Quiste epidermoide testicular: diagnóstico ecográfico preoperatorio y correlación radiopatológica / Testicular epidermoid cyst. preoperative ultrasound diagnosis and radiopathological correlation

The low incidence of testicular epidermoid cyst (1-2 percent of all testicular tumors), makes ultrasound findings the key to making, or at least suggesting, a precise preoperative diagnosis, thus making a conservative treatment possible. We present two cases with ultrasound diagnosis of epidermoid cyst, confirmed later after surgery. We review the literature, emphasizing the evaluation of the ultrasound images and their correlation with the anatomopathological findings.

La escasa incidencia del quiste epidermoide de testículo (1-2 por ciento de todos los tumores testiculares), hace de los hallazgos ecográficos la clave para realizar o al menos sugerir un diagnóstico prequirúrgico preciso, haciendo por tanto posible un tratamiento conservador. Presentamos dos casos con diagnóstico ecográfico de quiste epidermoide, confirmado posteriormente tras cirugía. Realizamos una revisión de la bibliografía, enfatizando en la valoración de las imágenes ecográficas y su correlación con los hallazgos anatomopatológicos.

Activity of a hydroxybibenzyl bryophyte constituent against Leishmania spp. and Trypanosoma cruzi: in silico, in vitro and in vivo activity studies.

The synthesis and potent antiprotozoal activity of 14-hydroxylunularin, a natural hydroxybibenzyl bryophyte constituent is reported. 14-hydroxylunularin was highly active in vitro assays against culture and intracellular forms of Leishmania spp. and Trypanosoma. cruzi, in absence of cytotoxicity against mammalian cells. Preliminary structure-activity relationship studies showed that the reported bioactivity depends on hybridization at the carbon-carbon bridge, position and number of free hydroxy group on the aromatic rings. The reported results were also in agreement with the in silico prediction using Non-Stochastic Quadratic Fingerprints-based algorithms. The same compound also showed antiprotozoal activity in Leishmania spp. infected mice by oral and subcutaneous administration routes, with an optimal treatment of a daily subcutaneous administration of 10 mg/kg of body weight for 15 days. This study suggested that 14-hydroxylunularin may be chosen as a new candidate in the development of leishmanicidal therapy.

Structure of human Eg5 in complex with a new monastrol-based inhibitor bound in the R configuration.

Drugs that target mitotic spindle proteins have been proven useful for tackling tumor growth. Eg5, a kinesin-5 family member, represents a potential target, since its inhibition leads to prolonged mitotic arrest through the activation of the mitotic checkpoint and apoptotic cell death. Monastrol, a specific dihydropyrimidine inhibitor of Eg5, shows stereo-specificity, since predominantly the (S)-, but not the (R)-, enantiomer has been shown to be the biologically active compound in vitro and in cell-based assays. Here, we solved the crystal structure (2.7A) of the complex between human Eg5 and a new keto derivative of monastrol (named mon-97), a potent antimitotic inhibitor. Surprisingly, we identified the (R)-enantiomer bound in the active site, and not, as for monastrol, the (S)-enantiomer. The absolute configuration of this more active (R)-enantiomer has been unambiguously determined via chemical correlation and x-ray analysis. Unexpectedly, both the R- and the S-forms inhibit Eg5 ATPase activity with IC(50) values of 110 and 520 nM (basal assays) and 150 nm and 650 nm (microtubule-stimulated assays), respectively. However, the difference was large enough for the protein to select the (R)- over the (S)-enantiomer. Taken together, these results show that in this new monastrol family, both (R)- and (S)-enantiomers can be active as Eg5 inhibitors. This considerably broadens the alternatives for rational drug design.