Bioguided isolation of a selective compound from Calea phyllolepis leaves against breast cancer cells.

Plants of the Calea genus have been reported to contain lipophilic compounds, such as sesquiterpene lactones, with cytotoxic effect against different cancer cell lines. The aim of this manuscript was to investigate the chemical profile and cytotoxic activity of different fractions from Calea phylolepis leaves on different human cancer cell lines. The fractions were prepared using solvent extraction of increasing polarity, yielding hexane, ethyl acetate and methanolic fractions. All fractions were chemically analysed by thin layer chromatography (TLC), and their cytotoxic activity against HT-29 (colon adenocarcinoma), MCF-7 (breast cancer), U-251MG (malignant glioblastoma) and L929 (mouse fibroblast) cell lines was investigated. Among these, the hexane and ethyl acetate fractions showed higher cytotoxic effects, while the methanolic fraction did not show any cytotoxic effects. The major bioactive compound from the hexane fraction (12.15%) was isolated using chromatographic methods and was identified by nuclear magnetic resonance spectroscopy (NMR) and gas chromatography-mass spectrometry (GC-MS) analysis as 6-epi-ß-verbesinol coumarate. This compound showed activity against breast cancer cells (IC50 = 5.8 ± 1.0 µg/ml), similar to etoposide. Furthermore, 6-epi-ß-verbesinol coumarate showed low cytotoxicity to normal fibroblast cells, suggesting a high selectivity index (SI = 7.39) against breast cancer cells.

Evaluation of the cytotoxic and genotoxic effects of Sida planicaulis Cav extract using human neuroblastoma cell line SH-SY5Y.

Sida planicaulis is a weed thought to have originated in Brazil, where it is present in abundant quantities, but also this plant is also found in south-central Florida, Indian Ocean Islands, and the Pacific Islands. Sida planicaulis produces neurotoxicity that adversely affects livestock breeding with heavy animal losses and consequent negative impact on Brazil's economy. The aim of this study was to determine the chemical profile, cytotoxic and genotoxic effects of ethanolic extracts of S. planicaulis collected in winter (leaf extract) and summer (leaf extract and leaf + flower extract) using an in vitro model of human neuroblastoma cell line SH-SY5Y. Phytochemical screening demonstrated the presence of alkaloids, flavonoids, and apolar compounds. Rutin, quercetin, and swainsonine were detected by HPLC and GC/MS, respectively. Phosphorus, potassium, iron, and zinc were the inorganic elements found. Extracts produced cytotoxicity at all concentrations tested (7-4,000 µg/ml) as evidenced by the colorimetric assay [3-(4,5-dimethyl-thiazol-2-yl) -2,5-diphenyl-tetrazolium bromide (MTT)]. Based upon the alkaline comet assay extracts were found to induce genotoxicity at concentrations ranging from 0.437 to 7 µg/ml. DNA damage produced by extracts was affirmed using a modified comet assay with the enzymes Endo III and FPG in a concentration dependent manner. Further, enzyme-modified comet assay showed both oxidized purines and pyrimidines, and consequently oxidative stress was related to genomic instability and cell death. Data suggest that low concentrations of ethanolic extracts of S. planicaulis (different seasons) induced increased DNA damage related to oxidative stress and chemical composition.

Biotoxicological Analyses of Trimeroside from Baccharis trimera Using a Battery of In Vitro Test Systems.

The use in folk medicine of Baccharis trimera and recent studies on DNA damage by oxidative stress mechanisms have motivated this study. We investigated the biotoxicological effects of trimeroside from this plant. Aqueous extract from aerial parts of B. trimera was fractioned by flash chromatography for further isolation by thin-layer chromatography. The novel nor-monoterpene glycoside, trimeroside, and three flavonoids, cirsimaritin, luteolin and quercetin, were isolated. The genotoxic and mutagenic potential of trimeroside was determined by Salmonella/microsome (TA98 and TA100), comet assay, and cytokinesis-block micronucleus cytome assay (CBMN-cyt) in HepG2 cells. We also screened trimeroside into different human tumoral cell lines by sulforhodamine B (SRB) assay. Mutagenicity was detected in TA100 strain with metabolic activation. Genotoxic effects were not observed in HepG2 by comet assay. However, a decrease in the nuclear index division in the 2.0 mg·mL-1 concentration and an increase of nucleoplasmic bridges in the 1.5 mg·mL-1 concentration were detected by CBMN-cyt assay indicating cytotoxic and mutagenic effects. In SRB assay, trimeroside showed weak antiproliferative activity against the cell lines.