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1.
Chem Biodivers ; : e202400686, 2024 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-38923804

RESUMO

Pereskia aculeata has been widely investigated due to its anti-inflammatory potential. Among the metabolites found in this species are the phytosterols beta-sitosterol (ß-SIT) and stigmasterol (STIG). The objective of the study was to evaluate the anti-inflammatory and toxicity activities of the hexane partition of P. aculeata (PHEX), as well as ß-SIT and STIG. PHEX was prepared and the phytosterols were quantified. In terms of toxicity against L929 fibroblast cells, PHEX showed toxicity up to 200 µg/mL; STIG and ß-SIT showed toxicity up to 25 µg/mL. PHEX inhibited 66% of nitric oxide radicals, while STIG and ß-SIT inhibited 33.73% and 34.94%, respectively. In an anti-inflammatory test against Zophobas morio larvae, all samples significantly reduced hemocyte levels. Additionally, the LD50 values were calculated: 229.6 mg/kg for PHEX, 101.5 mg/kg for STIG, and 103.8 mg/kg for ß-SIT. In conclusion, the study indicates that the phytosterols present in PHEX may contribute to its anti-inflammatory activity.

2.
J Dairy Res ; 91(1): 96-98, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38706325

RESUMO

We tested the hypothesis that milk proteins, through microencapsulation, guarantee protection against bioactive substances in coffee silverskin extracts. Therefore, the aim of this study was to carry out technological, nutritional and physicochemical characterisation of a coffee silverskin extract microencapsulated using instant skim milk powder and whey protein concentrate as wall materials. The aqueous extract of coffee silverskin was spray-dried using 10% (w/v) skim milk powder and whey protein concentrate. The samples were characterised by determining the water content, water activity, particle size distribution, colour analysis and total phenolic compound content as well as antioxidant activity using 2,2-diphenyl-radical 1-picrylhydrazyl scavenging methods, nitric oxide radical inhibition and morphological analysis. The product showed water activity within a range that ensured greater stability, and the reduced degradation of the dried coffee silverskin extract with whey protein concentrate resulted in better rehydration ability. The luminosity parameter was higher and the browning index was lower for the encapsulated samples than for the pure coffee silverskin extract. The phenolic compound content (29.23 ± 8.39 and 34.00 ± 8.38 mg gallic acid equivalents/g for the coffee silverskin extract using skimmed milk powder and whey protein concentrate, respectively) and the antioxidant activity of the new product confirmed its potential as a natural source of antioxidant phenolic compounds. We conclude that the dairy matrices associated with spray drying preserved the bioactive and antioxidant activities of coffee silverskin extracts.


Assuntos
Antioxidantes , Leite , Secagem por Atomização , Proteínas do Soro do Leite , Proteínas do Soro do Leite/química , Animais , Leite/química , Extratos Vegetais/química , Café/química , Manipulação de Alimentos/métodos , Proteínas do Leite/análise , Proteínas do Leite/química , Fenóis/análise , Tamanho da Partícula , Pós , Composição de Medicamentos/métodos
3.
An Acad Bras Cienc ; 93(suppl 4): e20210457, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34852065

RESUMO

Syzygium malaccense is popularly used to treat inflammation and pain-related ailments. The species was assessed regarding its antioxidant, antiglycant, anti-inflammatory, including anti-neuroinflammatory, and antinociceptive activities. Different models were employed to measure S. malaccense extract (ESM) antioxidant activity. The antiglycant activity was determined using the glucose-induced protein glycation model. LPS-induced neuroinflammation on murine BV-2 microglial cell line was used for anti-neuroinflammatory activity evaluation. The croton oil-induced ear edema test was accomplished to evaluate the in vivo anti-inflammatory activity. Acetic acid-induced writhing together with formalin-induced paw licking assays were performed to evaluate the antinociceptive potential. Finally, the chemical characterization was accomplished by a UHPLC-MS analysis. ESM presented relevant antioxidant and antiglycant activity. NO production by BV-2 cells was reduced, indicating the relevant neuroprotective activity. ESM significantly decreased the mice ear edema induced by croton oil and the nociceptive stimulus induced by acetic acid and formalin by central and peripheral mechanisms. The flavonoids myricitrin, myricetin and quercetin were identified and, as far as we know, the alkaloid reserpine was reported in the species for the first time. The antioxidant and antiglycant potential of ESM, may be related to the in vivo anti-inflammatory and antinociceptive effects, and to the in vitro neuroinflammation inhibition.


Assuntos
Antioxidantes , Syzygium , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Edema/induzido quimicamente , Edema/tratamento farmacológico , Camundongos , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico
4.
Microb Pathog ; 123: 385-392, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30053603

RESUMO

Vernonia condensata Baker is traditionally used to treat several inflammatory and infectious processes. So, this study evaluated the antibiotic, synergistic and antibiofilm effects, and the mode of action of ethyl acetate fraction from V. condensata leaves (Vc-EAF) against Staphylococcus aureus. Five S. aureus ATCC® and five methicillin-resistant S. aureus (MRSA) routine strains were used to determine Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration. The combinatory effect was evaluated by checkerboard and time kill methods; the mode of action through the bacterial cell viability and leakage of compounds absorbing at 280 nm; and the antibiofilm action by quantifying the percentage of adhesion inhibition. Vc-EAF was active against S. aureus (ATCC® 6538™), (ATCC® 25923™), (ATCC® 29213™), (ATCC® 33591™), (ATCC® 33592™), MRSA 1485279, 1605677, 1664534, 1688441 and 1830466, with MIC of 625 µg/mL for ATCC®, and 1250, 1250, >2500, 2500 and 2500 µg/mL for MRSA, in this order, with bacteriostatic effect for both ATCC® and MRSA strains. Vc-EAF plus ampicillin revealed a total synergic effect on MRSA 1485279, and Vc-EAF combined with chloramphenicol, a partial synergic action against S. aureus (ATCC® 29213™) and (ATCC® 25923™). The time kill data agreed with checkerboard results, and the treated cells number was reduced with release of bacterial content. An expressive bacterial adhesion inhibition for S. aureus (ATCC® 25923™) and MRSA 1485279 was detected. These results showed that V. condensata is a promising natural source of active substances against S. aureus, including multiresistant strains, interfering with their antibacterial growth and hampering their adhesion to surfaces.


Assuntos
Antibacterianos/farmacologia , Biofilmes/efeitos dos fármacos , Extratos Vegetais/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Vernonia/química , Ampicilina/farmacologia , Aderência Bacteriana/efeitos dos fármacos , Membrana Celular/efeitos dos fármacos , Cloranfenicol/farmacologia , Combinação de Medicamentos , Sinergismo Farmacológico , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Viabilidade Microbiana/efeitos dos fármacos , Folhas de Planta/química
5.
Bioorg Med Chem ; 26(17): 4898-4906, 2018 09 15.
Artigo em Inglês | MEDLINE | ID: mdl-30193941

RESUMO

Resveratrol is a natural polyphenol found mainly on red grapes and in red wine, pointed as an important anti-inflammatory/immunomodulatory molecule. However, its bioavailability problems have limited its use encouraging the search for new alternatives agents. Thus, in this study, we synthetize 12 resveratrol analogues (6 imines, 1 thioimine and 5 hydrazones) and investigated its cytotoxicity, antioxidant activity and in vitro anti-inflammatory/immunomodulatory properties. The most promising compounds were also evaluated in vivo. The results showed that imines presented less cytotoxicity, were more effective than resveratrol on DPPH scavenger and exhibited an anti-inflammatory profile. Among them, the imines with a radical in the para position, on the ring B, not engaged in an intramolecular hydrogen-interaction, showed more prominent anti-inflammatory activity modulating, in vivo, the edema formation, the inflammatory infiltration and cytokine levels. An immunomodulatory activity also was observed in these molecules. Thus, our results suggest that imines with these characteristics presents potential to control inflammatory disorders.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Iminas/química , Resveratrol/análogos & derivados , Adjuvantes Imunológicos/farmacologia , Animais , Anti-Inflamatórios/farmacocinética , Antioxidantes/farmacologia , Disponibilidade Biológica , Compostos de Bifenilo/metabolismo , Proliferação de Células/efeitos dos fármacos , Citocinas/antagonistas & inibidores , Citocinas/biossíntese , Regulação para Baixo/efeitos dos fármacos , Inflamação/prevenção & controle , Mediadores da Inflamação/antagonistas & inibidores , Mediadores da Inflamação/metabolismo , Linfócitos/citologia , Linfócitos/efeitos dos fármacos , Complexo Principal de Histocompatibilidade/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos C57BL , Peroxidase/biossíntese , Picratos/metabolismo , Células RAW 264.7
6.
An Acad Bras Cienc ; 89(3 Suppl): 2053-2073, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28813096

RESUMO

This study aimed to further investigate the cytotoxicity against tumor cell lines and several bacterial strains of Annona squamosa and its mode of action. Methanol extracts of A. squamosa leaves (ASL) and seeds (ASS) were used. ASL showed significant antibacterial activity against S. aureus, K. pneumoniae and E. faecalis with MIC values of 78, 78 and 39 µg/mL respectively. Moreover, ASL exhibited significant biofilm disruption, rapid time dependent kinetics of bacterial killing, increased membrane permeability and significantly reduced the cell numbers and viability. Regarding the cytotoxicity against tumor cell lines, ASS was more active against Jurkat and MCF-7 cells, with CI50 1.1 and 2.1 µg/mL, respectively. ASL showed promising activity against Jurkat and HL60, with CI50 4.2 and 6.4 µg/mL, respectively. Both extracts showed lower activity against VERO cells and reduced the clonogenic survival at higher concentrations (IC90) to MCF-7 and HCT-116 lineages. The alkaloids anonaine, asimilobine, corypalmine, liriodenine nornuciferine and reticuline were identified in extracts by UPLC-ESI-MS/MS analysis. This study reinforced that A. squamosa presents a remarkable phytomedicinal potential and revealed that its antimicrobial mechanism of action is related to bacterial membrane destabilization.


Assuntos
Annona/química , Antibacterianos/farmacologia , Enterococcus faecalis/efeitos dos fármacos , Klebsiella pneumoniae/efeitos dos fármacos , Extratos Vegetais/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Animais , Linhagem Celular Tumoral/efeitos dos fármacos , Membrana Celular/efeitos dos fármacos , Chlorocebus aethiops , Humanos , Testes de Sensibilidade Microbiana
7.
Int J Mol Sci ; 17(12)2016 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-27916942

RESUMO

Vernonia polyanthes Less. (Asteraceae), popularly known as "assa-peixe", is a plant species used in Brazilian traditional medicine for the treatment of cutaneous damage, cicatrization, inflammation, and rheumatism. Based on these ethnopharmacological findings, the current study evaluated the topical anti-inflammatory effects of the hexane (HEVP) and ethyl acetate (EAEVP) extracts from V. polyanthes leaves in experimental models of skin inflammation. Chemical characterization was carried out by HPLC-UV/DAD analysis. Anti-inflammatory activity was evaluated using Croton oil-, arachidonic acid (AA)-, phenol-, ethyl phenylpropiolate (EPP)-, and capsaicin-induced ear edema models in mice. Histopathological evaluation and measurements of myeloperoxidase (MPO) and N-acetyl-ß-d-glucosaminidase (NAG) enzymes were also performed. Rutin, luteolin, and apigenin were identified in EAEVP. Topically applied HEVP and EAEVP significantly (p < 0.05, p < 0.01 or p < 0.001) reduced edema induced by five different irritants at the doses tested (0.1, 0.5 and 1.0 mg/ear). Histopathological analysis revealed a reduction of edema, inflammatory cell infiltration, and vasodilation. In addition, the enzymes activity (MPO and NAG) in the ear tissues was reduced by the topical treatment of HEVP and EAEVP (p < 0.05, p < 0.01 or p < 0.001). The results suggest that V. polyanthes leaves are effective against cutaneous damage, which support its traditional use and open up new possibilities for the treatment of skin disorders.


Assuntos
Inflamação/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Pele/efeitos dos fármacos , Vernonia/química , Acetatos/química , Administração Tópica , Animais , Anti-Inflamatórios , Brasil , Hexanos/química , Humanos , Inflamação/patologia , Medicina Tradicional , Camundongos , Fitoterapia , Extratos Vegetais/química , Folhas de Planta/química , Pele/patologia
8.
Exp Parasitol ; 159: 143-50, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26424529

RESUMO

Leishmaniasis is a complex disease caused by protozoan parasite Leishmania and the treatment remains a serious problem since the available drugs exhibited high toxicity and side effects. Plant-derived natural products are promising leads for the development of novel chemotherapeutics. In this work the phytol-rich hexane fraction (PRF) from the leaves of Lacistema pubescens was obtained and identified by GC-MS analysis. When assayed for antileishmanial effects, PRF was active against promastigote and amastigote forms of Leishmania amazonensis (IC50 values of 44.0 and 25.8 µg/mL respectively). Furthermore, PRF did not show significant cytotoxicity on peritoneal macrophages being more destructive to the intracellular parasite than to mammalian cells. In addition, possible targets of PRF were investigated against L. amazonensis promastigotes. The results showed that PRF exerted its antipromastigote activity by marked depolarization of the mitochondrial membrane potential followed by the increase of ROS levels in L. amazonensis promastigotes. During these events, no rupture of the cell membrane integrity was observed. Our results indicated that PRF was effective and selective against L. amazonensis, and that this effect was mainly mediated by mitochondrial dysfunction associated to ROS production.


Assuntos
Leishmania mexicana/efeitos dos fármacos , Magnoliopsida/química , Fitol/farmacologia , Extratos Vegetais/farmacologia , Animais , Membrana Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Cromatografia Gasosa-Espectrometria de Massas , Concentração Inibidora 50 , Leishmania mexicana/metabolismo , Macrófagos Peritoneais/efeitos dos fármacos , Macrófagos Peritoneais/parasitologia , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos BALB C , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Folhas de Planta/química , Espécies Reativas de Oxigênio/metabolismo
9.
An Acad Bras Cienc ; 87(2): 733-42, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26062121

RESUMO

Leishmaniasis is a complex of diseases caused by Leishmania protozoa which treatment is restricted to a limited number of drugs that exhibit high toxicity, collateral effects and are often costly. There are a variety of tropical plants distributed in Brazil, and for many poor people the therapy for several diseases is based mainly on the use of traditional herbal remedies. In this work, the cytotoxic activity of 17 plant methanol extracts was evaluated on several Leishmania species and murine macrophages. Among them, the extract of Casearia sylvestris, Piptocarpha macropoda, Trembleya parviflora, Samanea tubulosa and Plectranthus neochilus showed a promissing leishmanicidal activity, exhibiting IC50 values below of 20 µg/mL against at least one species of Leishmania. Casearia sylvestris showed the most expressive activity against all promastigote forms of Leishmania species (IC50 values of 5.4 µg/mL, 5.0 µg/mL, 8.5 µg/mL and 7.7 µg/mL for L. amazonensis, L. braziliensis, L. chagasi and L. major, respectively), being more effective than the reference drug miltefosine. In spite of the cytotoxic effect on macrophages (CC50 value of 5.2 µg/mL), C. sylvestris exhibited a strong inhibition against intracellular amastigotes of L. braziliensis (IC50 value of 1.3 µg/mL). Further studies, including bio-guided fractionation will be conducted to identify the active compounds.


Assuntos
Antiprotozoários/farmacologia , Leishmania/efeitos dos fármacos , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Animais , Brasil , Casearia/química , Concentração Inibidora 50 , Leishmania/classificação , Camundongos , Plantas Medicinais/classificação
10.
An Acad Bras Cienc ; 87(1): 303-11, 2015 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-25714074

RESUMO

Manihot multifida (L.) Crantz (Euphorbiaceae) is widely used in popular medicine for the treatment of infected wounds. This study evaluated the in vitro antioxidant and antimicrobial potential of this species against strains of Gram-positive and Gram-negative bacteria and fungi, known to cause infections in humans. The extracts showed minimal inhibitory concentration (MIC) varying from 39 to 2500 µg/mL for antimicrobial activity. The methanolic extract of fruits, aqueous and hexane extracts of leaves showed a very strong activity against Candida albicans (ATCC 18804) with MIC of 39 µg/mL. Furthermore, the methanolic extract of M. multifida leaves exhibited DPPH (1,1-diphenyl-2-picrylhydrazyl) scavenging potential with inhibitory concentration (IC50) values of 46.9 µg/mL, followed by hexane extract of leaves with IC50 values of 59.2 µg/mL. The cytotoxic activity against brine shrimp was stronger for the methanolic extract of leaves (lethal concentration - LC50 of 15.6 µg/mL). These results suggest that M. multifida has interesting antimicrobial and antioxidant activities. Moreover, these results corroborate the popular use of this specie in treating fungal infections since it demonstrates significant activity against C. albicans.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Manihot/química , Extratos Vegetais/farmacologia , Animais , Artemia/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Folhas de Planta/química
11.
Pharm Biol ; 53(12): 1780-5, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26084799

RESUMO

CONTEXT: Pereskia aculeata Miller (Cactaceae) is a cactus distributed from south to northeast of Brazil, where its leaves are commonly used as a vegetable, in skin wound healing, and to treat inflammation. OBJECTIVES: The objective of this study was to perform the chemical characterization and to evaluate the antinociceptive activity of the hydromethanolic fraction obtained from the methanol extract of P. aculeata leaves. MATERIALS AND METHODS: Chemical characterization was performed by UPLC-MS analysis. The antinociceptive activity was evaluated by the acetic acid-induced writhing, formalin, and tail-flick tests in mice, administering the single oral doses of 100, 200, and 300 mg/kg 1 h before each test. RESULTS: Tryptamine, abrine, mescaline, hordenine, petunidin, di-tert-butylphenol isomers, and quercetin were identified. The antinociceptive activity was inversely proportional to the administered doses in the acetic acid test, as the dose of 100 mg/kg reduced by 78% the number of writhings, while the doses of 200 and 300 mg/kg reduced by 64% and 41%, respectively. In the formalin test, the dose of 300 mg/kg inhibited by 50% and 86% the licking paw time in the first and second phases, respectively, while the doses of 200 mg/kg (45% and 62%, respectively) and 100 mg/kg (15% and 48%, respectively) were less effective. The sample did not respond to the tail-flick test. Those results suggested a peripheral and central antinociception devoid of an opioid effect. CONCLUSION: Pereskia aculeata not only is a plant food with high nutritional value but also presents analgesic potential. It is the first time that this bioactivity is reported for this species.


Assuntos
Analgésicos/farmacologia , Cactaceae , Medição da Dor/efeitos dos fármacos , Extratos Vegetais/farmacologia , Verduras , Analgésicos/isolamento & purificação , Animais , Relação Dose-Resposta a Droga , Masculino , Camundongos , Medição da Dor/métodos , Extratos Vegetais/isolamento & purificação , Folhas de Planta
12.
Plant Foods Hum Nutr ; 69(3): 189-95, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24862084

RESUMO

The exploration of nature as a source of sustainable, novel bioactive substances continues to grow as natural products play a significant role in the search for new therapeutic and agricultural agents. In this context, plants of the genus Pereskia (Cactaceae) have been studied for their biological activities, and are evolving as an interesting subject in the search for new, bioactive compounds. These species are commonly used as human foodstuffs and in traditional medicine to treat a variety of diseases. This review focuses on the bioactivity and chemical composition of the genus Pereskia, and aims to stimulate further studies on the chemistry and biological potential of the genus.


Assuntos
Cactaceae/química , Extratos Vegetais/farmacologia , Analgésicos/química , Analgésicos/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Cactaceae/classificação , Diuréticos/química , Diuréticos/farmacologia , Humanos , Extratos Vegetais/química , Folhas de Planta/química , Especiarias/análise
13.
Phytother Res ; 27(6): 926-30, 2013 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-22933394

RESUMO

Cecropia pachystachya is widely used in the traditional medicine as anti-inflammatory, antitusive, expectorant, antiasthmatic and hypoglycemic. It is also commercially available to treat skin cancer. To validate some of the popular uses of this species, its methanol leaves extract (CPM) was tested for anti-inflammatory, antinociceptive and cytotoxic effects. The anti-inflammatory activity was evaluated by croton oil-induced ear edema test. When used orally, the anti-inflammatory effect of CPM at 300 mg/kg was similar to that of indomethacin with 53% inhibition of the ear edema. Also, results on topical treatment were similar to that of dexamethasone with 83% inhibition of the edema. To evaluate the antinociceptive activity, acetic acid-induced writhing and formalin-induced pain tests were employed. CPM (100 and 300 mg/kg) reduced the number of writhing by 61% and 67%, respectively. In both doses, the activity was comparable to the reference drug, indomethacin. The oral administration of CPM was ineffective in the first phase of formalin test but exhibited great effects on the second phase decreasing the licking time by 85% at 300 mg/kg. The cytotoxic potential of CPM was also investigated against HL60, HL60.bcl2 and Jurkat tumor cell lines and showed an inhibition of more than 50% of cell proliferation. The flavones orientin and isoorientin were detected in CPM.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Cecropia/química , Extratos Vegetais/farmacologia , Animais , Antineoplásicos Fitogênicos/farmacologia , Edema/tratamento farmacológico , Células HL-60 , Humanos , Células Jurkat , Masculino , Camundongos , Dor/tratamento farmacológico , Medição da Dor
14.
Plants (Basel) ; 12(8)2023 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-37111830

RESUMO

Polygonum hydropiperoides Michx. is an Asian native plant species that is also widely distributed in the Americas. Despite its traditional uses, P. hydropiperoides is scarcely scientifically exploited. This study aimed to chemically characterize and investigate the antioxidant and antibacterial activities of hexane (HE-Ph), ethyl acetate (EAE-Ph), and ethanolic (EE-Ph) extracts from aerial parts of P. hydropiperoides. The chemical characterization was performed through HPLC-DAD-ESI/MSn. The antioxidant activity was assessed by the phosphomolybdenum reducing power, nitric oxide inhibition, and the ß-carotene bleaching assays. The antibacterial activity was determined by the minimal inhibitory concentration (MIC) and the minimal bactericidal concentration followed by the classification of the antibacterial effect. Chemical characterization revealed the expressive presence of phenolic acids and flavonoids in EAE-Ph. An increased antioxidant capacity was revealed in EAE-Ph. Regarding antibacterial activity, EAE-Ph showed weak to moderate property against 13 strains tested with MIC values ranging from 625 to 5000 µg/mL, with bactericidal or bacteriostatic effects. Glucogallin and gallic acid stand out as the most relevant bioactive compounds. These results suggest that P. hydropiperoides is a natural source of active substances, supporting this species' traditional use.

15.
An Acad Bras Cienc ; 84(4): 1073-80, 2012 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-23207707

RESUMO

In our previous work (Fabri et al. 2009), we showed that different extracts of Mitracarpus frigidus had significant antibacterial, antifungal and leishmanicidal activities. In order to increase our knowledge about this species, this work assesses the chemical composition and the in vitro biological activity of its essential oil. Thus, the essential oil obtained by hydrodistillation of the aerial parts of M. frigidus was analyzed by GC/MS. Among several compounds detected, 11 were identified, being linalool and eugenol acetate the major components. The essential oil exhibited a moderate antibacterial effect against Staphyloccocus aureus, Bacillus cereus, Pseudomonas aeruginosa and Enterobacter cloacae (MIC 250 µg/mL). On the other hand, it showed a strong antifungal effect against Cryptoccocus neoformans (MIC 8 µg/mL) and Candida albicans (MIC 63 µg/mL). Expressive activity against L. major and L. amazonensis promastigote forms with IC50 values of 47.2 and 89.7 µg/mL, respectively, were also observed. In addition, the antioxidant activity was investigated through DPPH radical-scavenging and showed a significative activity with IC50 of 38 µg/mL. The cytotoxicity against Artemia salina was moderate with LC(50) of 88 µg/mL. The results presented here are the first report on the chemical composition and biological properties of M. frigidus essential oil.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antiprotozoários/farmacologia , Óleos Voláteis/farmacologia , Rubiaceae/química , Animais , Antibacterianos/isolamento & purificação , Antifúngicos/isolamento & purificação , Antiprotozoários/isolamento & purificação , Candida albicans/efeitos dos fármacos , Cryptococcus neoformans/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Leishmania/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Óleos Voláteis/química , Testes de Sensibilidade Parasitária , Rubiaceae/classificação
16.
An Acad Bras Cienc ; 84(4): 1081-90, 2012 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-23037306

RESUMO

The bioactivity guided fractionation of the dichloromethane extract of Mitracarpus frigidus afforded the pyranonaphthoquinone psychorubrin. This compound, hitherto unknown in the genus Mitracarpus, had its biological activity evaluated against one panel of bacteria and two fungi, three tumor cell lines (HL60, Jurkat and MCF-7) and four Leishmania species. Its identity was confirmed unambiguously by (1)H, (13)C, (1)H-COSY, IR and UV-Vis spectroscopy and mass spectrometry. Psychorubrin displayed a very promising antitumor with IC(50) of 4.5, 5.6 and 1.1 µM for HL60, Jurkat and MCF-7 cell lines, respectively. Antimicrobial activity, mainly against Cryptococcus neoformans (MIC of 87.3 µM) was observed. A pronounced antileishmanial potential was also verified with IC(50) varying from 1.7 to 2.7 µM for the Leishmania species tested. This is the first report of the presence of pyranonapthoquinones in the Mitracarpus genus, which may serve as a chemotaxonomical marker.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antiprotozoários/farmacologia , Naftoquinonas/farmacologia , Rubiaceae/química , Antibacterianos/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Antiprotozoários/isolamento & purificação , Linhagem Celular Tumoral , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Leishmania/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Naftoquinonas/isolamento & purificação
17.
Molecules ; 17(9): 10344-54, 2012 Aug 29.
Artigo em Inglês | MEDLINE | ID: mdl-22932215

RESUMO

Guaco (Mikania glomerata Sprengel) syrup is one of the most popular herbal medicines used to treat the symptoms of asthmatic bronchitis, cough and hoarseness. The coumarin 2H-1-benzopyran-2-one, is one of the major constituents of Guaco and contributes to its pharmacological effects. The pharmaceutical capsule form of dry extract of Guaco is recommended by the Brazilian Program of Medicinal Plants and Herbal Medicines and used in primary health care. In order to identify a new protocol to obtain the raw material for Guaco capsule production we evaluated two methods, including a freezedrying process (lyophilization) and the spray-dryer technique, as well as the use of two adjuvants, Maltodextrins and Aerosil®, in different concentrations. The coumarin levels of the dried extracts were analyzed by UV-spectrophotometry and HPLC-UV/DAD. The adjuvant Aerosil® 8% showed better dry powder physical appearance. Lyophilization was observed to be the best process to obtain the dry extract of Guaco based on the measured coumarin levels.


Assuntos
Cumarínicos/análise , Mikania/química , Extratos Vegetais/química , Cromatografia Líquida de Alta Pressão , Liofilização , Folhas de Planta/química , Espectrofotometria
18.
J Ethnopharmacol ; 265: 113344, 2021 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-32890711

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Siparuna guianensis Aublet leaves, known as negramina, are used by indigenous and local communities in Brazil and other countries in the Americas to treat pain and inflammatory diseases. AIM OF THE STUDY: To characterize the chemical constituents and to evaluate the antioxidant, anti-inflammatory, antinociceptive and locomotor activities of the dichloromethane fraction (DF) of S. guianensis leaves. Also, an acute oral toxicity test was accomplished. MATERIAL AND METHODS: The chemical characterization of DF was performed by ultra-high pressure liquid chromatography (UHPLC) analyses coupled with a high-resolution mass spectrometer. The antioxidant potential of DF was investigated using nitric oxide (NO) and hydroxyl radical (OH) scavenging test. The evaluation study of the anti-inflammatory activity was carried out in vitro by NO measurement in stimulated macrophages and, in vivo, by croton oil-induced ear edema, LPS-induced peritonitis, and zymosan-induced arthritis in mice. Different mechanisms of central and peripheral nociception were stimulated by acetic acid-induced writhing, formalin, and tail-flick tests. Besides that, the open field assay was performed. RESULTS: UHPLC analyses of DF showed the presence of a mixture of glycosylated and methoxylated flavonoids. DF was able to scavenge NO and OH radicals in vitro and showed anti-inflammatory activity by inhibiting NO production in LPS-stimulated murine macrophages. Oral administration of DF considerably inhibited the ear edema after croton oil application and reduced the leukocyte infiltrated in LPS-induced peritonitis. In the inflammatory intra-articular zymosan-induced process, DF showed a significant reduction in the inflammatory area and of the cells in the synovial and connective tissues adjacent to the joint. Also, DF was able to reduce the intra-articular edema. In nociception models, the oral administration of DF considerably inhibited the acetic acid-induced writhings. The formalin test showed that DF attenuated the licking time in both phases, which suggested that DF reduce the nociception by central and peripheral mechanisms. In the tail-flick test, DF showed no activity. Besides that, DF did not affect the animal locomotion, and no acute toxicity was observed. CONCLUSIONS: For the first time, the anti-inflammatory and antinociceptive activities of S. guianensis were reported, supporting its ethnopharmacological uses for some inflammatory diseases and painful conditions.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Laurales/química , Extratos Vegetais/farmacologia , Analgésicos/isolamento & purificação , Animais , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Brasil , Modelos Animais de Doenças , Edema/tratamento farmacológico , Locomoção/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Macrófagos/patologia , Masculino , Medicina Tradicional , Camundongos , Camundongos Endogâmicos C57BL , Óxido Nítrico/metabolismo , Nociceptividade/efeitos dos fármacos , Dor/tratamento farmacológico , Medição da Dor
19.
J Pharm Pharmacol ; 73(1): 82-92, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-33791804

RESUMO

OBJECTIVES: Evaluation of the in-vivo anti-inflammatory activity of the methanolic extract obtained from the aerial parts of Mitracarpus frigidus (MFM) in the infection caused by two Salmonella strains and its chemical fingerprint by UFLC-quadrupole time of flight-MS. METHODS: The efficacy of MFM was investigated in a classical in-vivo Salmonella infection mouse model. A Salmonella reference strain (ATCC 13311) and a clinical isolate were used to infect mice and then MFM was orally administered during 14 days. At the end of the treatment with MFM, the infection and inflammatory levels were assayed. KEY FINDINGS: MFM treatment showed a significant reduction in mice mortality by Salmonella infection and, also, did not cause alterations in the liver function. Inhibitions of inflammatory and oxidative stress mediators [malondialdehyde (MDA), catalase, and metalloproteinase] were possibly involved in the observed effects. Chlorogenic acid, clarinoside, quercetin-pentosylhexoside, rutin, kaempferol-3O-rutinoside, kaempferol-rhamnosylhexoside and 2-azaanthraquinone were identified in MFM. CONCLUSIONS: MFM was effective in some inflammatory parameters, in the experimental conditions that were used in the study. The results presented in this study and the previous in-vitro anti-Salmonella activity reported by our research group reinforce the importance of MFM studies to considerer it as an alternative treatment for salmonellosis.


Assuntos
Anti-Inflamatórios/uso terapêutico , Inflamação/prevenção & controle , Estresse Oxidativo/efeitos dos fármacos , Fitoterapia , Extratos Vegetais/uso terapêutico , Rubiaceae/química , Infecções por Salmonella , Animais , Antibacterianos/análise , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Anti-Inflamatórios/análise , Anti-Inflamatórios/farmacologia , Antioxidantes/análise , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Catalase/metabolismo , Modelos Animais de Doenças , Inflamação/etiologia , Inflamação/metabolismo , Fígado/efeitos dos fármacos , Masculino , Malondialdeído/metabolismo , Metaloproteases/metabolismo , Camundongos , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Componentes Aéreos da Planta , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Salmonella/efeitos dos fármacos , Salmonella/crescimento & desenvolvimento , Infecções por Salmonella/complicações , Infecções por Salmonella/tratamento farmacológico , Infecções por Salmonella/metabolismo , Infecções por Salmonella/microbiologia , Especificidade da Espécie
20.
J Ethnopharmacol ; 280: 114418, 2021 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-34271111

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The leaves of Cecropia pachystachya Trécul (Urticaceae), known as embaúba, are used as hypoglycemic and for weight reduction in Brazilian traditional medicine. AIM OF THE STUDY: This study investigated the effects of a pharmaceutical formulation (ECP20) containing C. pachystachya extract on some metabolic alterations caused by a hypercaloric diet in mice. MATERIAL AND METHODS: Mice were randomly fed with a standard or hypercaloric diet and orally treated with ECP20 or vehicle for 13 weeks. Subsequently, adiposity, glucose intolerance, and the presence of nonalcoholic fatty liver disease were assessed. Adipose tissue and liver were collected after euthanasia and frozen at -80 °C for histological and antioxidant analyzes. The effect of ECP20 on the differentiation of 3T3-L1 pre-adipocytes was also investigated. RESULTS: Animals treated with ECP20 showed less weight gain, reduced glycemia, glucose tolerance restored, and hepatoprotective effect. Also, ECP20 presented significant in vivo antioxidant activity. Treatment of 3T3-L1 preadipocytes with ECP20 did not inhibit cellular differencing. CONCLUSIONS: Therefore, ECP20 presented promising effects in the control of obesity and related disorders. Considering that glucose intolerance and hyperglycemia are strong evidence for the development of type 2 diabetes, the findings corroborated the traditional use of C. pachystachya to treat this disease. The chlorogenic acid and the flavonoids orientin and iso-orientin, present in the extract, might be involved in the activities found.


Assuntos
Fármacos Antiobesidade/farmacologia , Cecropia/química , Dieta/efeitos adversos , Ingestão de Energia/efeitos dos fármacos , Hepatopatias/prevenção & controle , Extratos Vegetais/farmacologia , Animais , Fármacos Antiobesidade/química , Glicemia/efeitos dos fármacos , Teste de Tolerância a Glucose , Masculino , Medicina Tradicional , Camundongos , Obesidade/induzido quimicamente , Obesidade/prevenção & controle , Fitoterapia , Extratos Vegetais/química , Plantas Medicinais
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