Anti-leishmanial effect of spiro dihydroquinoline-oxindoles on volume regulation decrease and sterol biosynthesis of Leishmania braziliensis.

Diverse spiro dihydroquinoline-oxindoles (JS series) were prepared using the BF3•OEt2-catalyzed imino Diels-Alder reaction between ketimine-isatin derivatives and trans-isoeugenol. Ten spiro-oxiindole derivatives were selected and evaluated at different stages of the life cycle of Leishmania braziliensis parasites, responsible for cutaneous leishmaniasis in South America. Among them, the 8'-ethyl-4'-(4-hydroxy-3-methoxyphenyl)-3'-methyl-3',4'-dihydro-1'H-spiro[indoline-3,2'-quinolin]-2-one called JS87 was able to inhibit the growth of promastigotes without affecting the mammalian cells viability, and to decrease the number of intracellular amastigotes of L. braziliensis. This spiro compound was found to act through the alteration of parasite internal regulation by disrupting the regulatory volume decrease (RVD), and to affect the sterol biosynthetic pathway at level of squalene epoxidase (SE) enzyme. These results revealed that the spiro annulation between quinoline and oxindole scaffolds enhances the anti-leishmanial activity, and could assist in the development of potent quinoline-oxindole hybrids against Leishmania braziliensis, the main etiological agent of cutaneous leishmaniasis in South America.

Cascarilla de cacao venezolano como materia prima de infusiones / Husk of Venezuelan cocoa as raw material of infusions

En la industria del cacao se subutilizan materiales que pudieran ser ingredientes en la elaboración de productos novedosos, uno de ellos es la cascarilla de cacao. Estudios previos le atribuyen a dicho material una alta capacidad antioxidante, lo que sumado a su relativo bajo costo, lo hacen un atractivo ingrediente para la elaboración de infusiones, pero antes de promoverlo como tal, se necesita garantizar su calidad. En este estudio se evaluó la composición química, la calidad microbiológica de la cascarilla de cacao, así como también aquellos parámetros que determinan su uso como materia prima en la preparación de infusiones. Las semillas de cacao fueron cultivadas en dos estados en Venezuela. A la cascarilla de cacao se le determinó el contenido de humedad, proteínas, grasa, cenizas, carbohidratos, minerales, calidad microbiológica, ocratoxina A y las propiedades como antioxidante, contenido de materias extrañas, cenizas insolubles en HCL y extracto acuoso. Los métodos aplicados se basan en normas nacionales e internacionales. Se determinaron diferencias significativas entre las muestras mediante la aplicación de ANOVA. Un bajo contenido de humedad pero alto en cenizas, una calidad microbiológica ajustada a la norma y la ausencia de ocratoxina A se observaron en la totalidad de las muestras analizadas. El bajo contenido de materias extrañas y alto valor del extracto acuoso y alto contenido de polifenoles con actividad antioxidante permite recomendar la cascarilla del cacao como materia prima para preparar infusiones.

In the cocoa bean industry, some by-products go underutilized. Some of these components could provide other innovative products, and such is the case with the husk of the cocoa bean. Previous studies have attributed the husk with a high antioxidant capacity, which added to its relative low cost, makes it an attractive ingredient for the production of infusions. However, prior to promoting it as such, its quality needs to be guaranteed. This study evaluated the chemical composition of the husk of cocoa, its microbiologic quality and other parameters in order to be considered raw material in the preparation of infusions. The cocoa was cultivated in two different states in Venezuela. Moisture, protein, fat, ash, carbohydrates, microbiologic quality and ochratoxin A as well antioxidant properties, content of foreign matter, insoluble ash in HCL and aqueous extract were evaluated in the husk of cocoa seeds. Applied methods were in compliance with national and international norms. Significant differences were determined between the samples through the ANOVA application. A low level in moisture content, but high in ash, along with a microbiologic quality that met the norm, and an absence of ochratoxin A were observed in the totality of the analyzed samples. Low levels of foreign matter, the high value of its aqueous extract and high phenolic compounds content with antioxidant activity allow for the recommendation of the husk of cocoa as raw material for the preparation of infusions.

[Husk of Venezuelan cocoa as raw material of infusions]. / Cascarilla de cacao venezolano como materia prima de infusions.

In the cocoa bean industry, some by-products go underutilized. Some of these components could provide other innovative products, and such is the case with the husk of the cocoa bean. Previous studies have attributed the husk with a high antioxidant capacity, which added to its relative low cost, makes it an attractive ingredient for the production of infusions. However, prior to promoting it as such, its quality needs to be guaranteed. This study evaluated the chemical composition of the husk of cocoa, its microbiologic quality and other parameters in order to be considered raw material in the preparation of infusions. The cocoa was cultivated in two different states in Venezuela. Moisture, protein, fat, ash, carbohydrates, microbiologic quality and ochratoxin A as well antioxidant properties, content of foreign matter, insoluble ash in HCL and aqueous extract were evaluated in the husk of cocoa seeds. Applied methods were in compliance with national and international norms. Significant differences were determined between the samples through the ANOVA application. A low level in moisture content, but high in ash, along with a microbiologic quality that met the norm, and an absence of ochratoxin A were observed in the totality of the analyzed samples. Low levels of foreign matter, the high value of its aqueous extract and high phenolic compounds content with antioxidant activity allow for the recommendation of the husk of cocoa as raw material for the preparation of infusions.