Uncommon Trimethoxylated Flavonol Obtained From Rubus Rosaefolius Leaves And Its Antiproliferative Activity

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)This study shows the evaluation the antiproliferative effect of the extract, fractions, and uncommon compounds isolated from R. rosaefolius leaves. The compounds were identified by conventional spectroscopic methods such as NMR-H-1 and C-13 and identified as 5,7-dihydroxy-6,8,4'-trimethoxyflavonol (1), 5-hydroxy-3,6,7,8,4'-pentamethoxyflavone (2), and tormentic acid (3). Both hexane and dichloromethane fractions showed selectivity formultidrug-resistant ovary cancer cell line (NCI-ADR/RES) with total growth inhibition values of 11.1 and 12.6 mu g/ml, respectively. Compound 1 also showed selective activity against the same cell line (18.8 mu g/ml); however, it was especially effective against glioma cells (2.8 mu g/ml), suggesting that this compound may be involved with the in vitro antiproliferative action.Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)ProPPEC/UNIVALICoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)CNPq [212RT0464

Is there still a place for involutional melancholia nowadays?

Ethnopharmacological relevance: Rubus niveus Thunb. plant belongs to Rosaceae family and have been used traditionally to treat wounds, burns, inflammation, dysentery, diarrhea and for curing excessive bleeding during menstrual cycle. The present study was undertaken to investigate the in vivo genotoxicity of Rubus niveus aerial parts extract and its possible chemoprotection on doxorubicin (DXR)-induced DNA damage. In parallel, the main phytochemicals constituents in the extract were determined.Materials and methods: The animals were exposed to the extract for 24 and 48 h, and the doses selected were 500, 1000 and 2000 mg/kg b.w. administered by gavage alone or prior to DXR (30 mg/kg b.w.) administered by intraperitoneal injection. The endpoints analyzed were DNA damage in bone marrow and peripheral blood cells assessed by the alkaline alkaline (pH > 13) comet assay and bone marrow micronucleus test.Results and conclusion: The results of chemical analysis of the extract showed the presence of tormentic acid, stigmasterol, quercitinglucoronide (miquelianin) and niga-ichigoside F1 as main compounds. Both cytogenetic endpoints analyzed showed that there were no statistically significant differences (p > 0.05) between the negative control and the treated groups with the two higher doses of Rubus niveus extract alone, demonstrating absence of genotoxic and mutagenic effects. Aneugenic/clastogenic effect was observed only at 2000 mg/kg dose. On the other hand, in the both assays and all tested doses were observed a significant reduction of DNA damage and chromosomal aberrations in all groups co-treated with DXR and extract compared to those which received only DXR. These results indicate that Rubus niveus aerial parts extract did not revealed any genotoxic effect, but presented some aneugenic/clastogenic effect at higher dose; and suggest that it could be a potential adjuvant against development of second malignant neoplasms caused by the cancer chemotherapic DXR. (C) 2015 Elsevier Ireland Ltd. All rights reserved.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP

GASTRO PROTECTIVE AND ANTI-HELICOBACTER PYLORI EFFECTS OF A FLAVONOID RICH FRACTION OBTAINED FROM ACHYROCLINE SATUREOIDES (LAM) D.C.

Objectives: The study aimed to investigate the gastroprotective effects of a flavonoid rich fraction (FRF) obtained from Achyrocline satureoides. Methods: The following protocols were employed: ethanol and NSAID-induced ulcer, ligature pylorus model, and free mucus quantification. Nitric oxide (NO) and sulfhydryl group participation were observed by pretreatment with L-NAME or NEM. Besides, it was assayed the acetic acid-induced chronic ulcer andthe anti-Helicobacter pyloriactivity in vitro. Results: The phytochemical profile of FRF showed three main flavonoids, luteolin, quercetin and 3-O-methyl-quercetin. The administration of FRF was able to prevent the damage evoked by ethanol and NSAID-induced ulcer models. The pH and concentration of H+ in the stomach were not modified by FRF treatment. However, the FRF treatment induces mucus secretion. The effect presented by FRF was mediated by nitric oxide (NO). In chronic ulcer model FRF reduced significantly the lesion area, promoting a cure ratio of 65.42±13.00, a similar data presented by cimetidine treated animals (61.35±11.88). Using an in vitro assay was observed that FRF at 500 µg/mL was able to inhibit bacterial growth. Conclusions: The results show that FRF provided a significant gastroprotective and ulcer healing activity, mainly due to their capacity to enhance mucus secretion

Uncommon Trimethoxylated Flavonol Obtained from Rubus rosaefolius

This study shows the evaluation the antiproliferative effect of the extract, fractions, and uncommon compounds isolated from R. rosaefolius leaves. The compounds were identified by conventional spectroscopic methods such as NMR-H1 and C13 and identified as 5,7-dihydroxy-6,8,4′-trimethoxyflavonol (1), 5-hydroxy-3,6,7,8,4′-pentamethoxyflavone (2), and tormentic acid (3). Both hexane and dichloromethane fractions showed selectivity for multidrug-resistant ovary cancer cell line (NCI-ADR/RES) with total growth inhibition values of 11.1 and 12.6 μg/ml, respectively. Compound 1 also showed selective activity against the same cell line (18.8 μg/ml); however, it was especially effective against glioma cells (2.8 μg/ml), suggesting that this compound may be involved with the in vitro antiproliferative action