RESUMO
OBJECTIVES: Dalbergia ecastaphyllum (L.) Taub. is a semi-prostrate species associated with estuaries, mangroves and dunes. This plant species has great ecological and economic importance, especially concerning apiculture pasture and Brazilian red propolis production. In this study, non-clinical toxicological evaluations of the hydroalcoholic extract of D. ecastaphyllum stems (DEHE), the resin production source, were conducted. In addition, the action of DEHE on genomic instability and colon carcinogenesis was investigated. METHODS AND RESULTS: The extract's chemical profile was analysed by HPLC, and medicarpin, vestitol and neovestitol were found as major compounds. DEHE showed an IC50 equivalent to 373.2 µg/ml and LC50 equal 24.4 mg/L, when evaluated using the XTT colorimetric test and the zebrafish acute toxicity assay, respectively. DEHE was neither genotoxic nor cytotoxic at the highest dose, 2000 mg/kg, by peripheral blood micronucleus test. The treatments DEHE (6 and 24 mg/kg) led to the reduction of micronuclei induced by doxorubicin (DXR) in mice. Furthermore, significantly higher serum levels of reduced glutathione were observed in animals treated with DEHE plus DXR, revealing an antioxidant effect. Treatments with DEHE (48 mg/kg) led to a significant reduction in pre-neoplastic lesions induced by the 1,2-dimethylhydrazine (DMH) carcinogen in the rat colon. Immunohistochemical analysis revealed significantly lower levels of expression of COX-2 (86%) and PCNA (83%) in the colon of rats treated with DEHE plus DMH, concerning those treated with the carcinogen. CONCLUSIONS: These results indicate the involvement of anti-inflammatory and antiproliferative pathways in the protective effect of DEHE.
Assuntos
Dalbergia , Própole , Animais , Camundongos , Ratos , Brasil , Carcinógenos , Quimioprevenção , Dalbergia/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Própole/química , Própole/farmacologia , Peixe-ZebraRESUMO
Red propolis is a substance produced by bees by mixing resins from plants with wax, oils, and other secretions to protect the hive against natural enemies. Dalbergia ecastaphyllum (L.) Taub. (Fabaceae) is the primary botanical source of the Brazilian red propolis, where bees Apis mellifera L. collect a reddish resin from the stems to produce propolis. This species occurs in coastal dune and mangrove ecosystems, where local beekeepers install their beehives for propolis production. The induction of propolis production was virtually unknown. Previous reports and field evidence suggested that the reddish resin available in D. ecastaphyllum stems was not produced spontaneously but induced by the presence of a parasitic insect that feeds on the plant's stems. Research in the apiaries of the beekeepers' association of Canavieiras, Bahia, Brazil, led to the capture of a jewel beetle of an unknown species of the genus Agrilus Curtis (Buprestidae). It was confirmed that this jewel beetle is a red propolis production inductor. The adult and immature of this new species, Agrilus propolis Migliore, Curletti, and Casari sp. nov. are here described and illustrated. Behavioral information on the biology and chemical ecology confirms that the reddish resin of D. ecastaphyllum is directly related to the beetle attack and only occurs when Agrilus propolis sp. nov. adults emerge from the plant stem. This information is very important for Brazilian propolis producers interested in expanding red propolis production, which can have favorable effects on the economy of mangrove communities, promoting income generation, creating new business opportunities, and helping to sustain local communities and families.
Assuntos
Besouros , Dalbergia , Própole , Animais , Brasil , Dalbergia/química , Ecossistema , Própole/química , Própole/farmacologiaRESUMO
Propolis is one of the most widely used products in traditional medicine. One of the most prominent types of Brazilian propolis is the red one, whose primary botanical source is Dalbergia ecastaphyllum (L.) Taub. Despite the potential of Brazilian red propolis for developing new products with pharmacological activity, few studies guarantee safety in its use. The objective of this study was the evaluation of the possible toxic effects of Brazilian red propolis and D. ecastaphyllum, as well as the cytotoxicity assessment of the main compounds of red propolis on tumoral cell lines. Hydroalcoholic extracts of the Brazilian red propolis (BRPE) and D. ecastaphyllum stems (DSE) and leaves (DLE) were prepared and chromatographed for isolation of the major compounds. RP-HPLC-DAD was used to quantify the major compounds in the obtained extracts. The XTT assay was used to evaluate the cytotoxic activity of the extracts in the human fibroblast cell line (GM07492A). The results revealed IC50 values of 102.7, 143.4, and 253.1 µg/mL for BRPE, DSE, and DLE, respectively. The extracts were also evaluated for their genotoxic potential in the micronucleus assay in Chinese hamster lung fibroblasts cells (V79), showing the absence of genotoxicity. The BRPE was investigated for its potential in vivo toxicity in the zebrafish model. Concentrations of 0.8-6.3 mg/L were safe for the animals, with a LC50 of 9.37 mg/L. Of the 11 compounds isolated from BRPE, medicarpin showed a selective cytotoxic effect against the HeLa cell line. These are the initial steps to determine the toxicological potential of Brazilian red propolis.
Assuntos
Dalbergia/química , Extratos Vegetais/farmacologia , Própole/farmacologia , Animais , Brasil , Células Cultivadas , Relação Dose-Resposta a Droga , Humanos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Própole/química , Própole/isolamento & purificação , Peixe-ZebraRESUMO
The Brazilian red propolis (BRP) constitutes an important commercial asset for northeast Brazilian beekeepers. The role of Dalbergia ecastaphyllum (L.) Taub. (Fabaceae) as the main botanical source of this propolis has been previously confirmed. However, in addition to isoflavonoids and other phenolics, which are present in the resin of D. ecastaphyllum, samples of BRP are reported to contain substantial amounts of polyprenylated benzophenones, whose botanical source was unknown. Therefore, field surveys, phytochemical and chromatographic analyses were undertaken to confirm the botanical sources of the red propolis produced in apiaries located in Canavieiras, Bahia, Brazil. The results confirmed D. ecastaphyllum as the botanical source of liquiritigenin (1), isoliquiritigenin (2), formononetin (3), vestitol (4), neovestitol (5), medicarpin (6), and 7-O-neovestitol (7), while Symphonia globulifera L.f. (Clusiaceae) is herein reported for the first time as the botanical source of polyprenylated benzophenones, mainly guttiferone E (8) and oblongifolin B (9), as well as the triterpenoids ß-amyrin (10) and glutinol (11). The chemotaxonomic and economic significance of the occurrence of polyprenylated benzophenones in red propolis is discussed.
Assuntos
Clusiaceae/química , Dalbergia/química , Isoflavonas/química , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/química , Benzofenonas/análise , Benzofenonas/química , Brasil , Chalconas/análise , Cromatografia Líquida de Alta Pressão , Desenho de Fármacos , Flavanonas/análise , Flavonoides/análise , Isoflavonas/análise , Espectroscopia de Ressonância Magnética , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/análise , Extratos Vegetais/análise , Pterocarpanos/análise , Terpenos/análise , Triterpenos/análiseRESUMO
The aim of this study was to investigate the antibacterial activity of red propolis and resin and their association with standard antibiotics to evaluate possible differences of activity. We also submitted red propolis and the resin to a HPLC analysis to confirm the botanical origin. The extracts were tested against P. aeruginosa and S. aureus alone and in association with gentamicin and imipenem. The HPLC analysis identified seven compounds with six of them present in both substances. The lowest MIC values obtained in this study were observed against S. aureus. In general, MIC values showed to be lower for red propolis against all species tested in comparison to resin. Despite the synergistic behavior to be similar for both substances, we observed that inhibitory concentrations of drugs were lower when associated with red propolis in comparison to resin.
Assuntos
Antibacterianos/farmacologia , Dalbergia/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Própole/farmacologia , Resinas Vegetais/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Brasil , Cromatografia Líquida de Alta Pressão , Avaliação Pré-Clínica de Medicamentos , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Própole/química , Própole/isolamento & purificação , Resinas Vegetais/química , Resinas Vegetais/isolamento & purificação , Staphylococcus aureus/efeitos dos fármacosRESUMO
For the first time, the anti-hemolytic activity and the enzyme inhibitory activities of Dalbergia ecastaphyllum leaves extracts were tested against α-amylase, α-glucosidase, lipase, acetylcholinesterase, butyrylcholinesterase, tyrosinase and hyaluronidase. The phenolic profile of the obtained extracts was also investigated by high-performance liquid chromatography with photodiode array detection (HPLC-PAD). The extracts showed inhibitory activity against all enzymes evaluated, with the highest inhibitory activity reported for the enzyme hyaluronidase (28.28 ± 2.43 to 72.19 ± 1.40 μg mL-1). The obtained extracts also demonstrate anti-hemolytic activity (52.22 ± 1.62 to 71.17 ± 1.82%). Among the phenolic compounds identified, protocatechuic, vanillic and β-resorcylic acids were the most abundant (1.13 ± 0.06 to 2.53 ± 0.06, 0.90 ± 0.06 to 2.19 ± 0.06 and 1.03 ± 1.62 to 22.11 ± 1.62 mg L-1, respectively). In the statistical analysis, a significant correlation was found between the flavonoids content and all enzymes inhibitory activities. The present study showed that D. ecastaphyllum leaves extracts may have the potential to be used in the therapeutic treatment of several diseases such as Alzheimer, Parkinson, type 2 diabetes mellitus, hyperglycemia, and pigmentation, as well as those associated with oxidative stress.
Assuntos
Dalbergia/química , Doenças Neurodegenerativas/metabolismo , Síndrome Metabólica , Estresse Oxidativo , Técnicas In VitroRESUMO
Dalbergia ecastaphyllum is a native Brazil plant with importance for beekeeping, and widely used in folk medicine. For the first time, the extracts of this plant were assessed for the presence of hydrophilic and lipophilic antioxidants, as well as inhibition of tyrosinase, free radicals scavenging and sunscreen protection. The antioxidant activity was evaluated by free radical scavenging (DPPH) and ß-carotene bleaching assay. The tyrosinase inhibitory activity was evaluated and calculated the EC50. The photoprotective activity was measured using different concentrations of D. ecastaphyllum extracts. The Sun Protection Factor (SPF) of the samples was higher than 6, and the sample from Ilhéus showed the most pronounced photoprotective effect. Sample from Canavieiras presented the highest antioxidant activity by free radical scavenging DPPH and ß-carotene bleaching method, with 92.41% and 48.34%, respectively. All samples inhibited the tyrosinase, especially the sample from Prado that was most effective (124.62 µg.mL-1). Significant negative correlation was found between flavonoid contents and inhibition of tyrosinase. The overall results provide relevant information about the Dalbergia ecastaphyllum species, indicating as potential material to cosmetic and pharmaceutical industry.
Assuntos
Antioxidantes , Dalbergia/química , Inibidores Enzimáticos , Monofenol Mono-Oxigenase/antagonistas & inibidores , Extratos Vegetais , Folhas de Planta/química , Protetores Solares , Antioxidantes/química , Antioxidantes/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Humanos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Protetores Solares/química , Protetores Solares/farmacologiaRESUMO
The treatment for leishmaniasis and Chagas disease can be hard and painful, such that many patients give up on the treatment. In order to find an alternative path for the treatment of these diseases, researchers are using natural products to fight these parasites. The aim of this study was to evaluate the antiprotozoan and cytotoxic activities of red propolis samples collected from different Brazilian states and seasons whilst searching for possible activity differences. We also compared the red propolis results with the ones obtained for the plant resin extract collected from Dalbergia ecastaphyllum trees. The hydroethanolic red propolis extracts from Pernambuco and Alagoas, and the D. ecastaphyllum resin were evaluated regarding their antileishmanial, antitrypanosomal and cytotoxic activity. All extracts showed antiprotozoan and cytotoxic activity. RP-PER showed to be more cytotoxic against protozoan parasites and fibroblast cells. All propolis extracts showed a higher cytotoxic activity when compared to resin extracts. The propolis sample collected in Pernambuco during the rainy season killed the parasites with lower concentrations than the sample collected in the dry season. The IC50 observed against the parasites could be used without high fibroblast cell damage.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Dalbergia/química , Leishmania/efeitos dos fármacos , Extratos Vegetais/farmacologia , Própole , Tripanossomicidas/farmacologia , Animais , Brasil , Linhagem Celular , Humanos , Concentração Inibidora 50RESUMO
The aim of this study is to investigate the biopotency of methanolic extracts of Vitex mollis, Psidium guajava, Dalbergia retusa, and Crescential alata leaves against various staphylococcal strains isolated from cattle and rabbits. Methicillin-resistant S. aureus strains were isolated from cattle, while other strains were isolated from rabbits using standard methodology. The total phytochemical phenolic and saponins contents were obtained being the main groups of the antinutritional factors. The antimicrobial activity of the extracts against the standard culture of S. aureus (control) and S. aureus isolated from cattle and rabbits were investigated comparatively relative to that of oxacillin. It was found that both the control S. aureus and the isolated S. aureus are susceptible to all the four plant extracts, and sensitive to oxacillin. Of all the S. aureus including the control, MRSA2 is the most susceptible to all the extracts at 1000 µg/mL, except that of V. mollis where it is the least susceptible. Among all the plant extracts, P. guajava is the most active against MRSA2 and SOSA2. Therefore, the isolates from cattle (MRSA1 and MRSA2) are more susceptible to all the plant extracts than the isolates from rabbits. Among all the rabbit isolates, CoNS3 is the least susceptible to the extracts. Since all the plant extracts exhibit remarkable inhibitory activities against all the S. aureus strains, they are promising towards the production of therapeutic drugs.
Assuntos
Antibacterianos/farmacologia , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Staphylococcus aureus Resistente à Meticilina/isolamento & purificação , Extratos Vegetais/farmacologia , Staphylococcus/efeitos dos fármacos , Animais , Bignoniaceae/química , Bovinos/microbiologia , Dalbergia/química , Hidroxibenzoatos/análise , México , Testes de Sensibilidade Microbiana , Oxacilina/farmacologia , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Folhas de Planta/química , Psidium/química , Coelhos/microbiologia , Saponinas/análise , Staphylococcus aureus/efeitos dos fármacos , Vitex/químicaRESUMO
International trade in Brazilian rosewood, Dalbergia nigra (Vell.) Allemão ex Benth., is regulated by the Convention on International Trade in Endangered Species of Wild Fauna and Flora (CITES). One problem in enforcing these regulations is the difficulty in distinguishing the wood of D. nigra from that of a closely-related but unregulated species, Dalbergia spruceana Benth. Using LC-MS to analyse methanol extracts of xylaria specimens, we identified a chemical marker for D. nigra heartwood, and determined its structure as the neoflavonoid 6-hydroxy-7-methoxy-4-(4-methoxyphenyl)-2H-1-benzopyran-2-one (4'-O-methylmelanettin; dalnigrin), using spectroscopic techniques. Dalnigrin was present in all nine available heartwood specimens of D. nigra, but it was not detected in extracts of 59 other heartwood samples representing 15 species of Dalbergia, including D. spruceana. Five other phenolic compounds were also isolated from D. nigra heartwood and similarly identified as the neoflavonoids 3'-hydroxymelanettin, melanettin, melannein and dalbergin, and the isoflavone caviunin. In extracts of D. spruceana heartwood, pseudobaptigenin was identified by LC-MS to be a major phenolic component that was not detected in wood extracts of D. nigra. We conclude that chemical analysis, in combination with anatomical investigation, can provide persuasive evidence to support the positive identification of untreated heartwood of D. nigra.