led to the best aromatase inhibitor 13 of this work with IC50 of 0.055 μM and Ki = 0.0225 μM (irreversible inhibition). Beyond these findings, it was concluded that position C-6α is better to functionalize than C-7α, except when there is a C-4 substituent simultaneously. In addition, the methyl group was the best substituent, followed by the allyl group and next by the hydroxyl group. To rationalize the structure–activity relationship of the best inhibitor 13, molecular modeling studies were carried out

Coronavirus Disease 2019: Quick Diet and Nutrition Guide for Patients With Chronic Kidney Disease.

Considering the Covid-19 pandemic and that patients with CKD are included in a high-risk group, a quick nutrition guide for patients with CKD in all stages was developed, and it is available in Portuguese at https://bit.ly/2zfSjl0, in English at https://bit.ly/covid19ckd, in Spanish at https://bit.ly/guia enfermedad renal and in French at https://bit.ly/covid19maladierenale

Hipertensão porta na esquistossomose mansônica: repercussões do tratamento cirúrgico no perfil histomorfométrico da mucosa gástrica Portal hypertension in mansonic schistosomiasis: profile of the gastric mucosa

Investigou-se, através da análise digital de imagens, as repercussões do tratamento cirúrgico para controle da hipertensão porta e seus efeitos na vasculatura gástrica de pacientes jovens portadores de esquistossomose mansônica. Foram incluídos no estudo pacientes no pré-operatório (n=5) e grupos de pacientes submetidos à intervenção cirúrgica, em diferentes períodos (0-2 anos, n=04; 2-6 anos, n=13; acima de 6 anos, n=10). Foram obtidas biópsias endoscópicas da mucosa do antro e corpo gástrico, submetidas à rotina histológica e montadas em blocos de parafina. Confeccionaram-se lâminas histológicas que foram usadas para a análise histomorfométrica dos seguintes parâmetros: número médio de vasos por campo, diâmetro médio e espessura da parede dos vasos. Os resultados obtidos evidenciaram uma diminuição significativa da densidade e do diâmetro dos vasos a partir dos dois anos de pós-operatório até o período superior a 6 anos. Os dados dão suporte ao conceito de que a técnica cirúrgica ministrada ameniza, em longo prazo, as alterações histopatológicas específicas, como a hemorragia e a ectasia.<br>The repercussions from surgical treatment for controlling portal hypertension and its effects on the gastric vasculature of young patients with mansonic schistosomiasis were investigated by digital image analysis. The study included five patients at the preoperative stage and 27 patients who had undergone surgical intervention at different times in the past: 0-2 years ago, n=4; 2-6 years ago, n=13, and more than 6 years ago, n=10. Endoscopic biopsies were taken from the mucosa of the gastric antrum and body endoscopic mucosa and the samples underwent routine histological tests after embedding in paraffin blocks. Histological thin sections were used for histomorphometric analysis of the following parameters: mean number of vessels per field, and mean diameter and thickness of the vessel walls. The results showed that, between the patients whose operation was not more than two years ago and those whose operation was more than six years ago, there was a significant decrease in the density and diameter of the vessels. These findings give support to the concept that the surgical treatment administered decreases specific histological alterations like hemorrhage and ectasia, over the long term