Recebido em 13/7/10; aceito em 24/12/10; publicado na web em 15/4/11 CHEMICAL AND PHARMACOLOGICAL ASPECTS OF Byrsonima (Malpighiaceae). Species of the Byrsonima genus are widely distributed around the neotropical zone, being frequently used in folk medicine to treat gastrointestinal, respiratory and skin diseases. This article briefly reviews the ethnopharmacology, pharmacology and phytochemistry of the Byrsonima genus. Eighty three compounds isolated from different species are reported, most of them being flavonoids or triperpenes. The pharmacological studies carried out with the extracts from these plants emphasize on the antimicrobial activity, however other activities have also been investigated leading to promising results. The data presented in this work strongly supports the view that plants of Byrsonima genus have potential therapeutic action.Keywords: Malpighiaceae; Byrsonima; review. INTRODUÇÃOMalpighiaceae é uma família de árvores, arbustos, subarbustos e lianas com aproximadamente 71 gêneros e 1250 espécies, que se distribuem em florestas tropicais, subtropicais e savanas do Velho e Novo Mundo, onde estão localizadas 85% das espécies.1 Várias espé-árias espé-cies dessa família são utilizadas com fins medicinais pela população de países americanos, principalmente como moduladores do sistema nervoso central (gêneros Banisteriopsis, Diplopterys, Galphimia e Heteropteris) e afrodisíacos (gênero Heteropteris). 2Uma revisão acerca da constituição química dessa família registra como principais fitoconstituintes os alcaloides carbolínicos, bases indólicas simples, fenilpropanoides, flavonoides, triterpenoides e polissacarídeos em diferentes gêneros. Esse mesmo trabalho destaca o uso ritualístico-religioso de algumas espécies, que é registrado até os dias atuais, além o valor nutricional de espécies do gênero Malpighia, ricas em ácido ascórbico (vitamina C) em seus frutos, que são saborosos e bastante apreciados na culinária brasileira. Entretanto, o gênero mais extensivamente estudado tem sido o Byrsonima, um dos maiores da família Malpighiaceae, possuindo 150 espécies com distribuição marcadamente neotropical.4 O Brasil concentra cerca de 50% das espécies, que são encontradas principalmente nas regiões Norte, Nordeste e Central, podendo também ser encontradas na região Sudeste do país, em áreas de cerrado. No Brasil, essas espécies são conhecidas popularmente como "muricis", sendo diferenciadas pela cor de suas flores e frutos, ou pelo local de ocorrência. Desse modo, recebem nomes como murici da várzea, murici da mata, murici-amarelo, entre outros. 5A madeira das espécies arbóreas é leve, sendo utilizada na construção civil para a fabricação de caibros e vigas. Algumas delas já foram bastante empregadas em curtumes e para tingir tecidos, devido à grande quantidade de taninos e matéria tintorial nas cascas. Com flores vistosas, frutos que atraem aves e rápido crescimento, tais espécies têm grande potencial como plantas ornamentais e também são úteis na recuperação de áreas degradadas. 6 Os frutos de B. cras...

Background. Byrsonima is a promising neotropical genus, rich in flavonoids and triterpenes, with several proven pharmacological properties. Nevertheless, Byrsonima duckeana W. R. Anderson is an Amazonian species almost not studied. Objective. To assess the antioxidant, anti-inflammatory, and analgesic activities of Byrsonima duckeana leaves. Materials and Methods. We analyzed an ethanol extract and its fractions for polyphenol content and UHPLC-MS/MS, phosphomolybdenum, DPPH, TBARS antioxidant tests, formalin-induced pain, carrageenan-induced peritonitis, acetic acid-induced abdominal writhings, and hot plate assays. Results. All the samples showed high polyphenol content and antioxidant capacity in the phosphomolybdenum, DPPH, and TBARS tests. We identified ethyl gallate, quinic acid, gallic acid, catechin, epicatechin, quercetrin, and quercetin in the samples. B. duckeana was able to reduce leukocyte migration in the carrageenan-induced peritonitis by 43% and the licking time in the formalin test by 57%. In the acetic acid-induced writhing test, the chloroform (FCL) and ethyl acetate (FEA) fractions were the most active samples. FEA was selected for the hot plate test, where all the dosages tested (5, 50, and 200 mg·kg−1) showed significant analgesic activity. Conclusion. B. duckeana has interesting analgesic and antioxidant activities, due to its high phenolic content, especially phenolic acids.

BJP 122 1-5 Revista Brasileira de Farmacognosia xxx (2015) xxx-xxx w w w . s b f g n o s i a . o r g . b r / r e v i s t a a b s t r a c t In Amazonas State (Brazil), Justicia acuminatissima (Miq.) Bremek., Acanthaceae, leaf teas are used in folk medicine to treat several inflammatory illnesses. In order to validate this medicinal application, we analyzed the acute toxicity and antioxidant, antiedematogenic and antinociceptive potentials of an aqueous extract of this species, using culture cells and animal models. The aqueous extract did not cause toxic effects on human lymphocytes in high concentration (400 g/mL), neither on mice treated with high doses (5000 mg/kg) in an acute toxicity analysis by oral route, and also did not cause lesions in the gastric mucosa of animals treated with 300 mg/kg, which was the maximal dose used in the anti-inflammatory screening. The aqueous extract caused inhibition of inflammatory pain in formalin-induced paw licking test with all tested doses, 30, 100 and 300 mg/kg, and antiedematogenic activity at 100 and 300 mg/kg. Additionally, the aqueous extract presented statistically significant action on the release of nitric oxide by lipopolysaccharide-activated macrophages. These results and other previously observed preliminarily Q2 studies support the folk use of this species, and further investigation of its action mechanism by inhibition of COX-2 or related metabolite would be interesting.

Species of the Byrsonima genus are widely used in Brazil, especially for the treatment of gastrointestinal disorders. However, species from the Amazonian region are still poorly studied. Thus, we studied the antioxidant, antinociceptive, and anti-inflammatory activities of for Amazonian species, Byrsonima crispa, Byrsonima duckeana, Byrsonima garcibarrigae, and Byrsonima incarnata. Phenolic composition was determined by chemical and chromatographic methods. The aqueous extracts were evaluated in DPPH , ABTS , and superoxide (O ) tests, LPS-activated macrophage assay, and formalin test. All species contained a high phenolic and flavonoid content. We identified 15 phenolic compounds, including phenolic acids, hydroxycinnamic acids, flavonoids, and catechins. The extracts showed high antioxidant activity and were more active than quercetin at inhibiting nitric oxide release in the LPS-activated macrophage assay. B. duckeana and B. garcibarrigae showed higher in vivo antinociceptive and anti-inflammatory activities. B. garcibarrigae presented significant effect on the early phase of the formalin test, pointing to an antinociceptive mechanism distinct from traditional anti-inflammatory medicines. In conclusion, the pharmacological potential of these species is closely related to their flavonoid-rich chemical composition, which seems to act through antioxidant mechanisms. Copyright © 2017 John Wiley& Sons, Ltd.

According to our results, it was concluded that stem bark of Byrsonima japurensis has significant and safe anti-inflammatory activity, which is closely related with their potent antioxidant activity, supporting the folk medicinal use of this species.

Justicia acuminatissima (Miq.) Bremek., Acanthaceae, is a subshrub found in northern Brazil, where it is widely used by the population of this region as an antiinfl ammatory medicine. Despite this popular use, there is no pharmacognostical data to support the correct identifi cation of this species. We therefore performed a morphoanatomical, histochemical and phytochemical analysis of the leaves of this species, using well-known methods. The leaves are simple, exstipulate, green on the surfaces, and pubescent, with a lanceolate shape, crenate margin, pinnate venation and decussate phyllotaxy. The parenchyma is palisade and spongy, and its vascular system is bilateral. Glandular and non-glandular trichome and cystoliths were also detected. There are diacytic stomata on both the adaxial and abaxial surfaces of epidermis. Histochemical tests revealed the presence of phenolic compounds, amide and protein. Phytochemical tests showed the presence of coumarins, tannins, catechins, saponins and steroids.

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A novel anti-inflammatory hybrid 3-ibuprofenyl-copalic acid (3-IbuCA) was synthesized from 3-hydroxy-copalic acid isolated from Amazonian copaiba oil (Copaifera multijuga Hayne), and the anti-inflammatory ibuprofen. After full characterization, several assays to verify its anti-inflammatory effects were performed in vitro, in vivo and in silico (molecular docking). Induced fit docking was performed to observe the interactions with the enzymes cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). In vitro tests of cytotoxicity and tumor necrosis factor (TNF)-α inhibition, and in vivo tests of pleurisy, protein expression and gastrocytotoxicity were performed. Molecular docking studies with COX-1 and 2 showed binding free energies (ΔG) of −2.2 and −7.8 kcal mol −1 , respectively, while for mofezolac and indomethacin, the binding free energies ΔG presented values of −8.5 and −10.1 kcal mol −1 , which makes 3-IbuCA selective for COX-2 inhibition. This hybrid showed no toxicity against human macrophage at concentrations up to 2 µM, and inhibited TNF-α production in lipopolysaccharide (LPS)-stimulated macrophages. In the pleurisy assays, 3-IbuCA reduced the total leukocytes and mononuclear cells, which was followed by reduction of p-IKBα (phosphorylated nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor, alpha) protein expression. Compared with ibuprofen alone, the hybrid caused less gastric damage. Thus, the docking, together with in vitro and in vivo studies suggest that this novel hybrid has potential as a new anti-inflammatory agent.