Background: The Parque Estadual do Forno Grande is a fully protected area in the southern Espírito Santo State, Brazil. It belongs to the Atlantic Forest domain, with predominantly dense, ombrophilous, seasonal semi-deciduous forests and herbaceous/shrubby vegetation on rock outcrops. The area is recognised as highly important for conservation, designated as a priority biological area for protecting the Atlantic Forest's biodiversity.
View Article and Find Full Text PDFBackground: The Atlantic Forest is one of the most diverse and threatened phytogeographical domains in the world. Despite that, it includes regions with poor floristic knowledge, even in protected areas. Although the importance of protected areas in conserving the Atlantic Forest hotspot is undisputed, it is necessary to recognise the floristic richness of these areas to propose effective conservation actions.
View Article and Find Full Text PDFAs part of our continuous research for the discovery of bioactive compounds against Trypanosoma cruzi and Leishmania infantum, the alkaloid (6aS)-dicentrine (1) was oxidized to afford (6aS,6S)- (2) and (6aS,6R)- (3) dicentrine-N-oxides. Evaluation of the cytotoxicity against NCTC cells indicated that 2 and 3 are non-toxic (CC>200 μM) whereas 1 demonstrated CC of 52.0 μM.
View Article and Find Full Text PDFIn the present work, the hexane extract of aerial parts of Kunth. was subjected to chromatographic fractionation to afford two alkyl phenylpropanoids: -docosyl (-coumarate () and -tetracosyl -coumarate () as well as five diterpenes: kaurenoic acid (), grandifloric acid (), 15β-senecioyl-oxy--kaur-16-en-19-oic acid (), and 15-oxo--kaurenoic acid (). Using an assay with macrophages infected with , compounds and demonstrated high potency against intracellular amastigotes, with EC values of 7.
View Article and Find Full Text PDFThe hexane extract from twigs of Piper truncatum Vell (Piperaceae) displayed activity against Trypanosoma cruzi and was subjected to chromatographic steps to afford six dibenzylbutyrolactolic lignans, being four knowns: cubebin (1), (-)-9α-O-methylcubebin (2), (+)-9β-O-methylcubebinin (3) and 3,4-dimethoxy-3,4-demethylenedioxycubebin (4) as well as two new, named truncatin A (5) and B (6). Initially, in vitro activity against trypomastigotes was evaluated and compounds 1, 4 and 6 exhibited EC values of 41.6, 21.
View Article and Find Full Text PDFEndemic in 21 countries, Chagas disease, also known as American Trypanosomiasis, is a neglected tropical disease (NTD) caused by the protozoan parasite . The available drugs for the treatment of this disease, benznidazole and nifurtimox, are outdated and display severe side effects. Thus, the discovery of new drugs is crucial.
View Article and Find Full Text PDFMenthinae, one of the five subtribes of Mentheae (Lamiaceae), with ca. 735 species, is represented in Brazil by a wide range of herbs and shrubs. During an investigation of the taxonomic history of the group for the Flora e Funga do Brasil project, several nomenclatural issues with typifications in the group have been identified.
View Article and Find Full Text PDFThis study presents the cytotoxic activity evaluation of the natural diterpenes ent-kaurenoic acid (1) and its 15β-hydroxy (2), 15β-senecioyloxy (3), and 15β-tiglinoyloxy (4) derivatives, isolated from Brazilian native plants, Baccharis retusa and B. lateralis (Asteraceae). Using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) colorimetric assay, it was observed that compound 1 displayed in vitro activity towards the aggressive MDA-MB-231 adenocarcinoma cell line and reduced toxicity against MCF-10A nontumorigenic epithelial cells, indicating expressive selectivity.
View Article and Find Full Text PDFBackground: The Atlantic Forest is one of the most threatened biomes in the world. Despite that, this biome still includes many areas that are poorly known floristically, including several protected areas, such as the "Floresta Nacional do Rio Preto" ("Flona do Rio Preto"), located in the Brazilian State of Espírito Santo. This study used a published vascular plant species list for this protected area from the "Catálogo de Plantas das Unidades de Conservação do Brasil" as the basis to synthesise the species richness, endemism, conservation and new species occurrences found in the "Flona do Rio Preto".
View Article and Find Full Text PDFBackground: In the present work the bioactivity-guided fractionation of n-hexane extract from aerial parts of Baccharis sphenophylla (Asteraceae) against trypomastigote forms of Trypanosoma cruzi was performed.
Purpose: To evaluate the antitrypanosomal potential of diterpenes ent‑kaurenoic (1), grandifloric (2). and 15β-tiglinoyloxy‑ent-kaurenoic (3) acids, isolated from n-hexane extract from aerial parts of B.
The search for the pharmacophore of a bioactive compound, crucial for drug discovery studies, involves the adequate arrangement of different atoms in the molecule. As part of a continuous work aiming discovery of new drug candidates against the protozoan parasite Trypanosoma cruzi, the hexane extract of Hydrocotyle bonariensis was subjected to a bioactivity-guided fractionation to afford two chemically related dibenzylbutyrolactone lignans - hinokinin (1) and hibalactone (2). Compounds 1 and 2 showed activity against trypomastigote with EC values of 17.
View Article and Find Full Text PDFPhenylphenalenones, metabolites found in (Haemodoraceae), are a class of specialized metabolites with many biological activities, being phytoalexins in banana plants. In the constant search to solve the problem of glyphosate and to avoid resistance to commercial herbicides, this work aimed to investigate the phytotoxic effect of the methanolic extract of seeds. The chemical composition of the seed extract was directly investigated by NMR and UPLC-QToF MS and the pre- and post-emergence phytotoxic effect on a eudicotyledonous model () and a monocotyledonous model () was evaluated through germination and seedling growth tests.
View Article and Find Full Text PDFThe hexane extract from aerial parts Baccharis sphenophylla Dusén ex Malme (Asteraceae) displayed activity against amastigote forms of Trypanossoma cruzi and was subjected to chromatographic steps to afford one unreported - 7α-hydroxy-ent-abieta-8(14),13(15)-dien-16,12β-olide (1) and three known diterpenes - ent-kaur-16-en-19-oic acid, (2), grandifloric acid (3), and 15β-tiglinoyloxy-ent-kaur-16-en-19-oic acid (4), two sesquiterpenes - spathulenol (5) and oplopanone (6) - as well as hexacosyl p-coumarate (7). Isolated compounds were characterized by NMR and ESI-HR-MS spectra and were evaluated in vitro for activity against amastigote forms of the parasite T. cruzi - the relevant clinical form in the chronic phase of Chagas disease.
View Article and Find Full Text PDFTwigs of were extracted using a solution of the ionic liquid 1-butyl-3-methylimidazolium bromide (BMImBr) in HO, assisted by microwave (MAE). After successive chromatographic steps, one sesquiterpene, costic acid, and three new related lactones, 3(7)--3-hexadec-21-enylidene-5-(hydroxymethyl)tetrahydrofuran-2-one (), 3(7)--3-hexadecylidene-5-(hydroxymethyl)tetrahydrofuran-2-one (), and 3(7)--3-docosylidene-5-(hydroxymethyl)tetrahydrofuran-2-one (), were isolated. After structural elucidation using IR, UV, HRESIMS, NMR, ECD, and VCD, compounds were tested against trypomastigote forms of .
View Article and Find Full Text PDFOne new aporphine, dicentrine-β-N-oxide (1), together with five related known alkaloids dehydrodicentrine (2), predicentrine (3), N-methyllaurotetanine (4), cassythicine (5), and dicentrine (6) were isolated from the leaves of Ocotea puberula (Lauraceae). Antiprotozoal activity of the isolated compounds was evaluated in vitro against trypomastigote forms of Trypanosoma cruzi. Among the tested compounds, alkaloid 1 exhibited higher potential with EC value of 18.
View Article and Find Full Text PDFBackground: Brazilian protected areas are essential for plant conservation in the Atlantic Forest domain, one of the 36 global biodiversity hotspots. A major challenge for improving conservation actions is to know the plant richness, protected by these areas. Online databases offer an accessible way to build plant species lists and to provide relevant information about biodiversity.
View Article and Find Full Text PDFPraziquantel is the only available drug to treat schistosomiasis, and therefore, urgent studies must be performed to identify new anthelmintic agents. This study reports the anthelmintic evaluation of two related -kaurane diterpenes isolated from aerial parts of (Asteraceae), -kaur-16-en-19-oic acid () and 15β-senecioyl-oxy--kaur-16-en-19-oic acid () against and in a murine model of schistosomiasis. Both compounds exhibited activity with lethal concentration 50% (LC) values of 26.
View Article and Find Full Text PDFIn the present work, the oxoaporphine alkaloid dicentrinone was isolated, for the first time, from leaves of Ocotea puberula (Lauraceae). This alkaloid exhibited antiparasitic activity against trypomastigote forms of Trypanosoma cruzi (IC of 16.4 ± 1.
View Article and Find Full Text PDFSchistosomiasis is one of the most important parasitic infections in terms of its negative effects on public health and economics. Since praziquantel is currently the only drug available to treat schistosomiasis, there is an urgent need to identify new anthelmintic agents. Piplartine, also known as piperlongumine, is a biologically active alkaloid/amide from peppers that can be detected in high amounts in the roots of Piper tuberculatum.
View Article and Find Full Text PDFBioorg Chem
January 2020
As part of our continuous studies on prospecting metabolites from Brazilian plant species with pharmacologic activity against Trypanosoma cruzi, the n-hexane extract from twigs of Nectandra barbellata (Lauraceae) was subjected to a bioactivity-guided fractionation to afford the sesquiterpene costic acid. As results, costic acid induced a trypanocidal effect with IC of 37.8 and 7.
View Article and Find Full Text PDFBackground: From a previous screening of Brazilian biodiversity for antitrypanosomal activity, the n-hexane extract from twigs of Nectandra oppositifolia (Lauraceae) demonstrated in vitro activity against Trypanosoma cruzi.
Purpose: To perform the isolation and chemical characterization of bioactive compounds from n-hexane extract from twigs of N. oppositifolia and evaluate their therapeutical potential as well as to elucidate their mechanism of action against T.
Baccharis retusa, a medicinal Brazilian plant from Asteraceae, has been used in Brazilian folk medicine to treatment of several illnesses, including parasitic diseases. Bioactivity-guided fractionation of the n-hexane extract from the aerial parts of B. retusa resulted in the isolation and characterization of three active related diterpenes: ent-15β-senecioyl-oxy-kaur-16-en-19-oic acid (1), ent-kaur-16-en-19-oic (2) and ent-16-oxo-17-nor-kauran-19-oic (3) acids.
View Article and Find Full Text PDFis a Brazilian plant species that has been used in folk medicine to treat a range of diseases. Our ongoing work focuses on the discovery of new bioactive natural products derived from Brazilian flora. The current study describes the identification of cytotoxic compounds from the EtOH extract of leaves from using bioactivity-guided fractionation.
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