Free 2-propen-1-amine Derivative And Inclusion Complexes With β-cyclodextrin: Scanning Electron Microscopy, Dissolution, Cytotoxicity And Antimycobacterial Activity

Inclusion complexes and physical mixtures of isomeric mixture of E/Z (50:50) of 3-(4′-bromo-[1,1′-biphenyl]-4-yl)-3-(4-bromophenyl)-N,N- dimethyl-2-propen-1-amine (BBAP) and β-cyclodextrin (β-CD) in the molar proportion of 1:1 and 1:2 were analyzed by scanning electron microscopy. The dissolution behavior of BBAP and of the inclusion complexes were also evaluated for six hours. By scanning electron microscopy (SEM), it was possible to observe an inclusion complex formed between BBAP and β-CD by co-evaporation, either in the molar proportion of 1:1 or 1:2. In the physical mixtures, no complex was observed as previously detected by physicochemical analysis. The dissolution studies showed that the inclusion complexes BBAP/β-CD 1:1 and 1:2 released respectively 49.07 ± 1.48 and 40.26 ± 3.90% of BBAP during six hours. Free BBAP was less soluble than the inclusion complex and reached 9.00 ± 0.75% of dissolution. Biological assays, such as cytotoxicity to J774 macrophages and to a permanent lung fibroblast cell line (V79), indicated that the BBAP does not exhibit any additional toxic effect with the β-CD complexes. However, the complexes were less cytotoxic to V79 cells than the free form. The BBAP/β-CD inclusion complexes were more effective (MIC) than the free compound on several mycobacteria strains. Similar behavior was observed for BBAP/β-CD complexes and rifampicin, a front-line antitubercular drug, on M. tuberculosis H37Rv growing inside J774 macrophages.155682689Bibby, D.C., Davies, N.M., Tucker, I.G., (2000) Int. J. Pharm., 197, p. 1De Souza, A.O., Sato, D.N., Aily, D.C.G., Durán, N., (1998) J. Antimicrob. Chemother., 42, p. 407Pereira, D.G., De Castro, S.L., Durán, N., (1998) Acta Tropica, 69, p. 205De Souza, A.O., Santos Júnior, R.R., Ferreira-Júlio, J.F., Rodrigues, J.A., Melo, P.S., Haun, M., Sato, D.N., Durán, N., (2001) Eur. J. Med. Chem., 36, p. 843De Souza, A.O., Hemerly, F.P., Busollo, A.C., Melo, P.S., Machado, G.M.C., Miranda, C.C., Santa-Rita, R.M., Durán, N., (2002) J. Antimicrob. Chemother., 50, p. 629De Conti, R., Gimenez, S.M.N., Haun, M., Pilli, R.A., De Castro, S.L., Durán, N., (1996) Eur. J. Med. Chem., 31, p. 915De Souza, A.O., Santos Jr., R.R., Sato, D.N., Lima, H.O.S., Andrade-Santana, M.H., Alderete, J.B., Faljoni-Alario, A., Durán, N., (2000) Abstracts of the 29 a Reunião Anual Da Sociedade Brasileira de Bioquímica, , Caxambu, BrazilHiguchi, T., Connors, K.A., (1965) Adv. Anal. Chem. Instrum., 4, p. 117Collins, L.A., Franzblau, S.G., (1997) Antimicrob. Agents Chemother., 41, p. 1004Oh, Y.K., Nix, D.E., Straubinger, R.M., (1995) Antimicrob Agents Chemother., 39, p. 2104Cingi, M.R., De Angelis, I., Fortunati, E., Reggiani, D., Bianchi, V., Tiozzo, R., Zucco, F., (1991) Toxicol. In Vitro, 5, p. 119Denizot, F., Lang, R., (1986) J. Immun. Methods, 89, p. 271Borenfreund, E., Puerner, J.A., (1984) J. Tiss. Cult. Meth., 9, p. 7Melo, P.S., Maria, S.S., Vidal, B.C., Haun, M., Durán, N., (2000) In Vitro Cell Rev. Biol. Animal, 36, p. 539Melo, P.S., Durán, N., Haun, M., (2001) Toxicology, 159, p. 135Shrivastava, R., John, G.W., Rispat, G., Chevalier, A., Massingham, R., (1991) ATLA - Alt. Lab. Anim., 19, p. 39

Evolution of the use of corticosteroids for the treatment of hospitalised COVID-19 patients in Spain between March and November 2020: SEMI-COVID national registry

Objectives: Since the results of the RECOVERY trial, WHO recommendations about the use of corticosteroids (CTs) in COVID-19 have changed. The aim of the study is to analyse the evolutive use of CTs in Spain during the pandemic to assess the potential influence of new recommendations. Material and methods: A retrospective, descriptive, and observational study was conducted on adults hospitalised due to COVID-19 in Spain who were included in the SEMI-COVID- 19 Registry from March to November 2020. Results: CTs were used in 6053 (36.21%) of the included patients. The patients were older (mean (SD)) (69.6 (14.6) vs. 66.0 (16.8) years; p < 0.001), with hypertension (57.0% vs. 47.7%; p < 0.001), obesity (26.4% vs. 19.3%; p < 0.0001), and multimorbidity prevalence (20.6% vs. 16.1%; p < 0.001). These patients had higher values (mean (95% CI)) of C-reactive protein (CRP) (86 (32.7-160) vs. 49.3 (16-109) mg/dL; p < 0.001), ferritin (791 (393-1534) vs. 470 (236- 996) µg/dL; p < 0.001), D dimer (750 (430-1400) vs. 617 (345-1180) µg/dL; p < 0.001), and lower Sp02/Fi02 (266 (91.1) vs. 301 (101); p < 0.001). Since June 2020, there was an increment in the use of CTs (March vs. September; p < 0.001). Overall, 20% did not receive steroids, and 40% received less than 200 mg accumulated prednisone equivalent dose (APED). Severe patients are treated with higher doses. The mortality benefit was observed in patients with oxygen saturation </=90%. Conclusions: Patients with greater comorbidity, severity, and inflammatory markers were those treated with CTs. In severe patients, there is a trend towards the use of higher doses. The mortality benefit was observed in patients with oxygen saturation </=90%

Registro ACESUR: atención de pacientes adultos con crisis epilépticas en servicios de urgencias: diferencias entre primer episodio y recurrencia

Objetivo. Describir las características y la atención recibida de pacientes adultos que consultan por crisis epiléptica (CE) en los servicios de urgencias hospitalarios (SUH), diferenciando entre primera crisis y recurrencia en epiléptico conocido. Método. ACESUR es un registro observacional de cohortes multipropósito, prospectivo y multicéntrico con un muestreo sistemático, los días pares de febrero y julio alternando con los impares de abril y octubre de 2017. Se incluyeron pacientes 18 años con diagnóstico de CE en los SUH. Se recogieron variables clínico-asistenciales de la visita índice de pacientes, distinguiendo entre primera CE y recurrencia en epiléptico. Resultados. El registro ACESUR recogió a 664 pacientes procedentes de 18 SUH españoles, 229 (34, 5%) con primera CE y 435 (65, 5%) con CE recurrentes. Los pacientes con primera CE fueron de mayor edad (p < 0, 001), presentaron motivos de consulta distintos (p < 0, 001) y requirieron más traslados en ambulancia (p < 0, 001). La atención recibida en el SUH fue diferente, en pacientes con primera CE se solicitó con mayor probabilidad una prueba complementaria específica (OR ajustada = 13, 94; IC95%:7, 29-26, 7; p < 0, 001) y se necesitó mayor hospitalización o estancia prolongada en el SUH (OR ajustada = 1, 69; IC95%:1, 11-2, 58; p = 0, 015). No hubo diferencias en cuanto al tratamiento farmacológico en fase aguda ni preventivo (OR ajustada = 1, 40; IC95%:0, 94-2, 09; p = 0, 096). Se inició tratamiento con fármacos antiepiépticos (FAE) en 100 pacientes (43, 7%) tras primera CE y se reinició o modificó añadiendo nuevo FAE en 142 pacientes (32, 6%) con CE recurrentes. Conclusiones. Las características clínicas y la atención recibida de pacientes adultos con primera CE en SUH en España difieren de las recurrencias en epiléptico conocido. Objective. To describe the characteristics of care received by patients who come to the emergency department with a first epileptic seizure versus a recurrent seizure in a patient with diagnosed epilepsy. Methods. ACESUR (Acute Epileptic Seizures in the Emergency Department) is a prospective multicenter, multipurpose registry of cases obtained by systematic sampling on even days in February and July 2017 and on odd days in April and October 2017. Patients were aged 18 years or older and had an emergency department diagnosis of epileptic seizure. We recorded clinical variables and details related to care given during each patient''s visit, including whether the event was a first or recurrent seizure. Results. A total of 664 patients attended by 18 Spanish emergency departments were entered into the ACESUR registry. Two hundred twenty-nine (34.5%) were first seizures and 435 (65.5%) were recurrences. Patients who were attended for first seizures were older, consulted for a wider variety of reasons, and were transported in ambulances (P<.001, all comparisons). Care received differed between patients with first seizures versus recurrent seizures. Specific complementary testing was more likely in patients with first seizures (adjusted odds ratio [aOR], 13.94; 95% CI, 29-26.7; P<.001), and they were more often hospitalized or stayed longer in the emergency department, (aOR, 1.69; 95% CI, 1.11-2.58; P=.015). Pharmacologic treatment did not differ between the groups, either in the acute phase or for prevention (aOR, 1.40; 95% CI, 0.94-2.09; P=.096). Antiepileptic drugs were given to 100 patients (43.7%) after a first seizure and were restarted or changed in 142 patients with recurrent seizure (32.6%). Conclusions. The clinical characteristics of adults attended for a first epileptic seizure differ from those of patients with diagnosed epilepsy who were attended for recurrent seizures in Spain. The care received also differs

Mapping local patterns of childhood overweight and wasting in low- and middle-income countries between 2000 and 2017

A double burden of malnutrition occurs when individuals, household members or communities experience both undernutrition and overweight. Here, we show geospatial estimates of overweight and wasting prevalence among children under 5 years of age in 105 low- and middle-income countries (LMICs) from 2000 to 2017 and aggregate these to policy-relevant administrative units. Wasting decreased overall across LMICs between 2000 and 2017, from 8.4 (62.3 (55.1�70.8) million) to 6.4 (58.3 (47.6�70.7) million), but is predicted to remain above the World Health Organization�s Global Nutrition Target of <5 in over half of LMICs by 2025. Prevalence of overweight increased from 5.2 (30 (22.8�38.5) million) in 2000 to 6.0 (55.5 (44.8�67.9) million) children aged under 5 years in 2017. Areas most affected by double burden of malnutrition were located in Indonesia, Thailand, southeastern China, Botswana, Cameroon and central Nigeria. Our estimates provide a new perspective to researchers, policy makers and public health agencies in their efforts to address this global childhood syndemic. © 2020, The Author(s)

Author Correction: Mapping local patterns of childhood overweight and wasting in low- and middle-income countries between 2000 and 2017 (Nature Medicine, (2020), 26, 5, (750-759), 10.1038/s41591-020-0807-6)

An amendment to this paper has been published and can be accessed via a link at the top of the paper. © 2020, The Author(s)

Author Correction: Mapping local patterns of childhood overweight and wasting in low- and middle-income countries between 2000 and 2017 (Nature Medicine, (2020), 26, 5, (750-759), 10.1038/s41591-020-0807-6)

An amendment to this paper has been published and can be accessed via a link at the top of the paper. © 2020, The Author(s)

Por trás das pelagens dos equídeos – Revisão de Literatura

Coat color is the name given to the color of the sum of the coat of the skin, fur, mane, tail and extremity of horses and is used mainly to identify them. The objective was to carry out this literature review on the genetics of coats and peculiarities of equines to avoid economic losses in production and expand the horse’s agribusiness. The coat is determined by several genes and pairs of alleles that will influence the distribution of melanocytic cells and the type of pigment. There are two types of pigments that give rise to equine coats, eumelanin and pheomelanin. These pigments are regulated by the activation or inactivation of the surface receptor on the melanocyte called MC1R and by the action of surface receptors encoded by the extension locus and agouti locus. From the action of pigments, other modifying and diluting genes can act, originating the variations of coats. The particularities of depigmented skin and white hair are explained by independent mutations in the MITF and PAX3 genes, and variants in the EDNRB and KIT genes. When the KIT and MITF loci act together, there is an increase in the extent of depigmented particularities in the phenotype. The genetic study of coats is necessary for the correct identification of horses, as well as avoiding diseases and economic losses and helping to expand the horse’s agribusinessPelagem é o nome dado à coloração do somatório do revestimento da pele, pelo, crina, cauda e extremidade dos equídeos e é utilizada principalmente para identifica-los. Objetivou-se realizar essa revisão de literatura sobre a genética das pelagens e particularidades dos equídeos visando evitar perdas econômicas na produção e expandir o agronegócio do cavalo. A pelagem é determinada por diversos genes e pares de alelos que irão influenciar a distribuição das células melanocíticas e no tipo de pigmento. Existem dois tipos de pigmentos que dão origem as pelagens dos equídeos, a eumelanina e a feomelanina. Esses pigmentos são regulados pela ativação ou inativação do receptor de superfície no melanócito denominado MC1R e pela atuação dos receptores de superfície codificados pelo locus extension e locus agouti. A partir da atuação dos pigmentos, outros genes modificadores e diluidores podem atuar originando as variações de pelagens. As particularidades de pele despigmentada e pelos brancos são explicadas por mutações independentes nos genes MITF e PAX3, e variantes nos genes EDNRB e KIT. Quando há atuação conjunta dos loci KIT e MITF, ocorre um aumento na extensão das particularidades despigmentadas no fenótipo. O estudo genético das pelagens é necessário para correta identificação dos equinos, assim como evitar doenças e perdas econômicas e auxiliar na expansão do agronegócio do caval