A methanolic extract and two fractions (n-hexane and ethyl acetate) from Virola oleifera leaves and some compounds (one lignan and two flavonoids) were investigated to verify the analgesic activity by using the writhing test in mice. The crude methanolic extract showed a moderate analgesic effect (about 40% of inhibition in this test at 10 mg/kg), whereas n-hexane and ethyl acetate fractions caused inhibition of 51.3 ± 5.9% and 50.5 ± 6.3% , respectively. Oleiferin-C (1), a lignan isolated from the n-hexane fraction, showed an interesting analgesic potential in this model when compared to two standard drugs, paracetamol (4-acetamidophenol) and aspirin (acetylsalicylic acid). The ID50 calculated for this compound was 17.25 μmol/kg, with confidence interval between 13.7 and 21.3 μmol/kg, being about 8 times more potent than the standard drugs. The mixture of two glycoside-flavonoids, identified as astilbin (2) and quercitrin (3), also exhibited good analgesic activity, causing 63% of reduction of abdominal constriction in mice. These results suggest beneficial effect of this plant to treat dolorous processes.
From the stems of Croton micans Sw., five new 3,4-seco-ent-kaurene dimers: micansinoic acid (1), isomicansinoic acid (2), and the dimethyl (3), monomethyl (4) and monoethyl ester (5) of micansinoic acid were isolated. The structures of the new compounds were elucidated by spectroscopic data interpretation, mainly 1D and 2D NMR experiments and MS. These compounds are the first 3,4-seco-ent-kaurene dimers from a Croton species.
As part of the program of our research group to search for new and effective substances from the Brazilian biodiversity, the present work evaluates the antibacterial activity of four species from the Brazilian flora (Garcinia achachairu, Macrosiphonia velame, Rubus niveus and Pilea microphylla) against Bacillus subtilis, Staphylococcus aureus and S. saprophyticus (Gram-positive bacteria), Escherichia coli (Gram-negative bacterium) and Candida albicans (yeast). The extracts of R. niveus and M. velame showed promising antibacterial activity with MICs, ranging from 1000 to 125 µg/mL. Bio-guided fractionation of M. velame yielded four compounds, with the highest inhibition being observed for compound 3, with a MIC of 125 µg/mL against S. aureus. The combinations of fractions 2 and 4 showed beneficial effect against Gram-positive bacteria (additive effect), suggesting a possible synergistic effect.
Floating-Harbor syndrome (FHS) is a rare inherited developmental disorder characterized by bone mineralization delay and growth deficits frequently associated with skeletal and craniofacial defects and mental retardation. The major cause of FHS is heterozygous truncating mutations in Srcap, which encodes the ATPase SRCAP, the core catalytic subunit of the homonymous multiprotein chromatin-remodeling complex in humans. This complex promotes the exchange of canonical histone H2A with the H2A.Z variant. SRCAP is also implicated in several cellular processes, but the molecular basis of FHS still needs to be elucidated. Using a combined approach, we studied the involvement of SRCAP in cell cycle progression in HeLa cells. In addition to the canonical localization in interphase nuclei, both SRCAP and its Drosophila orthologue localized to the mitotic apparatus after nuclear envelope breakdown, and their depletion impaired mitosis progression and cytokinesis in human and Drosophila cells, respectively. Importantly, SRCAP interacted with cytokinesis regulators and α-Tubulin during telophase, strongly supporting a direct role in cytokinesis, independent of its chromatin remodeling functions. Our results provide clues about previously undetected, evolutionarily conserved roles of SRCAP in ensuring proper mitosis and cytokinesis. We propose that perturbations in cell division contribute to the onset of developmental defects characteristic of FHS.
Dihydroxy‐acetophenon (I) reagiert mit (II) in Gegenwart von Kaliumcarbonat zum Monoäther (III), der mit Benzaldehyd bzw. p‐Hydroxy‐benzaldehyd zu den Chalkonen (IV) reagiert.
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