LC–MS characterization, anti-kinetoplastide and cytotoxic activities of natural products from Eugenia jambolana Lam. and Eugenia uniflora

Objective: To evaluate the trypanocidal, leishmanicidal and cytotoxic activity of Eugenia jambolana(E. jambolana) and Eugenia uniflora(E. uniflora) extracts and fractions.Methods: The products were characterized by LC–MS. Antiparasitic assays were performed and cytotoxicity was evaluated in fibroblastos. In vitro assays were performed using spectrophotometric evaluation. All assays were performed in thrice.Results: The results showed that the extracts and the tannic fraction from E. jambolana inhibited 100% of the epimastigote lines. The ethanolic extract was the most efficient in all concentrations tested against the three parasite strains. In the cytotoxicity assay the flavonoid fraction showed low toxicity. All E. uniflora samples showed cytotoxicity at the highest concentration tested, but the extract showed no toxic effect on the fibroblasts at the lowest concentration. The flavonoid and tannic fractions were more efficient against Leishmania braziliensis promastigotes compared to the extract. However, the extracts and the tannic fraction were more effective against Leishmania infantum strains. The effect on epimastigote cells was observed at all concentrations tested, with all E. uniflora samples. However, the samples were more effective at the highest concentration, where there was inhibition in 100% of the Trypanosoma cruzi strains.Conclusions: The species E. jambolana and E. uniflora presented antiparasitic activity against all tested parasite strains, indicating that these species can serve as an alternative therapy as they were efficient in the tests performed. The E. uniflora extract and the E. jambolana flavonoid fraction presented a low cytotoxicity, opening the floor for new biological studies.

Polyphenolic composition, antibacterial, modulator and neuroprotective activity of Tarenaya spinosa(Jacq.) Raf.(Cleomaceae)

Objective: To evaluate the antibacterial activity and neuroprotective capacity of the ethanolic and aqueous extracts of Tarenaya spinosa(T. spinosa) as well as to determine and quantify some of its polyphenols by high performance liquid chromatography with diode-array detection(HPLC-DAD). Methods: The bacterial Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa strains, grown in Heart Agar Infusion, were tested. The drugs gentamicin, norfloxacin and imipenem were used to evaluate the modulating or antagonistic capacity of the T. spinosa extracts. The extract was analysed by HPLC-DAD to determine the main phenolic compounds. For the cell viability tests, individual heads of the Nauphoeta cinerea arthropod model were removed, homogenized in Trifluoromethyl ketone and centrifuged afterwards. Subsequently, 20 μL of NaN O2 were added to the biological material, except in the control group, to evaluate the protection capacity of the extracts. The homogenate of the insect heads was incubated for 2 h in tubes containing tetrazolium bromide. Results: HPLC-DAD demonstrated that the ethanolic extract of T. spinosa presented caffeic acid as the major compound. The ethanolic extract also showed neuroprotective effects at concentrations ≥ 10 μg/mL, while aqueous extract was shown to have a protective effect only at the concentration of 100 μg/mL. The aqueous extract demonstrated a clinically relevant antibacterial activity against the Staphylococcus aureus multidrug resistant strain-MDR, with MIC 512 μg/m L. However, when the extracts were associated with gentamicin and imipenem, a synergism was detected against Staphylococcus aureus and Escherichia coli MDR strains. Conclusions: Although it does not present an antibacterial action, the extracts of T. spinosa can be used in the pharmaceutical industries since its extracts show modulating action of drugs. Besides, these natural products have neuroprotective capacity.

Antibacterial enhancement of antibiotic activity by Enterolobium contortisiliquum(Vell.)Morong

Objective: To identify the main chemical classes of compounds from aqueous extract of Enterolobium contortisiliquum(E. contortisiliquum) seed bark and to evaluate its antibacterial activity, as well as its potential to increase the activity of antibiotics against strains of Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli.Methods: Different classes of compounds in the aqueous extract of E. contortisiliquum were evaluated based on the visual changes in the coloration and the formation of precipitate after the addition of specific reagents. The antibacterial activity of the extract and its potential to increase of antibiotic activity of antibiotics drugs, gentamicin and norfloxacin was determined by using the microdilution method.Results: Our results demonstrated that the following secondary metabolites were presented in E. contortisiliquum seed bark: flavones, flavonols, xanthones, flavononols,chalcones, aurones, flavones and catechins. The extract itself had very low antibacterial activity against all bacterial strains tested(MIC ≥ 1024 μg/m L), but there was an increase in the antibiotic activity of gentamicin and norfloxacin when combined in the subinhibitory concentration(i.e., MIC/8).Conclusions: Our data suggests that E. contortisiliquum seed bark may be an alternative source for new drugs with the potential to increase antibiotic activity against different strains of bacteria.

Chemical composition, antiparasitic and cytotoxic activities of aqueous extracts of Ziziphus joazeiro Mart

Objective: To compare the in vitro antiparasitic activity of aqueous extracts from Ziziphus joazeiro leaves and stem bark against Trypanosoma cruzi, Leishmania braziliensis, and Leishmania infantum, as well as to evaluate its cytotoxicity in mammalian cells, in addition to identifying the chemical composition of the extracts. Methods: Ziziphus joazeiro leaf and stem bark aqueous extracts were prepared by cold extraction maceration and subjected to ultra-efficient liquid chromatography coupled to a quadrupole/time of flight system. The susceptibility assays used Trypanosoma cruzi CLB5 strains and promastigote forms of Leishmania braziliensis and Leishmania infantum for antiparasitic activity of the extracts. Moreover, mammalian fibroblasts NCTC clone 929 were used for cytotoxicity analysis. Results: Terpenoid compounds, flavonoids and phenolic acid were identified in extracts. The stem bark aqueous extracts presented more significant results in terms of antiparasitic activity compared with the leaf aqueous extracts, especially against Leishmania braziliensis and Leishmania infantum promastigote forms with an IC50 < 500 μg/mL. The cytotoxicity evaluation showed moderate toxicity of the stem bark aqueous extracts, which is relevant information for the rational use of this plant part since it is widely used by the population. Conclusions: These preliminary results may contribute to the formulation of new therapeutic agents against this group of neglected diseases, so further investigations are required to delineate the mechanisms of action mainly of the aqueous extract of stem bark of Ziziphus joazeiro.