Herbal medicines containingPassifloraspecies have been widely used to treat anxiety since ancient times. The speciesPassiflora incarnataL. is included in many Pharmacopoeias, and it is the most used species in food, cosmetic, and pharmaceutical industries. However, there are around 600 species of the genusPassifloraand probably other species that can be used safely. Thus, this article was based on a search into the uses of the main species of the genusPassiflorawith anxiolytic activity and its main secondary metabolites and some pharmacological studies, patents, and registered products containingPassiflora.Furthermore, the Brazilian Regulatory Health Agency Datavisa, Medicines and Healthcare Products Regulatory Agency of the United Kingdom, and the European Medicines Agency websites were consulted. The results showed thatPassifloraspecies have health benefits but clinical trials are still scarce. The complexity ofPassifloraextracts creates challenges for the development of herbal medicines.P. incarnatais the most studied species of the genus and the most used in natural anxiolytic herbal medicine formulations. However, there are hundreds ofPassifloraspecies potentially useful for medicinal and nutraceutical purposes that are still little explored.
1 January 2019 in Journal of Enzyme Inhibition and Medicinal Chemistry
Inhibition of Leishmania arginase leads to a decrease in parasite growth and infectivity and thus represents an attractive therapeutic strategy. We evaluated the inhibitory potential of selected naturally occurring phenolic substances on Leishmania infantum arginase (ARGLi) and investigated their antileishmanial activity in vivo. ARGLi exhibited a Vmax of 0.28 ± 0.016 mM/min and a Km of 5.1 ± 1.1 mM for L-arginine. The phenylpropanoids rosmarinic acid and caffeic acid (100 µM) showed percentages of inhibition of 71.48 ± 0.85% and 56.98 ± 5.51%, respectively. Moreover, rosmarinic acid and caffeic acid displayed the greatest effects against L. infantum with IC50 values of 57.3 ± 2.65 and 60.8 ± 11 μM for promastigotes, and 7.9 ± 1.7 and 21.9 ± 5.0 µM for intracellular amastigotes, respectively. Only caffeic acid significantly increased nitric oxide production by infected macrophages. Altogether, our results broaden the current spectrum of known arginase inhibitors and revealed promising drug candidates for the therapy of visceral leishmaniasis.
Based on the ethnopharmacological evidences about the antileishmanial activity ofCopaiferaspp. oleoresins, the effects of crude extracts and fractions of oleoresin of two specimens fromCopaifera pauperawere evaluated onLeishmania amazonensisandLeishmania infantumstrains. The oleoresin rich inα-copaene (38.8%) exhibited the best activity againstL. amazonensis(IC50= 62.5 μg/mL) and againstL. infantum(IC50= 65.9 μg/mL). The sesquiterpeneα-copaene isolated was tested alone and exhibited high antileishmanial activityin vitrowith IC50values forL. amazonensisandL. infantumof 17.2 and 11.4 μg/mL, respectively. In order to increase antileishmanial activity, nanoemulsions containing copaiba oleoresin andα-copaene were developed and assayed againstL. amazonensisandL. infantumpromastigotes. The nanoemulsion containingα-copaene (NANOCOPAEN) showed the best activity against both species, with IC50of 2.5 and 2.2 μg/mL, respectively. This is the first report about the antileishmanial activity ofα-copaene.
The difficulties encountered and the numerous side effects present in the treatment of cutaneous leishmaniasis have encouraged the research for new compounds that can complement or replace existing treatment. The growing scientific interest in the study of plants, which are already used in folk remedies, has led our group to test Endlicheria bracteolata essential oil against Leishmania amazonensis. Several species of the Lauraceae family, or their compounds, have relevant antiprotozoal activities Therefore, the biological potential on L. amazonensis forms from the essential oil of Endlicheria bracteolata leaves was verified for the first time in that work. The antileishmanial activity was evaluated against promastigotes and intracellular amastigotes, and cytotoxicity were performed with J774.G8, which were incubated with different concentrations of E. bracteolata essential oil. Transmission electron microscopy and flow cytometry were performed with E. bracteolata essential oil IC50. Promastigote forms showed E. bracteolata essential oil IC50 of 7.945 ± 1.285 µg/mL (24 h) and 6.186 ± 1.226 µg/mL (48 h), while for intracellular amastigote forms it was 3.546 ± 1.184 µg/mL (24 h). The CC50 was 15.14 ± 0.090 µg/mL showing that E. bracteolata essential oil is less toxic to macrophages than to parasites. Transmission electron microscopy showed that E. bracteolata essential oil treatment is capable of inducing mitochondrial damage to promastigote and intracellular amastigote forms, while flow cytometry showed ΔѰm disruption in treated parasites. These results could bring about new possibilities to develop products based on E. bracteolata essential oil to treat cutaneous leishmaniasis, especially for people who cannot receive the conventional therapy.
Species of the genusAlpiniaare widely used by the population and have many described biological activities, including activity against insects. In this paper, we describe the bioactivity of the essential oil of two species ofAlpiniagenus,A. zerumbetandA. vittata, againstRhodnius nasutus, a vector of Chagas disease. The essential oils of these two species were obtained by hydrodistillation and analyzed by GC-MS. The main constituent ofA. zerumbetessential oil (OLALPZER) was terpinen-4-ol, which represented 19.7% of the total components identified. In the essential oil ofA. vittata(OLALPVIT) the monoterpeneβ-pinene (35.3%) was the main constituent. The essential oils and their main constituents were topically applied onR. nasutusfifth-instar nymphs. In the first 10 min of application, OLALPVIT and OLALPZER at 125 μg/mL provoked 73.3% and 83.3% of mortality, respectively. Terpinen-4-ol at 25 μg/mL andβ-pinene at 44 μg/mL provoked 100% of mortality. The monitoring of resistant insects showed that both essential oils exhibited antifeedant activity. These results suggest the potential use ofA. zerumbetandA. vittataessential oils and their major constituents to controlR. nasutuspopulation.