Metabolic profiling and correlation analysis for the determination of killer compounds of proliferating and clonogenic HRT-18 colon cancer cells from Lafoensia pacari.

ETHNOPHARMACOLOGICAL RELEVANCE: Lafoensia pacari A. St.-Hil., belonging to the family Lythraceae and popularly known as 'dedaleira' and 'mangava-brava,' is a native tree of the Brazilian Cerrado, and its barks have been traditionally used as a tonic to treat inflammatory conditions, particularly related to gastric ulcers, wounds or fevers and various types of cancer. AIM OF THE STUDY: We have previously demonstrated the apoptogenic effects of the methanolic extract of L. pacari using various cancer cell lines. In the present study, this extract has been partitioned into fractions to identify the components that might be responsible for the apoptogenic effects using HRT-18 cells, which have been previously demonstrated to be sensitive to this extract. MATERIALS AND METHODS: A standard methanolic extract was prepared and fractionated by centrifugal partition chromatography. The fractions were submitted to cytotoxicity and clonogenic assays to monitor the effects in parallel with LC-DAD-MS and statistical analyses to suggest the potential bioactive compounds. RESULTS: Besides ellagic acid, the primary constituent of the plant and also the biomarker of the species, punicalin, pedunculagin and punicalagin isomers, catechin and ellagic acid derivatives were putatively identified. CONCLUSIONS: The barks of L. pacari are rich in ellagic acid and various hydrolysable tannins, some of which were reported for the first time in this species, such as punicalagin and ellagitannins. This mixture of substances had the ability to kill proliferating cells and abrogate the growth of clonogenic cells in a similar manner shown by the methanolic extract of our previous study. The collective data reported herein suggest that the biological activities of the L. pacari barks used by population to treat cancer conditions are due to the apoptogenic effects promoted by a mixed content of ellagitannins.

Cytotoxicity and apoptogenic effects of Lafoensia pacari.

ETHNOPHARMACOLOGICAL RELEVANCE: The stem barks of Lafoensia pacari have been traditionally used not only by South Amerindians but also by Brazilian and Paraguayan populations for treating a variety of unhealthy conditions to which their biological potential has been scientifically documented in several reports over the last decade. Although its anticancer usage is also popular, no scientific support for such activity has been found. AIM: To provide scientific evidence for the anticancer popularity of Lafoensia pacari. MATERIALS AND METHODS: Extracts prepared according to the popular use along with a methanol extract and its four fractions were produced from Lafoensia pacari stem barks. The chromatogram profile of each one was obtained by HPLC. Several tumor cell lines were exposed to these solutions in in vitro assays and the effects evaluated by morphological, growth, and cell cycle status changes. RESULTS: High toxicity determined by the lactate dehydrogenase levels with a significant drop in the cell proliferation index were found for all cell lines included in this study after exposition to Lafoensia pacari extract and fractions. The morphological features along with the expression of annexin V have strongly suggested apoptosis induction, which has been confirmed by G0/G1 cell cycle arrest. CONCLUSIONS: The data have clearly shown that exposition of human tumor cell lines to Lafoensia pacari stem barks extract leads to apoptosis induction due to cell cycle arrest in G0/G1 phases, supporting its anticancer use.

Lipid-lowering effects of standardized extracts of Ilex paraguariensis in high-fat-diet rats.

Mate (Ilex paraguariensis A. St.-Hil) is a native species of South America used to prepare traditional beverages. Recently a possible effect of its infusion on oxidative stress found in dyslipidemias has been reported. The main compounds related to these activities are phenolic compounds derived from chlorogenic acid. This study aimed to determine the anticholesteremic effect of the hydroethanolic extract (HEIP) and its n-butanolic fraction (n-BFIP), with standardized content of phenolic compounds derived from chlorogenic acid, in rats treated with high-fat diet (HFD). The contents of these compounds in the ethanol extract and n-butanol fraction were respectively two and three times higher than in traditional infusion with predominance of dicaffeoylquinic derivatives. The extracts were able to reduce serum triglycerides and cholesterol and decrease the atherogenic index in treated animals. These results support a potential effect of the mate extract in cardiovascular disease.