RESUMO
The species Inga laurina is native to the Brazilian Cerrado. There are no studies about the chemical composition and biological activities of extracts of this endangered species. The ethanolic extract and its successive fractions are rich in phenolic compounds and presented good antifungal activities. HPLC/MS-MS/MS and H1/C13 analysis led to the identification of seventeen compounds, most of which are gallic acid derivatives, myricetin and quercetin glycosides. The ethyl acetate fraction (EAF) contained high levels of total phenolics, expressed in milligrams of gallic acid equivalents per gram of extract (475.3 ± 1.9 mg GAE gextract -1) and flavonoids expressed in milligrams of quercetin equivalents per gram of extract (359.3 ± 10.6 mg QE gextract -1). This fraction was active against fungi of the Candida genus. The EAF showed MIC value 11.7 µg mL-1 against C. glabrata and a selectivity index of 1.6 against Vero cells. The flavonol glycoside myricetin-3-O-rhamnoside was isolated for the first time from the Inga laurina. These results make I. laurina a promising plant as a source of pharmaceutical and biological active antifungal compounds.
Assuntos
Antifúngicos/farmacologia , Citotoxinas/farmacologia , Fabaceae/química , Extratos Vegetais/farmacologia , Antifúngicos/química , Antifúngicos/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Citotoxinas/química , Citotoxinas/isolamento & purificação , Flavonoides/química , Flavonoides/isolamento & purificação , Fenóis/química , Fenóis/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Proantocianidinas/química , Proantocianidinas/isolamento & purificação , Espectrometria de Massas em TandemRESUMO
Copaiba oleoresins are used in alternative medicine as anti-inflammatory, antitumoral, and antimicrobial treatments. (-)-Copalic acid (CA) is the major diterpene found in exudates from Copaifera species. We have examined the genotoxicity and the chemopreventive potential of Copaifera multijuga oleoresin (CM) and CA. Genotoxicity assessment was examined with the peripheral blood micronucleus test and the comet assay (male Swiss mouse hepatocytes). In the chemoprevention study, we evaluated the effects of CM and CA on the formation of 1,2-dimethylhydrazine (DMH)-induced aberrant crypt foci (ACF) in male Wistar rat colon. Neither agent caused a significant increase in micronucleus frequency relative to controls, but the highest CM dose tested (400mg/kg b.w.) caused DNA damage in the comet assay. Both agents significantly reduced the frequency of DMH-induced ACF. Both CM and CA suppressed ACF formation and may have a protective effect against colon carcinogenesis.
Assuntos
Anticarcinógenos/farmacologia , Dano ao DNA , Diterpenos/farmacologia , Fabaceae/química , Micronúcleos com Defeito Cromossômico/induzido quimicamente , Extratos Vegetais/farmacologia , Focos de Criptas Aberrantes/prevenção & controle , Animais , Anticarcinógenos/isolamento & purificação , Anticarcinógenos/toxicidade , Neoplasias do Colo/prevenção & controle , Ensaio Cometa , Diterpenos/isolamento & purificação , Diterpenos/toxicidade , Relação Dose-Resposta a Droga , Hepatócitos/efeitos dos fármacos , Hepatócitos/patologia , Masculino , Camundongos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Ratos WistarRESUMO
Solanum cernuum Vell is a Brazilian shrub or small tree, restricted to Southeast states of the country. The leaves are commercialized as "panacéia" and indicated for the treatment of urinary disorders, gonorrhea, scabies, skin diseases and as desobstruent, diuretic and antiarrhythmic. The hydroalcholic extract is active in the treatment of gastric ulcer. The aim of this study was to evaluate the genotoxic and antigenotoxic potential of S. cernuum hydroalcoholic extract (SC) in Swiss mice by micronucleus and comet assays. The animals were treated by gavage with the doses of 500, 1000 and 2000mg/kg body weight (b.w.). For antigenotoxicity assessment, the doses of 15, 30, 60, 120 and 240mg/kg b.w SC were administered simultaneously with the mutagen methyl methanesulfonate (MMS, 40mg/kg b.w., i.p.). The results showed that the SC was not genotoxic in both micronucleus and comet assays. On the other hand, the treatment with the lowest dose of SC (15mg/kg b.w.) plus MMS showed a statistically significant reduction in the frequency of micronuclei compared to treatment only with MMS. For the comet assay, significant reduction in extensions of DNA damage was observed in all treatments with SC combined with MMS in comparison with only MMS. The antigenotoxic activity observed for the SC may be due to the antioxidant potential of the compounds present in the extract such as guanidine alkaloids and flavonoids.
Assuntos
Cromossomos de Mamíferos/metabolismo , Dano ao DNA/genética , Genoma , Metanossulfonato de Metila/toxicidade , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Solanum/química , Animais , Cromatografia Líquida de Alta Pressão , Hepatócitos/efeitos dos fármacos , Hepatócitos/patologia , Masculino , Camundongos , Folhas de Planta/químicaRESUMO
In this work, we used the Minimum Inhibitory Concentration (MIC) technique to evaluate the antibacterial potential of the apitoxin produced by Apis mellifera bees against the causative agents of tooth decay. Apitoxin was assayed in natura and in the commercially available form. The antibacterial actions of the main components of this apitoxin, phospholipase A2, and melittin were also assessed, alone and in combination. The following bacteria were tested: Streptococcus salivarius, S. sobrinus, S. mutans, S. mitis, S. sanguinis, Lactobacillus casei, and Enterococcus faecalis. The MIC results obtained for the commercially available apitoxin and for the apitoxin in natura were close and lay between 20 and 40 µg / mL, which indicated good antibacterial activity. Melittin was the most active component in apitoxin; it displayed very promising MIC values, from 4 to 40 µg / mL. Phospholipase A2 presented MIC values higher than 400 µg / mL. Association of mellitin with phospholipase A2 yielded MIC values ranging between 6 and 80 µg / mL. Considering that tooth decay affects people's health, apitoxin and its component melittin have potential application against oral pathogens.
Assuntos
Antibacterianos/farmacologia , Venenos de Abelha/farmacologia , Enterococcus faecalis/efeitos dos fármacos , Lacticaseibacillus casei/efeitos dos fármacos , Streptococcus/efeitos dos fármacos , Animais , Venenos de Abelha/química , Venenos de Abelha/enzimologia , Meliteno/farmacologia , Testes de Sensibilidade Microbiana , Fosfolipases A2/farmacologiaRESUMO
The seasonal chemical composition of essential oils from Inga laurina was determined by GC/MS. In the stem bark's essential oil extracted during the dry season, the presence of terpenoids (30.05%) stood out, and phytol (9.76%) was the major compound identified. For the stem bark oil obtained during the rainy season, in addition to terpenoids (26.63%), a large amount of fatty acids (46.84%) were identified, in particular palmitic acid (25.40%). Regarding the leaves' essential oil obtained in the dry season, esters (42.35%) were the main components. The main ester present was (Z)-hex-3-enyl benzoate (10.15%) and the major compound of this oil was (Z)-hex-3-en-1-ol (14.23%). Terpenoids (33.84%), long-chain alkanes (27.04%) and fatty acids (21.72%) were the main components of the essential oil from leaves in the rainy season. Phytol (33.21%), nonacosane (21.95%) and palmitic acid (15.20%) were the major compounds identified. The antimicrobial activity against aerobic and anaerobic oral bacteria was evaluated by the microdilution broth method and cytotoxic activity was carried out with Vero cells. The essential oils from the rainy season showed a better inhibition of the bacterial growth with Minimal Inhibitory Concentrations (MIC) values of 25 or 50 µg·mL⻹ for aerobic bacteria, and high selectivity against bacteria was observed. The large amount of fatty acids in rainy season oils may be related to the better inhibitory effects observed.
Assuntos
Anti-Infecciosos/química , Citotoxinas/química , Fabaceae/química , Óleos Voláteis/química , Óleos de Plantas/química , Animais , Anti-Infecciosos/farmacologia , Bactérias Aeróbias/efeitos dos fármacos , Bactérias Aeróbias/crescimento & desenvolvimento , Bactérias Anaeróbias/efeitos dos fármacos , Bactérias Anaeróbias/crescimento & desenvolvimento , Sobrevivência Celular/efeitos dos fármacos , Chlorocebus aethiops , Citotoxinas/farmacologia , Ésteres , Ácidos Graxos/classificação , Ácidos Graxos/isolamento & purificação , Óleos Voláteis/farmacologia , Especificidade de Órgãos , Casca de Planta/química , Folhas de Planta/química , Óleos de Plantas/farmacologia , Estações do Ano , Terpenos/classificação , Terpenos/isolamento & purificação , Células VeroRESUMO
Baccharin (3-prenyl-4-(dihydrocinnamoyloxy)cinnamic acid) is an important chemical compound isolated from the aerial parts of Baccharis dracunculifolia DC (Asteraceae), a native plant of South America, and the most important plant source of Brazilian green propolis. The present study was designed to investigate the ability of baccharin to modulate the genotoxic effects induced by doxorubicin and methyl methanesulphonate in male Swiss mice using the micronucleus and comet assays, respectively. The different doses of baccharin [0.12, 0.24 and 0.48 mg/kg body-weight (b.w.)] were administered simultaneously to doxorubicin (micronucleus test; 15 mg/kg b.w.) and to methyl methanesulphonate (comet assay; 40 mg/kg b.w.). The results showed a significant decrease in the frequency of micronucleated polychromatic erythrocytes in animals treated with baccharin and doxorubicin compared to animals that received only doxorubicin. This reduction ranged from 39.8% to 50.7% in the micronucleus test. The extent of DNA damage in liver cells was significantly lower in animals treated with different concentrations of baccharin combined with methyl methanesulphonate in comparison with the damage observed for animals treated only with methyl methanesulphonate. These differences resulted in a significant reduction in the extent of DNA damage, which ranged from 47.8% to 60.6%.