Isolation and X-ray crystal structure of tetrahydroisoquinoline alkaloids from Calycotome villosa Subsp. intermedias

Two tetrahydroisoquinoline alkaloids were extracted from the alkaloid fraction of a methanol extract of the seeds of Calycotome Villosa Subsp. intermedia. Their structures were established as (R)-1-hydroxymethyl-7-8-dimethoxy-1,2,3,4-tetrahydro- isoquinoline (1) and (S)-7-hydroxymethyl-2-3-dimethoxy-7,8,9,10-tetrahydroisoquinoline chloride (2) by spectroscopic techniques and X-ray diffraction analysis

Diammonium tris­[hexa­aqua­magnesium(II)] tetra­kis­[hydrogenphosphate(III)], (NH4)2[Mg(H2O)6]3(HPO3)4

The framework of the title compound is made up of discrete Mg(H2O)6 octa¬hedra, and HPO3 and NH4 tetra¬hedra, which are organized in planes parallel to (010). Strong hydrogen bonding between the building units stabilizes the structure. The hydrogenphosphate(III) tetra¬hedra, the ammonium tetra¬hedron and one of the two Mg atoms lie on positions with m symmetry, whereas the second Mg atom is located on a position with 2/m symmetry

In vitro and in vivo studies of the trypanocidal activity of four terpenoid derivatives against Trypanosoma cruzi.

Four terpenoid derivatives were examined for their activity against Trypanosoma cruzi. Our results show that two compounds were very active in vitro against both extra- and intracellular forms. These compounds, non-toxic for the host cells, are more effective than the reference drug benznidazole. The capacity to infect cells was negatively affected and the number of amastigotes and trypomastigotes was reduced. A wide range of ultrastructural alterations was found in the epimastigote forms treated with these compounds. Some metabolic changes occurred presumably at the level of succinate and acetate production, perhaps caused by the disturbance of the enzymes involved in sugar metabolism inside the mitochondria. In vivo results were consistent with those observed in vitro. The parasitic load was significantly lower than in the control assay with benznidazole. The effects of these products showed the reduction of the anti-T. cruzi antibodies level during the chronic stage

Síntesis de compuestos bioactivos a partir de ácidos diterpénicos

Tesis Univ. Granada. Departamento de Química Orgánica. Leída el 25 de mayo de 200

Procedimiento para la preparación de merosesquiterpenos y compuestos relacionados a partir de diterpenos labdánicos

Número de publicación: ES2327196 B2. Número de solicitud: 200800837.Procedimiento para la preparación de merosesquiterpenos a partir de diterpenos labdánicos. La presente invención describe un procedimiento para la obtención de merosesquiterpenos, más concretamente drimenilbencenos y drimenilnaftoquinonas, mediante una reacción Diles Alder entre un diterpeno labdánico y un dienófilo. A continuación una deshidrogenación conduce a los derivados aromatizados.Universidad de Granad

Diammonium tris­[hexa­aqua­magnesium(II)] tetra­kis­[hydrogenphosphate(III)], (NH4)2[Mg(H2O)6]3(HPO3)4

The framework of the title compound is made up of discrete Mg(H2O)6 octa¬hedra, and HPO3 and NH4 tetra¬hedra, which are organized in planes parallel to (010). Strong hydrogen bonding between the building units stabilizes the structure. The hydrogenphosphate(III) tetra¬hedra, the ammonium tetra¬hedron and one of the two Mg atoms lie on positions with m symmetry, whereas the second Mg atom is located on a position with 2/m symmetry

Meroxest improves the prognosis of immunocompetent C57BL/6 mice with allografts of E0771 mouse breast tumor cells.

Recently, we have reported the antitumor properties of a new family of synthetic merosesquiterpenes, among which meroxest is highlighted, since it has high activity and specificity for ER+ breast cancer cells. In this paper, we characterize allografts of ER+ E0771 mouse breast tumor cells in immunocompetent C57BL/6 mice, and also analyze the effect of meroxest on the prognosis of the disease. Twenty female C57BL/6 mice were injected with 106 E0771 cells. Once the tumors reached the appropriate size, the mice were divided into two groups, one control and another treated orally with 15 mg/kg of meroxest. After 20 days, tumor samples were taken for histopathological study and for determination of the expression of the prognostic markers Ki67 and vascular endothelial growth factor (VEGF) by immunofluorescence. In sections stained with hematoxylin-eosin, we observed that tumors have a well-defined capsule enclosing E0771 tumor cells. The central area of tumors contains necrotic regions with leukocyte infiltration. Meroxest treatment significantly reduces tumor size (68%, p Meroxest improves the prognosis of mice since it reduces leukocyte infiltration, and decreases the expression of Ki67 and VEGF markers. Consequently, the merosesquiterpene could become a useful antiangiogenic drug in the treatment of breast cancer. These results encourage us to deepen the study of meroxest, in order to find more evidence that supports the convenience of its evaluation in a clinical study or trial

Análogos sintéticos de merosesquiterpenos y compuestos relacionados con actividad antitumoral

Número de publicación: ES2355786 B1. Número de solicitud: 201050019.La invención se refiere a las propiedades antitumorales frente a tumores sólidos, tales como los cánceres de mama, neuroblastomas, pulmón, colorrectal, hepático y páncreas tanto en humanos como en animales, de compuestos sintéticos que presentan una estructura merosesquiterpénica relacionada con los metabolitos marinos del tipo puupehenona.Universidad de GranadaUniversidad de Jaé