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).

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.