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

Structural and physicochemical characterization and purity assessment of myrsinoic acids A and B, active compounds isolated from Rapanea ferruginea barks

The present study provided a chemical, physical and physicochemical characterization of myrsinoic acids A (MAA) and B (MAB) isolated from stem bark of Rapanea ferruginea Mez (Myrsinaceae). In previous pre-clinical studies these compounds have shown important anti-inflammatory, anticholinesterasic and antimicrobial activities. A gradient stability-indicating LC–UV method was developed, and a forced degradation study was carried out. Purity, logP, solubility, and pKa were determined. Thermal analysis (DSC/TG) was conducted for both compounds. MAB was characterized by X ray powder diffraction (XRPD) and scanning electron microscopy (SEM). When submitted to stress conditions, both markers showed degradation, with MAA presenting higher lability. The purity of MAA (oil) was 76.20%, while that of MAB (powder) was 98.90%. MAA and MAB exhibited logP values of 3.30 and 3.22, respectively. MAA was very slightly soluble in methanol and acetonitrile, while MAB was slightly soluble in both solvents. Both were practically insoluble in water. MAA and MAB showed pKa of 4.5 and 4.8, respectively. In the SEM analysis, MAB showed a semi-crystalline morphology and high purity when analyzed by XRPD and DSC. This data will contribute to the development, quality control and standardization of pharmaceuticals using MAA and MAB

Dragon's blood Croton palanostigma induces genotoxic effects in mice

Ethnopharmacological relevance: Dragon's blood is a dark-red sap produced by species from the genus Croton (Euphorbiaceae), which has been used as a famous traditional medicine since ancient times in many countries, with scarce data about its safe use in humans. in this research, we studied genotoxicity and clastogenicity of Croton palanostigma sap using the comet assay and micronucleus test in cells of mice submitted to acute treatment.Material and methods: HPLC analysis was performed to identify the main components of the sap. the sap was administered by oral gavage at doses of 300 mg/kg, 1000 mg/kg and 2000 mg/kg. for the analysis, the comet assay was performed on the leukocytes and liver cells collected 24 h after treatment, and the micronucleus test (MN) on bone marrow cells. Cytotoxicity was assessed by scoring 200 consecutive polychromatic (PCE) and normochromatic (NCE) erythrocytes (PCE/NCE ratio).Results and conclusion: the alkaloid taspine was the main compound indentified in the crude sap of Croton palanostigma. the results of the genotoxicity assessment show that all sap doses tested produced genotoxic effects in leukocytes and liver cells and also produced clastogenic/aneugenic effects in bone marrow cells of mice at the two higher doses tested. the PCE/NCE ratio indicated no cytotoxicity. the data obtained suggest caution in the use of Croton palanostigma sap by humans considering its risk of carcinogenesis. (C) 2013 Elsevier Ireland Ltd. All rights reserved.Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Univ Estadual Paulista UNESP, Dept Fonoaudiol, Fac Filosofia & Ciencias, BR-17525900 Marilia, SP, BrazilUniv Vale Itajai UNIVALI, Nucleo Invest Quim Farmaceut NIQFAR, Itajai, SC, BrazilUniversidade Federal de São Paulo UNIFESP, Dept Ciencias Exatas & Terra, Diadema, SP, BrazilUniversidade Federal de São Paulo UNIFESP, Dept Ciencias Exatas & Terra, Diadema, SP, BrazilWeb of Scienc

Antiproliferative effect of Synadenium grantii Hook f. stems (Euphorbiaceae) and a rare phorbol diterpene ester

Synadenium grantii is frequently used for the treatment of various diseases such as allergies, gastric disorders, and especially cancer. The aim of this study was to evaluate the possible antiproliferative potential of the methanol extract, fractions, and pure compounds from the stems of S grantii. Phytochemical analysis was carried out by conventional chromatographic techniques, and the antiproliferative activity was analyzed using the sulforhodamine B assay and an MTT-based assay. Nonpolar fraction and its subfractions from the stems of S grantii exhibited promising cytostatic effect against several human tumor cell lines (glioma, breast, kidney, and lung), with total grown inhibition values ranging from 0.37 to 2.9 μg/mL. One of the active principles of this plant was identified as a rare phorbol diterpene ester, denoted as 3,4,12,13-tetraacetylphorbol-20-phenylacetate. This compound demonstrated antiproliferative activity against glioma, kidney, lung, and triple-negative breast cancer cell lines. These results demonstrate that S grantii stems produce active principles with relevant antiproliferative potential.Peer Reviewe

Reproductive toxicology and clastogenic evaluation in mice of a phytotherapeutic formulation obtained from Cinchona calisaya Weddel (Rubiaceae) used in Brazilian folk medicine as female fertility stimulant

Ethnopharmacological relevance: In Brazil, a phytotherapeutic preparation produced from a standardized tincture of Cinchona calisaya Weddel such that each mL of product contains 400 mu g of quinine, known in Portuguese as Agua Inglesa (R) (English water), is indicated by the manufacturer as a tonic, appetite stimulant, and digestive. However, this preparation has long been used in folk medicine as a female fertility stimulant. Despite its widespread use in folk medicine to stimulate female fertility, no study has been undertaken to assess the potential teratogenic and genotoxic effects of this phytotherapeutic preparation. The aim of the present study was to investigate possible toxic reproductive effects in mice caused by exposure to Agua Inglesa (R), either before mating or during the pre- and post-embryo implantation periods. The genotoxic potential was evaluated using the micronucleus assay.Material, Methods, and Results: Virgin female mice, with at least one estrous cycle evidenced by vaginal cytology, were divided into five groups of 15 individuals each (Group I - control, Group II - treated with ethanol solution at 16%, Groups III, IV and V treated with phytotherapeutic preparation at 1.5 mL/kg/day, 3.0 mL/kg/day and 4.5 mL/kg/day, respectively). After the first 28 days of treatment, females were caged individually with adult fertile males. Pregnant females continued to receive treatment for seven days (preimplantation period). Body weight was recorded weekly during treatment. Signs of toxicity (weight loss, food intake, piloerection, apathy, prostration, diarrhea, seizures, behavioral changes, and locomotion) were also observed. The females were sacrificed on the 15th day of pregnancy, uterine horns were evaluated for implantation, and the placental index was recorded. In the micronucleus test, 2000 polychromatic erythrocytes (PCE) per animal, obtained from bone marrow, were scored. Results The results showed that exposure of the females during the pre- and post-implantation periods did not significantly alter the reproductive capacity (p 0.05) in terms of the average number of micronucleated polychromatic erythrocytes.Conclusions: Although folk medicine suggests that the Agua Inglesa (R) preparation is useful as a female fertility stimulant, no such effect was confirmed in mice. (C) 2014 Elsevier Ireland Ltd. All rights reserved