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1.
Chem Biodivers ; 14(1)2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-27546206

RESUMO

This article reports on the in vitro activity of the hydroalcoholic extract of Pfaffia glomerata roots, its hydrolyzed fractions, and pfaffic acid against Trypanosoma cruzi. The hydroalcoholic extract obtained from dried, milled P. glomerata roots was submitted to acid hydrolysis followed by partition with CHCl3 . The concentrated CHCl3 fraction was suspended in MeOH/H2 O and partitioned with hexane (F1), CHCl3 (F2), and AcOEt (F3), in this sequence. The trypanocidal activity of the hydrolyzed extract and its fractions was evaluated in vitro. The hydroalcoholic extract displayed low activity, but fraction F1 was active against trypomastigotes of the Y strain of T. cruzi, with IC50 = 47.89 µg/ml. The steroids campesterol (7.7%), stigmasterol (18.7%), ß-sitosterol (16.8%), Δ7 -stigmastenol (4.6%), and Δ7 -spinasterol (7.5%) were the major constituents of F1, along with fatty acid esters (7.6%) and eight aliphatic hydrocarbons (30.1%). Fractions F2 and F3 exhibited moderate activity, and pfaffic acid, one of the main chemical constituents of these fractions, displayed IC50 = 44.78 µm (21.06 µg/ml). On the other hand, the hydroalcoholic extract of P. glomerata roots, which is rich in pfaffosides, was inactive. Therefore, the main aglycone of pfaffosides, pfaffic acid, is much more active against trypomastigotes of the Y strain of T. cruzi than its corresponding glycosides and should be further investigated.


Assuntos
Amaranthaceae/química , Extratos Vegetais/farmacologia , Triterpenos/farmacologia , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Fracionamento Químico , Hidrólise , Extratos Vegetais/isolamento & purificação , Raízes de Plantas/química , Triterpenos/isolamento & purificação , Tripanossomicidas/isolamento & purificação
2.
Nat Prod Commun ; 11(4): 493-6, 2016 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-27396202

RESUMO

The antimicrobial activity and possible synergistic effects of extracts and compounds isolated from Usnea steineri were evaluated against four resistant bacterial species. A phytochemical study of the acetone extract of U. steineri resulted in the isolation and characterization of difractaic acid and (+)-usnic acid as the main compounds. The acetone extract showed strong activity (less than 10 µg/mL) against resistant strains of Staphylococcus epidermidis and Enterococcus faecalis, and (+)-usnic acid exhibited strong activity against S. epidermidis (MIC 3.12 µg/mL), S. aureus and S. haemnolyticus (MIC 12.5 µg/mL). Combinations of penicillin and tetracycline with (+)-usnic acid did not show any synergistic antimicrobial effects. Difractaic acid was inactive. Our results showed that the acetone extract of U. steineri possesses significant in vitro antimicrobial activity, which is likely related to the presence of (+)-usnic acid.


Assuntos
Antibacterianos/análise , Benzofuranos/isolamento & purificação , Depsídeos/isolamento & purificação , Usnea/química , Depsídeos/química , Farmacorresistência Bacteriana Múltipla , Testes de Sensibilidade Microbiana , Usnea/metabolismo
3.
Pharm Biol ; 51(9): 1087-90, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23738822

RESUMO

CONTEXT: Despite several pharmacological applications of Rosmarinus officinalis L. (Lamiaceae), studies on its analgesic and anti-inflammatory properties have been scarce. OBJECTIVE: The aim of this work was to use in vivo models to evaluate the analgesic and anti-inflammatory activities of the aqueous extracts obtained from leaves (AEL) and stems (AES) of Rosmarinus officinalis, as well as its isolated compound--rosmarinic acid (RA). We also prepared and assessed the acetyl ester derivative of RA. MATERIALS AND METHODS: The analgesic activity was evaluated using abdominal constriction and formalin tests. For the evaluation of the anti-inflammatory effects, carrageenin-induced paw edema in rats were used. The extracts were used at doses of 100, 200 and 400 mg kg⁻¹ compounds were tested at 10, 20 and 40 mg kg⁻¹. RESULTS: Orally administered AEL, AES and RA were not significantly active at any of the doses tested during the abdominal constriction test; the acetyl ester derivative of RA displayed significant analgesic activity. In the carrageenin-induced paw edema assay, the acetyl derivative of RA at all the tested doses produced significant anti-inflammatory effects and reduced the number of paw licks in the second phase of the formalin test. DISCUSSION AND CONCLUSION: The results suggest that the analgesic effects of the acetyl derivative of RA operate via a peripheral-mediated mechanism. The acetyl ester derivative of RA is potentially applicable as a new lead compound for the management of pain and inflammation.


Assuntos
Anti-Inflamatórios não Esteroides/uso terapêutico , Cinamatos/uso terapêutico , Depsídeos/uso terapêutico , Modelos Animais de Doenças , Neuralgia/prevenção & controle , Inflamação Neurogênica/prevenção & controle , Extratos Vegetais/uso terapêutico , Rosmarinus/química , Acetilação , Administração Oral , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Comportamento Animal/efeitos dos fármacos , Brasil , Cinamatos/administração & dosagem , Cinamatos/química , Cinamatos/isolamento & purificação , Depsídeos/administração & dosagem , Depsídeos/química , Depsídeos/isolamento & purificação , Relação Dose-Resposta a Droga , Etnofarmacologia , Masculino , Medicina Tradicional , Camundongos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Caules de Planta/química , Ratos , Ratos Wistar , Ácido Rosmarínico
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