Evaluation of the Acute Toxicity, Cytotoxicity, and Genotoxicity of Chresta martii (Asteraceae).

Chresta martii (Asteraceae), found in the Xingó region, northeastern Brazil, is used in the treatment of gastrointestinal (GIT) and liver disorders and malaria. However, there are few studies regarding efficacy and safety of use for this species. Thus, the objective of this study was to determine in vivo acute toxicity and in vitro cytotoxicity of organic extracts of C. martii as well as in vivo genotoxicity of its semipurified fraction. Dried aerial parts of C. martii were extracted using three organic solvents (cyclohexane [ECCm], ethyl acetate [EACm], and ethanol [EECm]), and these extracts were examined for acute toxicity (50-2000 mg/kg ip or po) and cytotoxicity (50 µg/ml) in carcinogenic human cell lines (HL-60, NCIH-292, and MCF-7). The EACm, which showed evidence of toxicity (in vivo and in vitro), was fractionated on a silica column, yielding four fractions (F1-F4). The F1 was utilized for genotoxicity (50 mg/kg ip), by in vivo micronucleus (MN) assay. ECCm showed no indication of acute toxicity or occurrence of death, while the LD50 estimated for the extracts (EACm and EECm) was 500 mg/kg po and 200 mg/kg ip. The EACm (50 µg/ml) inhibited growth of tumor cells HL-60 (96.54%), NCIH-292 (73.43%), and MCF-7 (15%). The F1 fraction induced MN formation in polychromatic erythrocytes of Swiss Webster mice. Organic extracts from C. martii exhibited acute toxicity classified as mild to moderate, in addition to cytotoxicity (in vitro), while the F1 semipurified fraction induced genotoxicity (in vivo).

Parkinsonia aculeata aqueous extract fraction: biochemical studies in alloxan-induced diabetic rats.

The antidiabetic effect of Parkinsonia aculeata water soluble fraction (WSF) made of aerial parts of the plant (leaves and flowers) was investigated in alloxan diabetic rats. Its effect was compared with that of insulin (positive control). The physico-metabolic parameters measured were: body weight, food and liquid intake, urinary volume, hepatic glycogen, serum glucose, total cholesterol, HDL-cholesterol, triglycerides, urinary glucose and urea, and the weight of epididymal adipose tissue, liver, kidneys and the skeletal muscles (soleus and extensor digitorum longus). Oral administration of WSF (125 or 250 mg/kg) for 16 days exhibited a significant reduction in serum and urinary glucose, urinary urea, total cholesterol, HDL-cholesterol and triglycerides in alloxan diabetic rats. An improvement of hepatic glycogen, a decrease of liquid and food intake, and a significantly positive actions in the weight of skeletal muscles (soleus and extensor digitorum longus) and kidneys were also observed, but just diabetic group treated with WSF at a dose of 125 mg/kg showed significant reduction in urinary volume, body weight, an improvement of epididymal adipose tissue and a positive action in liver weight. The effects of WSF on the physico-metabolic parameters was comparable to those observed in diabetic insulin treated group. The results of this work suggest that P. aculeate may have new clinical significant choice in diabetes mellitus illness, and could explain the basis for its traditional use to manage diabetes-related complications by rural community of northeast of Brazil.

Study of the Gastroprotective Effect of Extracts and Semipurified Fractions of Chresta martii DC. and Identification of Its Principal Compounds.

Chresta martii (Asteraceae) is a species widely used by the population of the Xingu region of Sergipe, Brazil, in the form of a decoction (aerial parts) for the treatment of gastrointestinal diseases. The study aims to assess the gastroprotective activity of organic extracts and semipurified fractions and identify the principal compounds present in C. martii responsible for such activity. The organic extracts (cyclohexane: ECCm, ethyl acetate: EACm, and ethanol: EECm) were obtained from the dried aerial parts (500 g) of C. martii. For evaluation of the gastroprotective activity of extracts (50, 100, or 200 mg/kg; p.o.), male Swiss Webster mice (25-30 g) were used which had gastric ulcers induced by indomethacin (40 mg/kg, s.c.) or ethanol (0.2 mL/animal; p.o.). Among the extracts evaluated, EACm exhibited significant (P < 0.05) gastroprotective activity in the models used. The fractionation of EACm was performed in a silica gel column 60 eluted with the following compounds: [chloroform-F1 yield (10%)], [chloroform/ethyl acetate (1/1)-F2 yield (6%)], [ethyl acetate-F3 yield (8%)], and [ethyl/methanol acetate (1/1)-F4 yield (5%)]. Of the fractions described above, the F1 (25 mg/kg; p.o.) had greater gastroprotective activity (P < 0.05) than that displayed by ranitidine (80 mg/kg; p.o.) in the ethanol-induced ulcer model. The refractionation of F1 produced 23 subfractions and from these two yellow amorphous compounds were obtained by recrystallization, Rf: 0.46 and 0.31 (ethyl acetate : chloroform 5 : 5). The compounds isolated were characterized by nuclear magnetic resonance spectroscopy ((1)H-NMR and (13)C-NMR) and identified as flavones: chrysoeriol (yield: 0.43%) and 3',4'-dimethoxyluteolin (yield: 0.58%). Conclusion. Flavone 3',4'-dimethoxyluteolin is the principal compound present in the species C. martii and is probably responsible for gastroprotective activity observed in this species.

Protective effect of Chresta martii extract against indomethacin-induced gastric lesions in mice.

Chresta martii (Asteraceae) is a plant found in the Xingó region (semi-arid area) in Northeastearn Brazil, and is recognized by the local population as a traditional herb used to treat gastric diseases. This is the first report of the chemical composition, acute toxicity, and gastroprotective effect in mice of the hydroalcoholic extract (HAE) from the aerial parts (leaves and flowers) of Chresta martii. Animals received HAE doses from 10 to 2000 mg/kg, i.p. or 50 to 3000 mg/kg, p.o.) and were observed over 48 h for toxicity signs and mortality; sub-chronic toxicity was evaluated through 14 days treatment with once-daily HAE doses (400 mg/kg, p.o.). The gastroprotective effect of HAE was demonstrated on the indomethacin-induced gastric ulcer model after the administration of extracts. Data comparison of ulcer index averages between saline and HAE (100 or 400 mg/kg, p.o.) groups showed significant (P < 0.01) inhibition (71.73 and 76.72 %, respectively) of indomethacin-induced gastric lesions. Histological analyses showed significant (P < 0.05) inhibition of leukocyte migration in HAE-treated groups. A fingerprint of the HAE obtained by HPLC/UV/MS analysis showed major peaks characteristic of sesquiterpene lactones. Compound 1 was isolated and elucidated as a new natural product. Its capacity to prevent leukocyte chemotaxis was demonstrated in vitro, corroborating the pharmacological effects observed for C. martii HAE.

Atividade in vitro do extrato hidroalcoólico de Lippia sidoides Cham sobre larvas de terceiro estádio de nematódeos gastrintestinais (família Trichostrongylidae) de caprinos / In vitro activity of the hydroalcoholic extract of Lippia sidoides Cham on buoyant larvae of third-stage gastrointestinal nematodes (family Trichostrongylidae) of goats

Avaliou-se in vitro a atividade larvicida do extrato hidroalcóolico de alecrim pimenta (Lippia sidoides Cham) sobre larvas de terceiro estádio de nematoides gastrintestinais de caprinos. Os resultados encontrados demonstraram que a concentração de 500 mg mL-1 apresentou atividade efetiva e com capacidade de ação de 95,89%, demonstrando desta forma a possibilidade do uso terapêutico anti-helmíntico para esse extrato.

The in vitro larvicidal activity of the hydroalcoholic extract of rosemary pepper (Lippia sidoides Cham) was evaluated on buoyant larvae of third-stage gastrointestinal gastrointestinal nematodes of goats. The results demonstrated that the concentration of 500 mg mL-1 presented effective activity, with a capacity of action of 95.89%, thus demonstrating the possibility of anthelmintic therapeutic use for this extract.

Antiinflammatory and chronic toxicity study of the leaves of Ageratum conyzoides L. in rats.

The hydroalcoholic extract (HAE) of Ageratum conyzoides leaves was studied for its antiinflammatory effect on subacute (cotton pellet-induced granuloma) and chronic (formaldehyde-induced arthritis) models of inflammation in rats. The absence or presence of toxicity by prolonged use of HAE was also evaluated through biochemical and hematological analysis of rats blood samples using daily oral doses of 250 or 500 mg/kg body wt., during 90 days. The results showed that the group of rats treated with HAE (250 mg/kg body wt.; p.o.) had a 38.7% (p < 0.05) reduction in cotton-pellet granuloma. The development of chronically induced paw edema was also reduced significantly (p < 0.05) by the plant extract. The toxicity study did not show any treatment-related abnormalities in biochemical and hematological parameters. The biochemical analysis from blood samples drawn from group of rats treated orally with 500 mg/kg body wt. did, however, present 30.2% (p < 0.05) reduction of SGPT activity as compared to the corresponding control group. These results confirm the antiinflammatory properties of A. conyzoides, with no apparent hepatotoxicity.

Avaliação in vitro do extrato hidroalcoólico (EHA) de alecrim pimenta (Lippia sidoides Cham. ) sobre o desenvolvimento de ovos de nematódeos gastrointestinais (Trichostrongylidae) / In vitro evaluation of alecrim pimenta (Lippia sidoides Cham. ) hydroalcoholic extract (HAE) on the development of gastrointestinal nematode (Trichostrongylidae) eggs

Atualmente a fito medicina vem sendo usada no controle de diversas doenças parasitárias particularmente as parasitoses gastrointestinais. Objetivou-se com este estudo avaliar a eficácia do extrato hidroalcoólico (EHA) de Lippia sidoides Cham sobre o desenvolvimento de ovos de nematódeos gastrointestinais. O efeito ovicida foi determinado através de análise probabilística, modelo logístico, utilizados os softwares R versão 2.2.1 e EPI6. Foram obtidos ovos embrionados em fezes de cabras naturalmente infectadas com nematóides Trichostrongylidae e o número de ovos fecais foi determinado usando-se a técnica modificada de McMaster. Cinquenta μL da suspensão contendo 40 ovos foram transferidas a placas de poliestireno e incubadas com 12 concentrações diferentes do EHA sendo avaliada durante 72 horas a temperatura ambiente. Os resultados demonstraram diferentes eficácias para o fito medicamento com menor taxa de desenvolvimento de ovos na concentração de 500 mg mL-1 . Conclui-se que o EHA pode ter papel importante sobre o desenvolvimento in vitro de ovos de nematóides gastrintestinais, revelando atividade ovicida.

Phytomedicine has been currently used in the control of several parasitic diseases, particularly gastrointestinal ones. The aim of this study was to evaluate the efficacy of the hydroalcoholic extract (HAE) from Lippia sidoides Cham. on the development of gastrointestinal nematode eggs. The ovicidal effect was determined through probabilistic analysis, logistic model, by using the programs R version 2.2.1 and Epi InfoTM 6. Embryonated eggs were obtained from feces of goats naturally infected with Trichostrongylidae nematodes and the fecal egg count was determined by using the modified McMaster technique. Fifty microliters of the suspension containing 40 eggs were transferred to polystyrene plates and incubated with 12 different HAE concentrations, and evaluations were performed during 72h at room temperature. The results demonstrated different efficacy of extracts, with lower egg development rate at 500 mg mL-1. In conclusion, HAE may play an important role on the in vitro development of gastrointestinal nematode eggs, indicating ovicidal activity.

Determinação de atividade antimicrobiana de extratos de plantas de uso popular como antiflamatório

Antimicrobial activities of “babaçu” (Orbignya martiana), “cardo santo” (Argemone mexicana), “mentrasto” (Ageratum conyzoides), “cavalinha” (Equisetum yeamalis) and “terramicina” (Alternanthera brasiliana), used by Brazilian population as antiinflamatory medicine, were studied on Staphylococcus aureus. The freezer dried hydroalcoholic extracts solutions were tested for 7 strains of Staphylococcus aureus, which two of those are methicillin resistant (MRSA). The diffusion method on agar-agar, using holes technique, with tetracycline chlorydrate as standard. “Babaçu”, “cardo santo” and “terramicina” showed antimicrobial activity, within of those “terramicina” inhibited 6 strains, presenting zone inhibition of 22 mm compared to standard antibiotic (34 mm), except the seventh strain which was also tetracycline resistant.