Therapeutic Effects of Morinda citrifolia Linn. (Noni) Aqueous Fruit Extract on the Glucose and Lipid Metabolism in High-Fat/High-Fructose-Fed Swiss Mice.

The aim of this study was to evaluate the therapeutic effects of two different doses (250 and 500 mg/kg) of Morinda citrifolia fruit aqueous extract (AE) in high-fat/high-fructose-fed Swiss mice. The food intake, body weight, serum biochemical, oral glucose tolerance test (OGTT), and enzyme-linked immunosorbent assay (ELISA), as well as histological analyses of the liver, pancreatic, and epididymal adipose tissue, were used to determine the biochemical and histological parameters. The chemical profile of the extract was determined by ultra-fast liquid chromatography-diode array detector-tandem mass spectrometry (UFLC-DAD-MS), and quantitative real-time PCR (qRT-PCR) was used to evaluate the gene expressions involved in the lipid and glucose metabolism, such as peroxisome proliferative-activated receptors-γ (PPAR-γ), -α (PPAR-α), fatty acid synthase (FAS), glucose-6-phosphatase (G6P), sterol regulatory binding protein-1c (SREBP-1c), carbohydrate-responsive element-binding protein (ChREBP), and fetuin-A. Seventeen compounds were tentatively identified, including iridoids, noniosides, and the flavonoid rutin. The higher dose of AE (AE 500 mg/kg) was demonstrated to improve the glucose tolerance; however, both doses did not have effects on the other metabolic and histological parameters. AE at 500 mg/kg downregulated the PPAR-γ, SREBP-1c, and fetuin-A mRNA in the liver and upregulated the PPAR-α mRNA in white adipose tissue, suggesting that the hypoglycemic effects could be associated with the expression of genes involved in de novo lipogenesis.

Chemical profile and gastroprotective effect of Jatropha elliptica (Pohl) Oken roots.

Jatropha elliptica (Pohl) Oken (Euphorbiaceae) roots are used in folk medicine to treat gastric ulcers. The purpose of this work was to evaluate the gastroprotective activity of ethanol extract (JER) and hexane fraction (ERH) of J. elliptica roots in mice, as well as to analyze the acute toxicity of the extract and identify the potential active compounds. No signs of toxicity were observed in JER. In both acidified ethanol and indometacin-induced gastric ulcer models, all doses tested of JER and ERH significantly reduced gastric lesions. Dereplication of JER was performed by HPLC-DAD-ESI-MS/MS and resulted in the annotation of compounds fraxetin, propacin, jatrophone and jatropholones A and B. GC-MS analysis of ERH revealed the diterpenes jatrophone, jatropholone A and jatropholone B as the major components. The chemical study of this fraction has led to the isolation of these compounds, in addition to the sequiterpene cyperenoic acid and the diterpene 2ß-hydroxyjatrophone, both reported for the first time in J. elliptica. The isolated compounds were tested against L929 cells and only cyperenoic acid and the mixture of jatropholones A and B did not show toxicity, being then selected as good candidates for bioassays using acidified ethanol-induced gastric ulcer model. Cyperenoic acid significantly decreased gastric lesions and preserved gastric mucus layer. The mixture of jatropholones A and B caused a smaller reduction of gastric lesions, without preservation of the gastric mucus layer. The study showed that J. elliptica roots present gastroprotective activity in mice, without causing acute toxic effects. The activity is related, at least in part, to the occurrence of terpenes, mainly the sesquiterpene cyperenoic acid.

Nutraceutical and Medicinal Potential of the Morus Species in Metabolic Dysfunctions.

Many populations use medicinal plants as a therapeutic treatment, due to their lower cost and greater access. Among the plant species used for medicinal purposes are those of the genus Morus. The most known species are Morus alba, rubra, and nigra. This review aims to collect data from the literature, predominantly from cell and animal studies, which presents a possible nutraceutical and medicinal potential of the species Morus for use in metabolic dysfunctions. The fruits and leaves of mulberry are used for therapeutic purposes. For scientific confirmation of these effects, they were studied for laxative properties, antibacterial activity, anti-atherogenic activity, and hepatoprotective function. Furthermore, the genus Morus is recognized for the treatment and prevention of diabetes mellitus, through its hypoglycemic action. It may also provide health benefits through immunomodulatory, anti-inflammatory, and anti-nociceptive effects. It has been found that the Morus species have phenolic compounds, flavonoids, and anthocyanins that act as important antioxidants and promote beneficial effects on human health. These phytochemical compounds differ among species. Blackberry (Morus nigra) are rich in flavonoids, while the white mulberry (Morus alba) has low concentrations of flavonoids and anthocyanins. In addition, another important factor is to ensure a complete exemption of toxic risks in the use of medicinal plants for the treatment of diseases. Studies have shown no toxic effects by the administration of extracts of Morus species. Thus, the mulberry tree presents nutraceutical potential. It is therefore a promising alternative for medicinal products based on medicinal plants.

Seasonal effects and antifungal activity from bark chemical constituents of Sterculia apetala (Malvaceae) at Pantanal of Miranda, Mato Grosso do Sul, Brazil / Efeitos sazonais e atividade antifúngica dos constituintes químicos das cascas de Sterculia apetala (Malvaceae) no Pantanal de Miranda, Mato Grosso do Sul, Brasil

In the Southern Pantanal, the hyacinth macaw (Anodorhynchus hyacinthinus), an endangered species, often chooses the manduvi tree (Sterculia apetala) as a nesting site, because of its physical properties. In addition, the chemical composition of the wood may also contribute to a nesting selection by the hyacinth macaws. The objective of this study was to determine the main chemical components of S. apetala bark for two seasons, and evaluate its fungicidal potential. Bark samples from S. apetala trees with and without nests of A. hyacinthinus were collected in January (wet season) and August (dry season) of 2012. The inhibition of mycelium growth (MGI) from tree samples with and without nests were assessed using a phytochemical analysis to evaluate their antifungal activity against Trichoderma sp. Phytochemical analysis confirmed the presence of phenolic compounds and flavonoids. In both seasons, samples obtained from nested trees had higher content of total phenols than those collected from non-nested trees. The average content of total flavonoids was higher in January for samples with nest and in August for samples without nest. All selected samples showed antifungal activity, and those with nest collected in August (peak of hyacinth macaw breeding) resulted in an MGI of 51.3%. Therefore, this percentage, related to the content of flavonoids and the presence of coumarins, may influence the reproductive success of hyacinth macaws and other species of birds, in this region. This is the first chemical study report with the stem bark of S. apetala.

No Pantanal Sul, as araras-azuis (Anodorhynchus hyacinthinus), espécie em extinção, escolhem preferencialmente o manduvi (Sterculia apetala) como local de nidificação devido principalmente às características físicas da árvore. Porém, a composição química da madeira também pode interferir nesta seleção. Os objetivos deste trabalho foram determinar as principais classes de substâncias químicas presentes nas cascas de S. apetala em duas épocas do ano e seu potencial antifúngico. As cascas de árvores, com e sem a presença de ninhos de A. hyacinthinus, foram coletadas em janeiro (período de chuvas) e agosto (período de seca) de 2012. Por meio das análises fitoquímicas e quantificação de flavonóides, foram selecionadas amostras de uma árvore com ninho e outra sem ninho para determinar seu potencial antifúngico frente à Trichoderma sp. através da porcentagem de inibição do crescimento micelial (PIC). A investigação fitoquímica do extrato etanólico das cascas revelou a predominância de compostos fenólicos e flavonóides. O teor médio de fenóis totais foi superior para as amostras com ninho, em relação às sem ninho, nos dois períodos de coleta e, para flavonóides, os valores foram superiores em janeiro para a amostra com ninho e em agosto, para sem ninho. As amostras selecionadas apresentaram potencial antifúngico, sendo que com ninho, coletada em agosto (auge do período de reprodução das araras-azuis), resultou em um PIC de 51,3%, valor relacionado aos flavonóides e as cumarinas, fator que pode influenciar o sucesso reprodutivo da arara azul e outras espécies de aves nesta região. Este trabalho foi o primeiro a identificar os componentes químicos da casca do tronco de S. apetala.

Antiproliferative activity of pristimerin isolated from Maytenus ilicifolia (Celastraceae) in human HL-60 cells.

Pristimerin has been shown to be cytotoxic to several cancer cell lines. In the present work, the cytotoxicity of pristimerin was evaluated in human tumor cell lines and in human peripheral blood mononuclear cells (PBMC). This work also examined the effects of pristimerin (0.4; 0.8 and 1.7 microM) in HL-60 cells, after 6, 12 and 24h of exposure. Pristimerin reduced the number of viable cells and increased number of non-viable cells in a concentration-dependent manner by tripan blue test showing morphological changes consistent with apoptosis. Nevertheless, pristimerin was not selective to cancer cells, since it inhibited PBMC proliferation with an IC50 of 0.88 microM. DNA synthesis inhibition assessed by 5-bromo-2'-deoxyuridine (BrdU) incorporation in HL-60 cells was 70% and 83% for the concentrations of 0.4 and 0.8 microM, respectively. Pristimerin (10 and 20 microM) was not able to inhibit topoisomerase I. In AO/EB (acridine orange/ethidium bromide) staining, all tested concentrations reduced the number of HL-60 viable cells, with the occurrence of necrosis and apoptosis in a concentration-dependent manner, results in agreement with trypan blue exclusion findings. The analysis of membrane integrity and internucleosomal DNA fragmentation by flow cytometry in the presence of pristimerin indicated that treated cells underwent apoptosis. The present data point to the importance of pristimerin as representative of an emerging class of potential anticancer chemicals, exhibiting an antiproliferative effect by inhibiting DNA synthesis and triggering apoptosis.

Biomimetic synthesis of xuxuarines Ealpha and Ebeta: structure revision of Rzedowskia bistriterpenoids.

Reaction of pristimerin with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) resulted in a biomimetic-type coupling leading to xuxuarines Ealpha and Ebeta and not the previously reported Rzedowskia bistriterpenoids I and II suggesting that the structures proposed for these natural products need revision. A product obtained in this reaction by an unusual Diels-Alder addition followed by retro-Diels-Alder-type elimination was characterized as pristimerin dicyanophenalenedione. Complete 1H, and 13C NMR spectral assignments of xuxuarines Ealpha and Ebeta have been made by the application of 1D and 2D NMR techniques.

Antioxidant flavan-3-ols and flavonol glycosides from Maytenus aquifolium.

TLC autographic assay revealed, in the EtOAc extract obtained from leaves and root bark of Maytenus aquifolium (Celastraceae), the presence of fi ve compounds exhibiting antioxidant properties towards beta-carotene. They were isolated and identified as epigallocatechin (1), (+) ouratea-catechin (2), proanthocyanidin (3), kaempferol 3-O-alpha-L-rhamnopyranosyl (1-->6)-O-[beta-D-glucopyranosyl (1-->3)-O-alpha-L-rhamnopyranosyl-(1-->2)]-O-beta-D-glucopyranosyl (4) and quercetin 3-O-alpha-L-rhamnopyranosyl (1-->6)-O-[beta-D-glucopyranosyl (1-->3)-O-alpha-L-rhamnopyranosyl-(1-->2)]-O-beta-D-glucopyranosyl (5). The isolates were investigated for their redox properties using cyclic voltammetry and for their radical scavenging abilities through spectrophotometric assay on the reduction of 2,2-diphenyl-pycryl hydrazyl (DPPH). These results were correlated to the inhibition of beta-carotene bleaching on TLC autographic assay and to structural features of the flavonoids.

Quantitative determination for cytotoxic Friedo-nor-oleanane derivatives from five morphological types of Maytenus ilicifolia (Celastraceae) by reverse-phase high-performance liquid chromatography.

Five different morphological types of Maytenus ilicifolia of the same age and harvested under the same conditions showed distinct accumulations of some friedo-nor-oleananes. A rapid, sensitive and reliable reverse-phase HPLC method (employing an external standard) was used for the determination of the cytotoxic triterpenoids, 20 alpha-hydroxymaytenin, 22 beta-hydroxymaytenin, maytenin, celastrol and pristimerin in each of the five types. Well resolved peaks with good detection response and linearity in the range 1.0-100 micrograms/mL were obtained.