Cláudia Quintino da Rocha

Anti-inflammatory and antinociceptive effects of Arrabidaea brachypoda (DC.) Bureau roots.

AIM OF THE STUDY Arrabidaea brachypoda (DC.) Bureau has been used to relieve general pain, painful joints and kidney stones in Brazilian folk medicine. Nevertheless, scientific information regarding this species is scarce; there are no reports related to its possible analgesic and anti-inflammatory effects. This study was aimed at evaluating the traditional use of Arrabidaea brachypoda root using in vivo inflammatory and nociceptive models. MATERIALS AND METHODS Carrageenan-induced paw edema, peritonitis and fibrovascular tissue growth induced by s.c. cotton pellet implantation were used to investigate the anti-inflammatory activity of Arrabidaea brachypoda roots ethanolic extract (AbEE) in rats. Formalin and acetic acid-induced writhing tests were used to investigate the antinociceptive activity in mice. High-performance liquid chromatography (HPLC) was used to determine the fingerprint chromatogram of AbEE. RESULTS The AbEE at test doses of 30-300 mg/kg p.o. demonstrated anti-inflammatory effects. AbEE reduced paw edema induced by carrageenan, inhibited leukocyte recruitment into the peritoneal cavity and, in the model of chronic inflammation using the cotton pellet-induced fibrovascular tissue growth in rats, significantly inhibited the formation of granulomatous tissue. The extracts at test doses of 30-300 mg/kg p.o. clearly demonstrated antinociceptive activity, except during the first phase of the formalin test. The presence of quercetin and phenolic compounds in the extract Arrabidaea brachypoda was confirmed using HPLC. CONCLUSION Arrabidaea brachypoda ethanol extract markedly demonstrated anti-inflammatory action in rats and antinociceptive activity in mice, which supports the previous claims of traditional use.

Antinociceptive and anti-inflammatory properties of 7-epiclusianone, a prenylated benzophenone from Garcinia brasiliensis

7-Epiclusianone, a natural prenylated benzophenone, was extracted from Garcinia brasiliensis Planch. & Triana (Clusiaceae), a native plant commonly known as bacupari and used in traditional Brazilian medicine for the treatment of inflammatory diseases. As a result of the wide spectrum of biological activities attributed to polyisoprenylated benzophenones, the aim of this study was to evaluate the analgesic and anti-inflammatory effects of 7-epiclusianone using two animal models. Carrageenan-induced paw oedema and peritonitis were used to investigate the anti-inflammatory activity of 7-epiclusianone in rats. The acetic acid-induced writhing, formalin and hot-plate tests were used to investigate its antinociceptive activity in mice. At test doses of 5, 10 and 15 mg/kg p.o., 7-epiclusianone had an anti-inflammatory effect as demonstrated by the reduction of paw oedema induced by carrageenan and the inhibition of leukocyte recruitment into the peritoneal cavity. At the same doses, 7-epiclusianone inhibited nociception induced by an intraperitoneal injection of acetic acid, observed by the decrease in the number of writhing episodes. Additionally, 7-epiclusianone decreased licking time caused by a subplantar injection of formalin. Moreover, the hot plate test produced a significant increase in latency reaction, demonstrating an antinociceptive effect. The experimental data demonstrated that the polyisoprenylated benzophenone 7-epiclusianone has remarkable anti-inflammatory and antinociceptive activities.

Antiinflammatory properties of Morus nigra leaves

The aim of the present study was to investigate antiinflammatory activity of the methylene chloride extract of Morus nigra in animal models. Carrageenan‐induced paw edema as well as fibrovascular tissue growth induced by s.c. cotton pellet implantation were used to investigate the antiinflammatory activity of Morus nigra extract (MnE) in rats. A HPLC fingerprint was used for phytochemical analysis of the extracts. The MnE at test doses of 100–300 mg/kg p.o. clearly demonstrated antiinflammatory effects by reduced paw edema induced by carragenan and significantly inhibited the formation of granulomatous tissue. In addition, chemical compounds isolated from Morus nigra, including betulinic acid, β‐sitosterol and germanicol, may be responsible for the antiinflammatory effect of the extract. Copyright

Anti-inflammatory and antinociceptive effects of Garcinia brasiliensis

AIM OF THE STUDY In Brazilian folk medicine, the leaves of Garcinia brasiliensis are used to treat tumors, inflammation of the urinary tract and arthritis as well as to relieve pain. Nevertheless, scientific information regarding Garcinia brasiliensis is limited; there are no reports related to its possible anti-inflammatory and antinociceptive effects. This study employed in vivo inflammatory and nociceptive models to evaluate the scientific basis for the traditional use of Garcinia brasiliensis. MATERIALS AND METHODS Carrageenan-induced paw edema, peritonitis and fibrovascular tissue growth induced by s.c. cotton pellet implantation were used to investigate the anti-inflammatory activity of Garcinia brasiliensis ethanolic extract (GbEE) in rats. Formalin and acetic acid-induced writhing tests were used to investigate the antinociceptive activity in mice. RESULTS GbEE at test doses of 30-300 mg/kg p.o. clearly demonstrated anti-inflammatory effects by reduced paw edema induced by carrageenan, inhibited leukocyte recruitment into the peritoneal cavity, and in the model of chronic inflammation using the cotton pellet-induced fibrovascular tissue growth in rats, the GbEE significantly inhibited the formation of granulomatous tissue. The extracts at test doses of 30-300 mg/kg, p.o., clearly demonstrated antinociceptive activity, except for the first phase of the formalin test. CONCLUSION GbEE markedly demonstrated anti-inflammatory action in rats and antinociceptive activity in mice, which supports previous claims of the traditional use of species of the Garcinia genus for inflammation and pain.

Dimeric Flavonoids from Arrabidaea brachypoda and Assessment of Their Anti-Trypanosoma cruzi Activity

The nonpolar fraction of an aqueous ethanol extract of the roots of Arrabidaea brachypoda, a Brazilian medicinal plant, demonstrated significant in vitro activity against Trypanosoma cruzi, the parasite responsible for Chagas disease. Targeted isolation of the active constituents led to the isolation of three new dimeric flavonoids (1-3), and their structures were elucidated using UV, NMR, and HRMS analysis, as well as by chemical derivatization. The anti-T. cruzi activity and cytotoxicity toward mammalian cells were determined for these substances. Compound 1 exhibited no activity toward T. cruzi, while flavonoids 2 and 3 exhibited selective activity against these trypomastigotes. Compounds 2 and 3 inhibited the parasite invasion process and its intracellular development in host cells with similar potencies to benznidazole. In addition, compound 2 reduced the blood parasitemia of T. cruzi-infected mice. This study has revealed that these two dimeric flavonoids represent potential anti-T. cruzi lead compounds for further drug development.

Ilex paraguariensis supplementation may be an effective nutritional approach to modulate oxidative stress during perimenopause

Abstract Perimenopause is a period in a womans life that precedes menopause and is characterized by hormonal changes that result in increased oxidative stress. Since oxidative stress is associated with age‐related diseases and perimenopausal symptoms including somato‐vegetative manifestations, nutritional antioxidant supplementation may be an effective approach to minimizing this stress. Mate tea (MT) (Ilex paraguariensis), a typical and inexpensive beverage consumed in the Brazilian south‐east, Argentina and Uruguay, increases antioxidant defense. We hypothesized that MT could minimize oxidative stress during perimenopause by modulating enzymatic antioxidant defense. To test this, we analyzed the lipid oxidative damage and antioxidant defense in erythrocytes and liver of rats, after MT treatment. Female Wistar rats (aged 16 months) in proven perimenopause period received 20 mg/kg BW/day of mate tea, by gavage (PM + MT group) or water (PM group). Female rats aged 4 months (AD group) received water. Erythrocytes and liver were used to determine lipid oxidative damage, determined by malondialdehyde (MDA); superoxide dismutase (SOD), glutathione peroxidase (GPx) and catalase (CAT) activities. Total plasma antioxidant capacity was examined by ferric reducing antioxidant power assay (FRAP) and estrogen by radioimmunoassay. MT increased FRAP and did not change estrogen levels. Increased SOD and GPx, and reduced MDA were observed in both tissues studied. Increased CAT activity was observed only in the liver. We confirmed the hypothesis that MT was capable of minimizing oxidative stress in this period of life by modulating antioxidant defense. HighlightsPerimenopause increases oxidative stress in female rats in a tissue‐dependent manner.Mate tea enhances antioxidant system during perimenopause in a tissue‐dependent manner.Mate tea may be used to reduce oxidative stress during perimenopause.

Anthelmintic activity of plant extracts from Brazilian savanna

Helminth infections represent a serious problem for the production of small ruminants that is currently aggravated by resistance to anthelmintic products and has induced a search for control alternatives, such as natural products. In this study, extracts of Turnera ulmifolia L. (leaves and roots), Parkia platycephala Benth. (leaves and seeds) and Dimorphandra gardneriana Tul. (leaves and bark), which have been cited in ethnoveterinary studies and selected naturally by goats in the cerrado (Brazilian savanna), were tested in vitro against Haemonchus contortus. Hydroacetonic (ACT) and hydroalcoholic (ETH) extracts were evaluated using an Egg Hatching Assay (EHA), a Larval Exsheathment Inhibition Assay (LEIA) and a Larval Development Assay (LDA). A second set of incubations was performed using polyvinylpolypyrrolidone (PVPP) to determine the influence of polyphenols on the anthelmintic effects of EHA and LEIA. Data from each extract were used to calculate inhibition concentrations (IC50). All tested extracts showed activity against at least one life stage of H. contortus. The use of PVPP revealed that the tannins are not the only extracts of secondary metabolites responsible for the anthelmintic effects. The results showed clear in vitro anthelmintic activities against H. contortus at different stages and indicated the potential use of these species as a promising alternative approach to control helminthic infections of small ruminants.

Anatomical differentiation and metabolomic profiling: a tool in the diagnostic characterization of some medicinal Plantago species

Abstract There is a large list of plants used by the population as medicine, but in some case the choice of the right plant becomes a real drawback in phytotherapy, since it is often difficult to differentiate morphologically between the active and inactive species. Plantago species are widely used throughout the world as analgesic, anti-inflammatory, expectorant, digestive and wound healing. Nonetheless, Plantago spp. share very strong morphological similarities, which hinders their correct botanical identification and, in addition, they are equivocally marketed by the same common name “Plantain”. Therefore, the establishment of a reliable approach to distinguish unambiguously closely related species arises as an important task in the development of herbal medicines. In this work, we report a method that combines anatomical leaf features and chemical composition of four Plantago species to generate a multivariate model, which allows the differentiation of these species. Descriptive leaf anatomy was converted into a binary matrix to create a qualitative/quantitative non-metric multidimensional scaling (nmMDS) based on Jaccard index. The main results show that P. lanceolata L. is the most distinct species, the only one that owns mesophyll isolateral, colateral vascular bundle and a glandular trichome with spindle cells. Plantago major L. also has a unique glandular trichome, with enlarged basal cell and collar cell. This statistical-based anatomical approach is suitable to solve similar drawbacks in plant medicines of any other plant-cases. In addition, it was generated a nmMDS to chemical markers by mass spectrometry (FIA–ESI–IT–MS), to define how similar the species are regarding their chemical composition. Plantago major showed all compounds evaluated and is the only species to have the compounds hellicoside (m/z 655) and lavandulifolioside (m/z 755). The conversion of anatomical features into statistical data with the chemical composition emerges as a useful approach toward the quantitative differentiation of morphologically close related specimens.

Mutagenicity and chemopreventive activities of Astronium species assessed by Ames test

In the neotropical savannah, Astronium species are used in popular medicine to treat allergies, inflammation, diarrhea and ulcers. Given that natural products are promising starting points for the discovery of novel potentially therapeutic agents, the aim of the present study was to investigate the mutagenic and antimutagenic activities of hydroalcoholic extracts of Astronium spp. The mutagenicity was determined by the Ames test on Salmonella typhimurium strains TA98, TA97a, TA100 and TA102. The antimutagenicity was tested against the direct-acting and indirect-acting mutagens. The results showed that none of the extracts induce any increase in the number of revertants, demonstrating the absence of mutagenic activity. On the other hand, the results on the antimutagenic potential showed a moderate inhibitory effect against NPD and a strong protective effect against B[a]P and AFB1. This study highlights the importance of screening species of Astronium for new medicinal compounds. The promising results obtained open up new avenues for further study and provide a better understanding the mechanisms by which these species act in protecting DNA from damage. However, further pharmacological and toxicological investigations of crude extracts of Astronium spp., as well as of its secondary metabolites, are necessary to determine the mechanism(s) of action to guarantee their safer and more effective application to human health.

In vitro anthelmintic effects of Spigelia anthelmia protein fractions against Haemonchus contortus

Gastrointestinal nematodes are a significant concern for animal health and well-being, and anthelmintic treatment is mainly performed through the use of chemical products. However, bioactive compounds produced by plants have shown promise for development as novel anthelmintics. The aim of this study is to assess the anthelmintic activity of protein fractions from Spigelia anthelmia on the gastrointestinal nematode Haemonchus contortus. Plant parts were separated into leaves, stems and roots, washed with distilled water, freeze-dried and ground into a fine powder. Protein extraction was performed with sodium phosphate buffer (75 mM, pH 7.0). The extract was fractionated using ammonium sulfate (0–90%) and extensively dialyzed. The resulting fractions were named LPF (leaf protein fraction), SPF (stem protein fraction) and RPF (root protein fraction), and the protein contents and activities of the fractions were analyzed. H. contortus egg hatching (EHA), larval exsheathment inhibition (LEIA) and larval migration inhibition (LMIA) assays were performed. Proteomic analysis was conducted, and high-performance liquid chromatography (HPLC) chromatographic profiles of the fractions were established to identify proteins and possible secondary metabolites. S. anthelmia fractions inhibited H. contortus egg hatching, with LPF having the most potent effects (EC50 0.17 mg mL-1). During LEIA, SPF presented greater efficiency than the other fractions (EC50 0.25 mg mL-1). According to LMIA, the fractions from roots, stems and leaves also reduced the number of larvae, with EC50 values of 0.11, 0.14 and 0.21 mg mL-1, respectively. Protein analysis indicated the presence of plant defense proteins in the S. anthelmia fractions, including protease, protease inhibitor, chitinase and others. Conversely, secondary metabolites were absent in the S. anthemia fractions. These results suggest that S. anthelmia proteins are promising for the control of the gastrointestinal nematode H. contortus.