Biological activity of the aqueous extract of Lychnophora pinaster Mart

Lyophilized aqueous extract (LAE) from Lychnophora pinaster Mart (Asteraceae) aerial parts was evaluated in the search of possible biological activities. LAE exhibited trypanocidal activity (113.62 μg/mL), but could not inhibit 5-lipoxygenase in vitro (17% of inhibition). LAE chemical characterization by HPLC with UV-Diode Array Detector showed the presence of caffeic acid, isochlorogenic acid, vitexin, isovitexin and quercetin, in comparison with authentic samples

Genotoxicity of lapachol evaluated by wing spot test of Drosophila melanogaster

Abstract This study investigated the genotoxicity of Lapachol (LAP) evaluated by wing spot test of Drosophila melanogaster in the descendants from standard (ST) and high bioactivation (HB) crosses. This assay detects the loss of heterozygosity of marker genes expressed phenotypically on the fly's wings. Drosophila has extensive genetic homology to mammals, which makes it a suitable model organism for genotoxic investigations. Three-day-old larvae from ST crosses (females flr 3 /TM3, Bd s x males mwh/mwh), with basal levels of the cytochrome P450 and larvae of high metabolic bioactivity capacity (HB cross) (females ORR; flr 3 /TM3, Bd s x males mwh/mwh), were used. The results showed that LAP is a promutagen, exhibiting genotoxic activity in larvae from the HB cross. In other words, an increase in the frequency of spots is exclusive of individuals with a high level of the cytochrome P450. The results also indicate that recombinogenicity is the main genotoxic event induced by LAP

Genotoxicity of lapachol evaluated by wing spot test of Drosophila melanogaster

This study investigated the genotoxicity of Lapachol (LAP) evaluated by wing spot test of Drosophila melanogaster in the descendants from standard (ST) and high bioactivation (HB) crosses. This assay detects the loss of heterozygosity of marker genes expressed phenotypically on the fly's wings. Drosophila has extensive genetic homology to mammals, which makes it a suitable model organism for genotoxic investigations. Three-day-old larvae from ST crosses (females flr³/TM3, Bd s x males mwh/mwh), with basal levels of the cytochrome P450 and larvae of high metabolic bioactivity capacity (HB cross) (females ORR; flr³/TM3, Bd s x males mwh/mwh), were used. The results showed that LAP is a promutagen, exhibiting genotoxic activity in larvae from the HB cross. In other words, an increase in the frequency of spots is exclusive of individuals with a high level of the cytochrome P450. The results also indicate that recombinogenicity is the main genotoxic event induced by LAP

Atribuição completa e inequívoca dos sinais de deslocamento químico dos átomos de carbono e hidrogênio do ácido licnofórico extraído de Lychnophora pinaster

ABSTRACTThe investigation of the hexane extract from aerial parts of Lychnophora pinaster provided, besides others substances, the E-isomer of lychnophoric acid, a sesquiterpene derivative previously isolated from L. affinis. ________________________________________________________________________________ RESUMOO estudo químico das partes aéreas do extrato hexânico de Lychnophora pinaster forneceu, além de outras substâncias, o isômero E do ácido licnofórico, um sesquiterpeno anteriormente isolado de L. affinis

Antiplasmodial activity and cytotoxicity, isolation of active alkaloids, and dereplication of Xylopia sericea leaves ethanol extract by UPLC-DAD-ESI-MS/MS.

Objectives: To assess the antiplasmodial activity of the ethanol extract of Xylopia sericea leaves, Annonaceae, often associated with antimalarial use and to perform a bioguided isolation of active compounds. Methods: Dereplication of ethanol extract by the UPLC-DAD-ESI-MS/MS technique allowed the identification of the major constituents, isolation and identification of alkaloids. The antiplasmodial and cytotoxic activity of the extract, fractions and isolated compounds was evaluated against the chloroquine-resistant W2 strain Plasmodium falciparum and HepG2 cells, respectively. Key findings: Ethanol extract showed high reduction of parasitemia as well as moderate cytotoxicity (86.5 3.0% growth inhibition at 50 lg/ml and CC50 72.1 5.1 lg/ml, respectively). A total of eight flavonoids were identified, and two aporphine alkaloids, anonaine and O-methylmoschatoline, were isolated. Anonaine disclosed significant antiplasmodial effect and moderate cytotoxicity (IC50 23.2 2.7 lg/ml, CC50 38.3 2.3 lg/ml, SI 1.6) while O-methylmoschatoline was not active against P. falciparum and showed a low cytotoxicity (33.5 1.9% growth inhibition at 50 lg/ml, CC50 274.4 0.5 lg/ml). Conclusions: Characterization of Xylopia sericea leaves ethanol extract by UPLCDAD-ESI-MS/MS as well as its antiplasmodial activity and the occurrence of anonaine and O-methylmoschatoline in this Xylopia species are reported by the first time

Phytochemistry and antiplasmodial activity of Xylopia sericea leaves.

Aiming to investigate the antiplasmodial activity and the phytochemical composition of Xylopia sericea leaves, the essential oil and dichloromethane extract were analyzed by gas and liquid chromatography, respectively, both of them coupled to mass spectrometry, and were evaluated against the chloroquine-resistant Plasmodium falciparum strain (W2) and for cytotoxicity to HepG2 cells. Low growth inhibition of P. falciparum as well as low cytotoxicity to HepG2 cells were observed for the essential oil. The leaves dichloromethane extract showed moderate growth inhibition of P. falciparum and low cytotoxicity to HepG2 cells. Bioguided chromatographic fractionation of this extract led to fractions with increased antiplasmodial activity from which liriodenine (IC50 6.1???0.1??g/mL, CC50 > 1000.0??g/mL, SI > 164), an aporphine alkaloid, and an acetogenin-rich fraction containing mainly isomers of annomontacin and 4-deoxy-annomontacin (IC50 22.7???1.9??g/mL, CC50 336.1?? 15.5??g/mL, SI = 15) might be highlighted for their antiplasmodial activity

Phytochemical characterization and antioxidant, antibacterial and antimutagenic activities of aqueous extract from leaves of Alchornea glandulosa.

Plant extracts exist as a complex matrix which serves as a source of numerous bioactive metabolites. The ultra performance liquid chromatography with diode-array detection-coupled electrospray ionization-mass spectrometry/mass spectrometry technique was used to characterize the aqueous extract from leaves of Alchornea glandulosa (EAG), a species popularly used to treat gastrointestinal problems as an antiulcer agent. Quantification of phenolic derivatives was determined using Folin?Ciocalteu and aluminum trichloride (AlCl3) methods. In addition, antioxidant (2,2-diphenyl-1-picrylhydrazyl [DPPH? ] radical scavenging, ?-carotene?linoleic acid, and lipid peroxidation), antibacterial (agar well diffusion method and minimum inhibitory concentration), antimutagenic (Ames test), and antigenotoxic (plasmid cleavage) assays were also performed on this plant extract. The ellagitannin tris-galloyl-hexahydroxydiphenic acid-glucose was identified as the predominant compound along with tannins as majority metabolites. EAG showed high antioxidant activity accompanied by moderate antibacterial activity against Staphylococcus aureus. The highest antimutagenic activity was observed for TA97 strain without metabolic activation (S9) and with metabolic activation, TA100 and TA102 were completely inhibited. In addition, EAG exhibited potential signs of antigenotoxic action. The high antioxidant and antimutagenic activity observed for EAG suggests important therapeutic uses that still need to be verified in future studies