Research advance on structure and function of amides in Zanthoxylum plants / 中国中药杂志

Zanthoxylum belongs to the Rutaceae family, and there are 81 Zanthoxylum species and 36 varieties in China. Most of the Zanthoxylum plants are used as culinary spice. In recent years, scholars in China and abroad have carried out in-depth research on Zanthoxylum plants, and found that the peculiar numbing sensation of Zanthoxylum plants originates from amides. It is also determined that amides are an important material basis for exerting pharmacological effects, especially in anti-inflammatory analgesia, anesthesia and other aspects. In this paper, 123 amides in 26 Zanthoxylum plants and their pharmacological activity that have been reported were summarized, which provided scientific reference for the clinical application of Zanthoxylum plants and the research and development of new drugs, and also facilitated the sustainable development and utilization of Zanthoxylum plant resources.

Nivel de autoconcepto en niños con secuelas de quemaduras: estudio comparativo / Self-concept level in children with burns sequelae: A comparative study

Introducción: Autoconcepto es el conjunto de ideas y actitudes que se tiene acerca de sí mismo. Nuestro objetivo fue evaluar si existen diferencias en el nivel de autoconcepto de niños de 8-12 años con y sin secuelas de quemaduras, e identificar variables predictoras del autoconcepto en los niños con secuelas. Pacientes y método: Estudio comparativo, transversal de 109 niños con secuelas de quemaduras de 8 a 12 años de edad, con 109 niños sin secuelas de quemaduras, del mismo grupo de edad y nivel socioeconómico. Se utilizó la escala de autoconcepto de Piers-Harris, que entrega medida de autoconcepto general y dimensiones: conductual, estatus intelectual y escolar, apariencia y atributos físicos, ansiedad, popularidad, felicidad y satisfacción. Resultados: No hubo diferencias significativas en el nivel de autoconcepto general ni en sus dimensiones al comparar ambos grupos (p > 0,05). Dentro del grupo con secuelas de quemaduras la variable número de secuelas resultó ser un factor protector para las dimensiones ansiedad, popularidad, felicidad-satisfacción y autoconcepto general. La variable localización surgió como factor de riesgo para la dimensión conductual. Discusión: La ausencia de diferencias en autoconcepto entre niños con secuelas de quemaduras y sin ellas es similar a lo reportado por la literatura. El hallazgo en factores de riesgo y protectores motiva a continuar investigando, incorporando antecedentes premórbidos y familiares.

Introduction: Self-concept is the set of ideas and attitudes that a person has about him/herself. Objective: To evaluate whether there are differences in the level of self-concept in children 8-12 years old with and without burns sequelae. To identify predictive variables of self-concept in children with sequelae. Patients and method: A comparative cross-sectional study of self-concept in 109 children with burns sequelae, from 8 to 12 years old, with 109 children without burns sequelae, and of the same age and socioeconomic status. The Piers-Harris self-concept scale is used, which provides a general measurement of self-concept and behavioural, intellectual and school status, appearance, and physical attributes, anxiety, popularity, happiness and satisfaction dimensions. Results: There were no significant differences in the level of general self-concept or their dimensions (P > .05). In the group with burns sequelae, the protective factor was the variable number of sequels was associated with the dimensions of anxiety, popularity, happiness-satisfaction and general self-concept. The location variable emerged as a risk factor for the behavioural dimension. Discussion: The absence of differences in self-concept between children with burns sequelae and children without them is similar to that reported in the literature. The finding in the risk and protective factors encourages to further research, and perhaps incorporating pre-morbidity and family background.

Aliskiren: a novel renin inhibitor for hypertension.

Hypertension is one of the major causes of cardiovascular morbidity. Most patients who are on treatment for hypertension fail to achieve adequate control with the existing therapy and rates of cardiovascular morbidity remain high. As the renin-angiotensin-aldosterone system is strongly implicated in the development of hypertension-related target organ damage, intensive efforts have been devoted towards the development of drugs targeting this system. In addition to angiotensin converting enzyme inhibitors and angiotensin receptor blockers, inhibition of renin has also become a clinical reality. Aliskiren, a novel renin inhibitor, has overcome a number of shortcomings of existing drugs and is now available to address angiotensin production directly at its rate-limiting step.

Exploring QSAR of peripheral benzodiazepine receptor binding affinity of N,N-dialkyl-2-phenylindol-3-yl-glyoxylamides using physico-chemical descriptors.

The present QSAR study has attempted to explore the structural and physicochemical requirements of ligands N,N-dialkyl-2-phenylindol-3-yl-glyoxylamides for binding with peripheral benzodiazepine receptor (PBR). The calculated partition coefficient values show parabolic relations with the PBR binding affinity, suggesting that the binding affinity increases with increase in the partition coefficient of the compounds until it reaches the critical value after which the affinity decreases. The critical value of logP is within range of 6.052-6.410. Furthermore, positive Wang-Ford.charge values of carbonyl oxygens of the glyoxamide moiety and negative Wang-Ford charge value of the glyoxamide nitrogen are conducive for the binding affinity. Again, the indole moiety should have favorable charge distribution. Higher values of the parameters dipole moment (Dipole) and moment of inertia (I_z) of the ligands are conducive for the binding affinity. The presence of hydrogen atom at R2 and cyclic moiety at R1 and R2 positions are detrimental to the binding affinity.

Resolución del racemato antiepiléptico DL-2-hidroxi, 2-etil-fenil acetamida / Resolution of the recemic antiepileptic DL-2-Hydroxy-2-Ethyl-2-Phenyl acetamide

La distribución espacial de los grupos en un fármaco puede influir tanto en su actividad biológica como en su naturaleza química, por lo que es necesario resolver las mezclas racémicas de los nuevos fármacos para poder establecer si existe diferencia en la actividad farmacológica o en la toxicidad de sus estereoisómeros. En este trabajo se describe la resolución del racemato antiepiléptico (ñ)-HEPA, para lo cual se sintetizaron las sales diasteroeméricas de quinina del ácido 2-hidroxi, 2-etil, 2-fenil acético, se recristalizaron con etanol y su tratamiento con ácido sulfúrico concentrado liberó los ácidos ópticamente activos. La a 20º D del ácido dextrorrotatorio fue + 32.6º en agua, mientras que la correspondiente al ácido levorrotatorio fue -23.43º en agua. Este último se esterificó con metanol y el tratamiento del éster con amoniaco produjo la (+)-HEPA con a 20º D = + 10.71º en acetona

Colorimetric and fluorimetric assay of azintamide in pharmaceutical formulations

Simple, accurate and sensitive colorimetric and fluorimetric methods are described for the determination of the choleretic drug azintamide. The colorimetric methods are based on thionine formation, a blue colored compound, absorbing maximally at 600 nm. Thionine is formed by heating acidic azintamide solution with zinc powder in presence of p-phenylenediamine and then addition of iron [3] ammonium sulfate solution. The fluorimetric method is based on measurement of the previously formed thionine after extraction with n-butanol at 550 and 620 nm excitation and emission wave lengths, respectively. The colorimetric and fluorimetric methods were applicable over the concentration ranges of 50-250 and 10-50 ug ml-1, respectively. These methods were further applied for analysis of azintamide in pharmaceutical preparations and the results were in agreement with those obtained from direct UV spectrophotometric method