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61.
Valerio Tazzari Graziella Cappelletti Manolo Casagrande Elena Perrino Luigi Renzi Piero Del Soldato Anna Sparatore 《Bioorganic & medicinal chemistry》2010,18(12):4187-4194
A series of dithiolethione derivatives was synthesized and the in vitro HDAC inhibitory activity was tested. The most active compounds, 1 and 2, exhibited an IC50 in nM range with a strong hyperacetylation of histone H4 in A549 cells. The HDAC inhibitory activity comparable to that of SAHA and the inhibition of A549 cell proliferation suggest that these compounds are worthy of further studies as potential anticancer agents. 相似文献
62.
Ovulation generally takes two forms: spontaneous and induced. These two ovulatory modes are predicted to cause different levels of male–male competition due to differences in males’ ability to predict the timing of ovulation of females that use each mode. Ovulation mode has been shown to be correlated with differences in testis size, but it is not known whether ovulation type influences ejaculate traits, specifically sperm quantity (sperm concentration, ejaculate volume, total motile sperm per ejaculate) and/or sperm quality (% sperm motility, % normal sperm). Using a cross-species comparative analysis of 130 mammals, we found that sperm concentration and total motile sperm per ejaculate were significantly greater in spontaneous ovulators. In contrast, ejaculate volume, % sperm motility and % normal sperm were unrelated to ovulation type. These data show that ovulation alters sperm quantity by increasing sperm concentration but not ejaculate volume, and that sperm quality does not vary with ovulation mode. 相似文献
63.
Graziella Hanna Pereira Aline Queiroz Santos Miriam Park Patricia Rady Muller Soraia Padua Raquel Ferrari Marchesi Vera Lucia Aldred 《Mycopathologia》2010,170(4):259-261
Paracoccidioides brasiliensis rarely shows bone marrow involvement and its response to treatment with itraconazole in children needs further assessment. We describe here a child with a juvenile disseminated form of paracoccidioidomycosis, which showed reticuloendothelial system involvement and the presence of Paracoccidioides brasiliensis in the bone marrow. The patient showed an effective and rapid response to itraconazole therapy. 相似文献
64.
Michelle S. Libério Graziella A. Joanitti Ricardo B. Azevedo Eduardo M. Cilli Lanuse C. Zanotta Anna C. Nascimento Marcelo V. Sousa Osmindo R. Pires Júnior Wagner Fontes Mariana S. Castro 《Amino acids》2011,40(1):51-59
Nowadays, the emergence of resistance to the current available chemotherapeutic drugs by cancer cells makes the development
of new agents imperative. The skin secretion of amphibians is a natural rich source of antimicrobial peptides (AMP), and researchers
have shown that some of these wide spectrum molecules are also toxic to cancer cells. The aim of this study was to verify
a putative anticancer activity of the AMP pentadactylin isolated for the first time from the skin secretion of the frog Leptodactylus labyrinthicus and also to study its cytotoxic mechanism to the murine melanoma cell line B16F10. The results have shown that pentadactylin
reduces the cell viability of B16F10 cells in a dose-dependent manner. It was also cytotoxic to normal human fibroblast cells;
nevertheless, pentadactylin was more potent in the first case. The studies of action mechanism revealed that pentadactylin
causes cell morphology alterations (e.g., round shape and shrinkage morphology), membrane disruption, DNA fragmentation, cell
cycle arrest at the S phase, and alteration of mitochondrial membrane potential, suggesting that B16F10 cells die by apoptosis.
The exact mechanism that causes reduction of cell viability and cytotoxicity after treatment with pentadactylin is still unknown.
In conclusion, as cancer cells become resilient to death, it is worthwhile the discovery of new drugs such as pentadactylin
that induces apoptosis. 相似文献
65.
66.
This article reviews the current knowledge on time-dependent variations in the physiology of blood coagulation and in the anticoagulant effect of heparin and warfarin. Animal data indicated that the shortest blood clotting time and the highest levels of coagulation factors II, VII, and IX were recorded during the resting period of the animal. These circadian rhythms were not altered by modifications of the lighting regimens. In healthy volunteers, the prothrombin time was longer at the end of the afternoon than early in the morning; the acro-phases of activated partial thromboplastin time and thrombin time occurred in the evening or during the night. The acrophases of fibrinogen, factors II, VII, VIII, and a-1-antitrypsin were obtained in the morning. There is no agreement on the chronobiology of platelet aggregation, and differences can be found in the time of maximal aggregability. The chronopharmacological studies of heparin infused at a constant rate to patients with thromboembolic diseases suggested that maximal effectiveness occurred at 04:00, while it was minimal at 08:00. Animal data indicated that oral administration of warfarin at the end of the activity period of rats produced maximal inhibition of vitamin K-dependent factors. This was the time of day when warfarin interference with the vitamin K cycle of the liver was highest. Further studies are needed to determine the clinical significance of biological rhythms in the physiology and pharmacology of blood coagulation. 相似文献
67.
68.
Abstract New species of Stigmatomyces (Ascomycetes, Laboulbeniales) parasitic on Italian Diptera. – Three new Laboulbeniales parasitic on Italian Diptera are described: Stigmatomyces asteiae, parasitic on Asteia amoena Meig. (Asteiidae), Stigmatomyces athyroglossae, parasitic on Athyroglossa glabra (Meig.) (Ephydridae), and Stigmatomyces geomyzae, parasitic on Geomyza tripunctata Fall. (Opomyzidae). 相似文献
69.
Graziella Tocco Antonella Fais Gabriele Meli Michela Begala Gianni Podda M.Benedetta Fadda Marcella Corda Orazio A. Attanasi Paolino Filippone Stefano Berretta 《Bioorganic & medicinal chemistry letters》2009,19(1):36-39
In this work, the PEG-immobilization and the liquid phase synthesis of some coumarins derived from cardol are presented. Some preliminary results on their tyrosinase inhibitory activity are also included. 相似文献
70.