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1.
Inflammopharmacology ; 26(4): 1005-1016, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29138954

RESUMO

Palicourea rigida Kunth is traditionally used for the treatment of skin diseases, kidney pains and ovarian inflammation. Based on these traditional uses, this study evaluated the topical anti-inflammatory activity of the ethanol extract from P. rigida leaves (EEPR) and identified bioactive compounds. Ear edema was induced in Swiss mice by the topical application of Croton oil, arachidonic acid, phenol and capsaicin. Histopathological analysis and myeloperoxidase and N-acetyl-ß-D-glucosaminidase activities were determined. EEPR was characterized by UHPLC-UV-MS HPLC and the isolated compound was identified through 1H and 13C nuclear magnetic resonance and mass fragmentation. Interaction profiles between quercetin 3-O-ß-D-glucoside and cyclooxygenase-1 and -2 were established by molecular docking. EEPR significantly inhibited ear edema induced by Croton oil (p < 0.001), arachidonic acid (p < 0.01), phenol (p < 0.001) and capsaicin (p < 0.01 or p < 0.001). Histopathological analysis showed a reduction of edema, inflammatory cell infiltration and vasodilation. Additionally, the myeloperoxidase and N-acetyl-ß-D-glucosaminidase activities were decreased (p < 0.001). From spectroscopic data, quercetin 3-O-ß-D-glucoside was the identified compound. This compound can to interact with cyclooxygenase-1 and -2 through van der Waals interactions and dipole-dipole and hydrogen bonding's, demonstrating inhibition of these enzymes. The results indicate that EEPR is a source of active compounds with topical anti-inflammatory activity, justifying the traditional use of P. rigida and showing that this species has a therapeutic potential to treat skin inflammatory processes.


Assuntos
Anti-Inflamatórios/farmacologia , Edema/tratamento farmacológico , Extratos Vegetais/farmacologia , Rubiaceae/química , Administração Tópica , Animais , Anti-Inflamatórios/isolamento & purificação , Cromatografia Líquida de Alta Pressão/métodos , Modelos Animais de Doenças , Edema/patologia , Inflamação/tratamento farmacológico , Inflamação/patologia , Masculino , Camundongos , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Folhas de Planta
2.
An Acad Bras Cienc ; 88(3): 1471-1484, 2016 09.
Artigo em Inglês | MEDLINE | ID: mdl-27411067

RESUMO

The present study was designed to investigate the antioxidant, antinociceptive and anti-inflammatory activities of the ethanol extract from Ageratum fastigiatum branches. Phytochemical screening and total phenol and flavonoid contents were determined. The antioxidant activity was assessed by 2,2-diphenyl-1-pycrilhydrazin (DPPH) and iron reducing power methods. The antinociceptive effect was evaluated using the acetic acid-induced writhing, formalin, hot plate and tail immersion assays; while the carrageenan-induced paw edema and pleurisy tests were performed to examine the anti-inflammatory activity against acute inflammation. The extract revealed the presence of flavonoids, tannins, coumarins, terpenes, sterols and saponins. Expressive levels of total phenols and flavonoids and a promising antioxidant effect were quantified. At the doses of 50, 100 and 200 mg/kg, the extract inhibited the writhing, reduced both phases of paw licking time and increased the reaction time on the hot plate. In the tail immersion test, the extract (50, 100 and 200 mg/kg) caused a significant inhibition of pain. In these doses, the paw edema, exudate volume and leucocyte mobilization were significantly reduced. These results suggest that A. fastigiatum can be an active source of substances with antioxidant, antinociceptive and anti-inflammatory activities, adding scientific support to the appropriate use in the Brazilian folk medicine.

3.
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
4.
Molecules ; 19(7): 9257-72, 2014 Jul 02.
Artigo em Inglês | MEDLINE | ID: mdl-24991758

RESUMO

In this work we investigated the in vivo protective effects of Baccharis dracunculifolia leaves extract (BdE) against carbon tetrachloride (CCl4)- and acetaminophen (APAP)-induced hepatotoxicity. Total phenolic content, total flavonoid content, antioxidant DPPH radical scavenging activity, and HPLC analysis were performed. Our results showed that pretreatment with BdE significantly reduced the damage caused by CCl4 and APAP on the serum markers of hepatic injury, AST, ALT, and ALP. Results were confirmed by histopathological analysis. Phytochemical analysis, performed by HPLC, showed that BdE was rich in p-coumaric acid derivatives, caffeoylquinic acids and flavonoids. BdE also showed DPPH antioxidant activity (EC50 of 15.75±0.43 µg/mL), and high total phenolic (142.90±0.77 mg GAE/g) and flavonoid (51.47±0.60 mg RE/g) contents. This study indicated that B. dracunculifolia leaves extract has relevant in vivo hepatoprotective properties.


Assuntos
Acetaminofen/toxicidade , Analgésicos não Narcóticos/toxicidade , Baccharis/química , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Sequestradores de Radicais Livres/farmacologia , Extratos Vegetais/farmacologia , Animais , Tetracloreto de Carbono , Avaliação Pré-Clínica de Medicamentos , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/isolamento & purificação , Fígado/efeitos dos fármacos , Fígado/patologia , Masculino , Camundongos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Ratos Wistar
5.
Molecules ; 18(8): 9785-96, 2013 Aug 16.
Artigo em Inglês | MEDLINE | ID: mdl-23959191

RESUMO

The chemical composition of the essential oils obtained by hydrodistillation of different parts of Eremanthus erythropappus, including leaves, branches and inflorescences, was investigated by Gas Chromatography and Gas Chromatography/Mass Spectrometry. The antimicrobial activity of the oils was assessed by the disc diffusion and microdilution methods, while the antioxidant activity was evaluated by DPPH and reducing power tests. The main compounds found in the essential oils derived from the inflorescences and leaves were ß-caryophyllene, germacrene-D, α-copaene and ß-pinene. α-Bisabolol was the major component in the branches. The oils were active against Staphylococcus aureus, Streptococcus pyogenes and fungi, but not Escherichia coli and Pseudomonas aeruginosa. The MIC values ranged from 0.01 to 0.50 mg/mL. Using the DPPH test, the IC50 values ranged from 38.77 ± 0.76 to 102.24 ± 1.96 µg/mL, while the reducing power test produced IC50 values between 109.85 ± 1.68 and 169.53 ± 0.64 µg/mL. The results revealed that the E. erythropappus oils are new promising potential sources of antimicrobial and antioxidant compounds with good future practical applications for human health.


Assuntos
Asteraceae/química , Óleos Voláteis/química , Anti-Infecciosos/química , Antioxidantes/química , Escherichia coli/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Sesquiterpenos Monocíclicos , Óleos Voláteis/farmacologia , Sesquiterpenos Policíclicos , Pseudomonas aeruginosa/efeitos dos fármacos , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Sesquiterpenos de Germacrano/química , Staphylococcus aureus/efeitos dos fármacos , Streptococcus pyogenes/efeitos dos fármacos
6.
Data Brief ; 50: 109509, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37663780

RESUMO

Keystroke dynamics can valuably contribute to the development of intelligent authentication systems by enabling a single and continuous authentication process in a passive and non-intrusive manner by continuously verifying a user's identity. This work describes the KeyRecs dataset, which contains fixed-text and free-text samples of user typing behavior and demographic information of the participants age, gender, handedness, and nationality. The keystroke data was obtained from 99 participants of various nationalities who completed password retype and transcription exercises. The recorded samples consist of inter-key latencies computed in a digraph fashion measuring the time between each key press and release during an exercise. KeyRecs can be leveraged to improve the recognition of authorized users and prevent unauthorized access in biometric authentication software.

7.
Biomolecules ; 13(6)2023 06 07.
Artigo em Inglês | MEDLINE | ID: mdl-37371533

RESUMO

Over the last decades, the increased incidence of metabolic disorders, such as type two diabetes and obesity, has motivated researchers to investigate new enzyme inhibitors. In this study, the inhibitory effects of synthetic amino acid derivatives (PPC80, PPC82, PPC84, PPC89, and PPC101) on the activity of digestive enzymes were assessed using in vitro assays. The inhibitory effect was determined by the inhibition percentage and the 50% inhibitory concentration (IC50), and the mechanism of action was investigated using kinetic parameters and Lineweaver-Burk plots. PPC80, PPC82, and PPC84 inhibited pancreatic lipase (IC50 of 167-1023 µM) via competitive or mixed mechanisms. The activity of pancreatic α-amylase was suppressed by PPC80, PPC82, PPC84, PPC89, and PPC101 (IC50 of 162-519 µM), which acted as competitive or mixed inhibitors. Finally, PPC84, PPC89, and PPC101 also showed potent inhibitory effects on α-glucosidase (IC50 of 51-353 µM) as competitive inhibitors. The results suggest that these synthetic amino acid derivatives have inhibitory potential against digestive enzymes and may be used as therapeutic agents to control metabolic disorders.


Assuntos
Fármacos Antiobesidade , Hipoglicemiantes , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Fármacos Antiobesidade/farmacologia , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/química , alfa-Glucosidases/metabolismo , Aminoácidos
8.
Artigo em Inglês | MEDLINE | ID: mdl-37275573

RESUMO

B. dracunculifolia is popularly used to treat skin diseases. This work aimed to evaluate the topical anti-inflammatory properties of B. dracunculifolia root extract (BdR) and its major compound baccharis oxide (BOx) on mice ear edema models. BdR was analyzed by GC-MS, and BOx was isolated by chromatographic fractionation. Topical anti-inflammatory activities were determined by using the croton oil, capsaicin, histamine, and phenol-induced mouse ear edema models. N-acetyl-ß-D- glucosaminidase (NAG) and myeloperoxidase (MPO) activities, as well as NO dosage and histopathological analyses, were also evaluated. Phytochemical analysis of BdR showed BOx as one of the major constituents. BdR and BOx (both at 0.1, 0.5, and 1.0 mg/ear) significantly reduced croton oil, histamine, and phenol-induced ear edema, while only BOx was effective in reducing capsaicin-induced edema. MPO and NAG activities, as well as NO production, were significantly inhibited by BdR and BOx. Histopathological analysis confirmed the topical anti-inflammatory properties of BdR and BOx. Our findings showed that BdR and BOx demonstrated significant topical anti-inflammatory effects in mouse ear edema induced by different agents, suggesting their possible application on skin inflammatory diseases.

9.
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.

10.
Antibiotics (Basel) ; 12(3)2023 Mar 21.
Artigo em Inglês | MEDLINE | ID: mdl-36978489

RESUMO

Vernonia polyanthes is a medicinal plant used to treat many disorders, including infectious diseases. This study investigated the chemical constituents and the antibacterial activity of V. polyanthes leaf rinse extract (Vp-LRE). The chemical characterization of Vp-LRE was established using ultra-high performance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry (UHPLC/Q-TOF-MS), and glaucolide A was identified through 1H and 13C nuclear magnetic resonance (NMR) and mass fragmentation. The cytotoxicity was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT). The antibacterial activity was assessed by minimal inhibitory concentration and minimal bactericidal concentration. Interactions between ligands and beta-lactamase were evaluated via molecular docking. UHPLC/Q-TOF-MS detected acacetin, apigenin, chrysoeriol, isorhamnetin, isorhamnetin isomer, kaempferide, 3',4'-dimethoxyluteolin, 3,7-dimethoxy-5,3',4'-trihydroxyflavone, piptocarphin A and glaucolide A. Vp-LRE (30 µg/mL) and glaucolide A (10 and 20 µg/mL) were cytotoxic against RAW 264.7 cells. Glaucolide A was not active, but Vp-LRE inhibited the Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), Escherichia coli, Salmonella Choleraesuis and Typhimurium, with a bacteriostatic effect. The compounds (glaucolide A, 3',4'-dimethoxyluteolin, acacetin and apigenin) were able to interact with beta-lactamase, mainly through hydrogen bonding, with free energy between -6.2 to -7.5 kcal/mol. These results indicate that V. polyanthes is a potential natural source of phytochemicals with a significant antibiotic effect against MRSA strains.

11.
Int J Mol Sci ; 13(3): 3887-3899, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22489187

RESUMO

The ethanol extract from Vernonia polyanthes leaves (EEVP) was investigated for antinociceptive and anti-inflammatory effects at the doses (p.o.) of 100, 200 and 400 mg/kg in animal models. The extract reduced the number of abdominal contortions by 16.75% and 31.44% at a dose of 200 and 400 mg/kg, respectively. The results obtained showed that EEVP exerted a significant antinociceptive effect in the two phases of formalin. The EEVP increased the reaction time on a hot plate at the doses of 100, 200 and 400 mg/kg after 90 min of treatment. The paw edema was reduced by EEVP at the doses of 100, 200 and 400 mg/kg after 4 h of application of carrageenan. Doses of 200 and 400 mg/kg, administered 4 h before the carrageenan injection, significantly reduced the exudate volume (29.25 and 45.74%, respectively) and leukocyte migration (18.19 and 27.95%, respectively). These results suggest that V. polyanthes can be an active source of substances with antinociceptive and anti-inflammatory activities.


Assuntos
Analgésicos/uso terapêutico , Anti-Inflamatórios não Esteroides/uso terapêutico , Extratos Vegetais/uso terapêutico , Folhas de Planta/metabolismo , Vernonia/metabolismo , Animais , Carragenina , Edema/tratamento farmacológico , Etanol/química , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Masculino , Camundongos , Dor/induzido quimicamente , Dor/tratamento farmacológico , Manejo da Dor , Medição da Dor , Ratos , Ratos Wistar
12.
Molecules ; 17(9): 11056-66, 2012 Sep 13.
Artigo em Inglês | MEDLINE | ID: mdl-22976469

RESUMO

Essential oils of Duguetia lanceolata barks, obtained at 2 (T2) and 4 h (T4), were identified by gas chromatography and gas chromatography/mass spectrometry. ß-elemene (12.7 and 14.9%), caryophyllene oxide (12.4 and 10.7%) and ß-selinene (8.4 and 10.4%) were the most abundant components in T2 and T4, respectively. The essential oils inhibited the growth of Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli and Candida albicans. The essential oils were cytotoxic against brine shrimp. The extraction time influenced the chemical composition and biological activities of essential oils obtained from the barks of D. lanceolata.


Assuntos
Annonaceae/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Antibacterianos/toxicidade , Artemia/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Candida albicans/metabolismo , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Escherichia coli/metabolismo , Testes de Sensibilidade Microbiana , Óleos Voláteis/toxicidade , Casca de Planta/química , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimento , Staphylococcus aureus/metabolismo , Streptococcus pyogenes/efeitos dos fármacos , Streptococcus pyogenes/crescimento & desenvolvimento , Streptococcus pyogenes/metabolismo
13.
Rev Soc Bras Med Trop ; 55: e07322021, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35894404

RESUMO

BACKGROUND: Neglected tropical diseases are a growing threat to global health, and endemic Chagas disease has emerged as one of the most important health problems in America. The main strategy to prevent Trypanosoma cruzi transmission is chemical control of vectors. This study presents a descriptive analysis of synanthropic triatomines before and after the implementation of a vector-control program in Bahia, Brazil. METHODS: Descriptive analysis and geospatial statistics were performed on triatomine data, (1) the relative abundance and (2) proportional spatial distribution, from Bahia during two periods: (A) 1957 to 1971 and (B) 2006 to 2019. RESULTS: We observed a decrease in the relative abundance of Panstrongylus megistus (A: n=22.032, 61.9%; B: n=1.842, 1.0%) and Triatoma infestans (A: n=1.310, 3.7%; B: n=763, 0.43%), as well as an increase in the relative abundance of T. sordida (A: n=8.314, 23.4%, B: n=146.901, 81.6%) and T. pseudomaculata (A: n=894, 2.5%, B: n=16.717, 9.3%). CONCLUSIONS: Our results indicate a clear reduction in the occurrence of P. megistus and T. infestans (last record in 2015) and an increase in the relative abundance and geographical distribution of T. sordida and T. pseudomaculata after 40 years of the vector-control program. The high frequency of other triatomine species in the municipalities of the state of Bahia and their abundance in recent years highlight the need to reinforce permanent entomological surveillance actions to prevent Chagas disease.


Assuntos
Doença de Chagas , Triatoma , Triatominae , Trypanosoma cruzi , Animais , Brasil/epidemiologia , Humanos , Insetos Vetores , Doenças Negligenciadas
14.
Int J Mol Sci ; 12(12): 8993-9008, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-22272116

RESUMO

The present study was aimed at evaluating the antinociceptive and anti-inflammatory effects of the ethanol extract from Vernonia condensata leaves in animal models, in order to afford a better understanding of these properties. The extract reduced the number of abdominal contortions at doses of 100 (51.00 ± 3.00), 200 (42.00 ± 2.98) and 400 mg/kg (39.00 ± 4.00). In formalin tests, a significant reduction in the licking time (p < 0.01) was observed in the first phase by 25.14 (200 mg/kg = 51.50 ± 4.44) and 31.15% (400 mg/kg = 48.00 ± 4.37). The doses of 100 (43.37 ± 5.15), 200 (34.62 ± 4.16) and 400 mg/kg (28.37 ± 3.98) inhibited (p < 0.001) the second phase. After 60 and 90 min of treatment, a dose of 400 mg/kg (10.13 ± 0.39 and 11.14 ± 1.33, respectively) increased the latency time. Doses of 200 and 400 mg/kg potentiated the sleeping time induced by diazepam, pentobarbital and meprobamate. The extracts (100, 200 and 400 mg/kg) showed anti-inflammatory effects by a decrease in paw edema. The extracts also reduced the exudate volume at the doses of 200 and 400 mg/kg. The leukocyte migration had significant effect (p < 0.001) at doses of 100, 200 and 400 mg/kg. The completion of additional experiments in the investigation of the antinociceptive and anti-inflammatory activities of V. condensata allowed a better understanding of the central and peripheral mechanisms involved.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Extratos Vegetais/farmacologia , Veronica/química , Analgésicos/efeitos adversos , Animais , Etanol/química , Masculino , Camundongos , Nociceptividade/efeitos dos fármacos , Extratos Vegetais/efeitos adversos , Folhas de Planta/química , Ratos , Ratos Wistar , Sono/efeitos dos fármacos
15.
Basic Clin Pharmacol Toxicol ; 128(1): 91-102, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32780565

RESUMO

Solidagenone (SOL) is a labdane-type diterpenoid found in Solidago chilensis, a plant traditionally used to treat skin diseases, kidney pain and ovarian inflammation. In this study, the topical anti-inflammatory activity of SOL was evaluated using in vivo and in silico assays. Croton oil-, arachidonic acid (AA)- and phenol-induced ear oedema mouse models were applied in the in vivo studies. Myeloperoxidase (MPO) and N-acetyl-ß-D-glucosaminidase (NAG) activities and tumour necrosis factor alpha (TNF-α), interleukin-6 (IL-6) and nitric oxide (NO) levels were determined, as well as histopathological analyses were conducted. Interaction profiles between SOL and cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), glucocorticoid receptor, estradiol-17-ß-dehydrogenase and prostaglandin-E(2)-9-reductase were established using molecular docking. SOL significantly inhibited croton oil-, AA- and phenol-induced ear oedema (P < .001) at doses of 0.1, 0.5 and 1.0 mg/ear. The MPO and NAG activities and TNF-α, IL-6 and NO levels were decreased (P < .001). The histopathological data revealed that inflammatory parameters (oedema thickness, leucocyte infiltration and vasodilatation) were reduced by treatment with SOL at doses of 0.1, 0.5 and 1.0 mg/ear. The docking study showed that SOL interacts with COX-1 and prostaglandin-E(2)-9-reductase through hydrogen bonding, inhibiting these enzymes. These results indicate that SOL may be a promising compound for the treatment of cutaneous inflammatory disorders and has potential as a topical anti-inflammatory agent.


Assuntos
Inibidores de Ciclo-Oxigenase/farmacologia , Dermatite/prevenção & controle , Edema/prevenção & controle , Furanos/farmacologia , Hidroxiprostaglandina Desidrogenases/antagonistas & inibidores , Proteínas de Membrana/antagonistas & inibidores , Naftalenos/farmacologia , Extratos Vegetais/farmacologia , Pele/efeitos dos fármacos , Solidago , Acetilglucosaminidase/metabolismo , Animais , Ciclo-Oxigenase 1/metabolismo , Inibidores de Ciclo-Oxigenase/isolamento & purificação , Inibidores de Ciclo-Oxigenase/metabolismo , Dermatite/metabolismo , Dermatite/patologia , Modelos Animais de Doenças , Edema/induzido quimicamente , Edema/metabolismo , Edema/patologia , Furanos/isolamento & purificação , Furanos/metabolismo , Ligação de Hidrogênio , Hidroxiprostaglandina Desidrogenases/metabolismo , Interleucina-6/metabolismo , Masculino , Proteínas de Membrana/metabolismo , Camundongos , Simulação de Acoplamento Molecular , Naftalenos/isolamento & purificação , Naftalenos/metabolismo , Óxido Nítrico/metabolismo , Peroxidase/metabolismo , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/metabolismo , Ligação Proteica , Transdução de Sinais , Pele/metabolismo , Pele/patologia , Solidago/química , Fator de Necrose Tumoral alfa/metabolismo
16.
Parasit Vectors ; 14(1): 492, 2021 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-34563255

RESUMO

BACKGROUND: Triatomine bugs transmit Chagas disease across Latin America, where vector control-surveillance is increasingly decentralized. Locally run systems often deal with highly diverse native-vector faunas-plus, in some areas, domestic populations of non-native species. Flexible entomological-risk indicators that cover native and non-native vectors and can support local decision-making are therefore needed. METHODS: We present a local-scale entomological-risk score ("TriatoScore") that leverages and builds upon information on the ecology-behavior and distribution-biogeography of individual triatomine bug species. We illustrate our approach by calculating TriatoScores for the 417 municipalities of Bahia state, Brazil. For this, we (i) listed all triatomine bug species recorded statewide; (ii) derived a "species relevance score" reflecting whether each species is native/non-native and, if native, whether/how often it invades/colonizes dwellings; (iii) mapped each species' presence by municipality; (iv) for native vectors, weighted presence by the proportion of municipal territory within ecoregions occupied by each species; (v) multiplied "species relevance score" × "weighted presence" to get species-specific "weighted scores"; and (vi) summed "weighted scores" across species to get municipal TriatoScores. Using standardized TriatoScores, we then grouped municipalities into high/moderate/low entomological-risk strata. RESULTS: TriatoScores were higher in municipalities dominated by dry-to-semiarid ecoregions than in those dominated by savanna-grassland or, especially, moist-forest ecoregions. Bahia's native triatomines can maintain high to moderate risk of vector-borne Chagas disease in 318 (76.3%) municipalities. Historical elimination of Triatoma infestans from 125 municipalities reduced TriatoScores by ~ 27% (range, 20-44%); eight municipalities reported T. infestans since Bahia was certified free of Trypanosoma cruzi transmission by this non-native species. Entomological-risk strata based on TriatoScores agreed well with Bahia's official disease-risk strata, but TriatoScores suggest that the official classification likely underestimates risk in 42 municipalities. Of 152 municipalities failing to report triatomines in 2006-2019, two and 71 had TriatoScores corresponding to, respectively, high and moderate entomological risk. CONCLUSIONS: TriatoScore can help control-surveillance managers to flexibly assess and stratify the entomological risk of Chagas disease at operationally relevant scales. Integrating eco-epidemiological, demographic, socioeconomic, or operational data (on, e.g., local-scale dwelling-infestation or vector-infection frequencies, land-use change and urbanization, housing conditions, poverty, or the functioning of control-surveillance systems) is also straightforward. TriatoScore may thus become a useful addition to the triatomine bug control-surveillance toolbox.


Assuntos
Doença de Chagas/transmissão , Insetos Vetores/fisiologia , Triatominae/fisiologia , Trypanosoma cruzi/fisiologia , Animais , Brasil/epidemiologia , Doença de Chagas/epidemiologia , Doença de Chagas/parasitologia , Entomologia , Meio Ambiente , Qualidade Habitacional , Humanos , Insetos Vetores/classificação , Insetos Vetores/parasitologia , Fatores de Risco , Triatominae/classificação , Triatominae/parasitologia
17.
Int J Mol Sci ; 11(5): 2067-78, 2010 May 06.
Artigo em Inglês | MEDLINE | ID: mdl-20559502

RESUMO

Antinociceptive and anti-inflammatory activities of the ethanol extract from Annona muricata L. leaves were investigated in animal models. The extract delivered per oral route (p.o.) reduced the number of abdominal contortions by 14.42% (at a dose of 200 mg/kg) and 41.41% (400 mg/kg). Doses of 200 and 400 mg/kg (p.o) inhibited both phases of the time paw licking: first phase (23.67% and 45.02%) and the second phase (30.09% and 50.02%), respectively. The extract (p.o.) increased the reaction time on a hot plate at doses of 200 (30.77% and 37.04%) and 400 mg/kg (82.61% and 96.30%) after 60 and 90 minutes of treatment, respectively. The paw edema was reduced by the ethanol extract (p.o.) at doses of 200 (23.16% and 29.33%) and 400 mg/kg (29.50% and 37.33%) after 3 to 4 h of application of carrageenan, respectively. Doses of 200 and 400 mg/kg (p.o.), administered 4 h before the carrageenan injection, reduced the exudate volume (29.25 and 45.74%) and leukocyte migration (18.19 and 27.95%) significantly. These results suggest that A. muricata can be an active source of substances with antinociceptive and anti-inflammatory activities.


Assuntos
Analgésicos/farmacologia , Annona/química , Anti-Inflamatórios/farmacologia , Etanol/química , Extratos Vegetais/farmacologia , Analgésicos/química , Animais , Anti-Inflamatórios/química , Modelos Animais de Doenças , Masculino , Camundongos , Extratos Vegetais/química , Ratos , Ratos Wistar
18.
Int J Mol Sci ; 11(10): 3942-53, 2010 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-21152311

RESUMO

Antinociceptive and anti-inflammatory activities of the Muehlenbeckia platyclada leaves' ethanol extract were investigated in animal models. The extract (p.o.) reduced the number of abdominal contortions induced by acetic acid by 21.57% (400 mg/kg). After intraplantar injection of formalin, a dose of 400 mg/kg (p.o.) inhibited the time spent paw licking in the first phase (26.43%), while the second phase was inhibited by 10.90 and 36.65% at the doses of 200 and 400 mg/kg, respectively. The extract (p.o.) increased the reaction time on a hot plate at a dose of 400 mg/kg (32.68 and 40.30%) after 60 and 90 minutes of treatment, respectively. The paw edema was reduced by extract (p.o.) at doses of 100 (15.46 and 16.67%), 200 (22.68 and 25.64%) and 400 mg/kg (29.50 and 37.33%) after 3 to 4 h of carrageenan application, respectively. Doses of 100, 200 and 400 mg/kg (p.o.), administered 4 h after the carrageenan injection, reduced the exudate volume (11.28, 21.54 and 45.13%), while leukocyte migration was reduced by 21.21 and 29.70% at the doses of 200 and 400 mg/kg, respectively. These results indicate that the ethanol extract from M. platyclada may constitute a potential target for the discovery of new molecules with antinociceptive and anti-inflammatory activities that can be explored for their therapeutic use.


Assuntos
Analgésicos/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Polygonaceae/química , Analgésicos/química , Animais , Etanol/química , Camundongos , Nociceptividade/efeitos dos fármacos , Extratos Vegetais/química , Ratos , Ratos Wistar
19.
Oxid Med Cell Longev ; 2019: 9245951, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31827708

RESUMO

Kalanchoe brasiliensis Cambess. is a native Brazilian plant popularly known as "saião", and the juice of its fresh leaves is traditionally used to treat several disorders, including inflammatory and infectious processes such as dysentery. The goals of this study were to characterize the phytochemical composition and investigate the antioxidant activity, the antibiotic effect, and the mode of action against Salmonella of the hydroethanolic extracts from K. brasiliensis leaves collected in the summer and spring Brazilian seasons. These extracts had their chemical composition established by high-performance liquid chromatography with diode-array detection. Total phenolic and flavonoid contents were spectrophotometrically determined. 2,2-Diphenyl-1-picryl-hydrazyl radical scavenging, phosphomolybdenum reducing power and ß-carotene bleaching assays were carried out to evaluate the antioxidant capacity. Antibiotic potential was assessed by minimal inhibitory concentration against 8 bacterial ATCC® and 5 methicillin-resistant Staphylococcus aureus and 5 Salmonella clinical strains. The mode of action was investigated by time-kill, bacterial cell viability, and leakage of compounds absorbing at 280 nm assays against Salmonella. Chromatographic profile and UV spectrum analyses suggested the significant presence of flavonoid type patuletin and eupafolin derivatives, and no difference between both periods of collection was noted. Significant amounts of total phenolic and flavonoid contents and a promising antioxidant capacity were observed. Hydroethanolic extracts (70%, summer and spring) were the most active against the tested Gram-positive and Gram-negative bacterial strains, showing the bacteriostatic action of 5000 µg/mL. Time-kill data demonstrated that these extracts were able to reduce the Salmonella growth rate. Cell number was reduced with release of the bacterial content. Together, these results suggest that K. brasiliensis is a natural source of antioxidant and antibacterial agents that can be applied in the research and development of new antibiotics for the treatment of Salmonella gastroenteritis because they are able to interfere in the Salmonella growth, probably due to cell membrane damage.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Resistência a Múltiplos Medicamentos/efeitos dos fármacos , Kalanchoe/química , Extratos Vegetais/farmacologia , Infecções por Salmonella/tratamento farmacológico , Salmonella/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/farmacologia , Folhas de Planta/química , Salmonella/isolamento & purificação , Infecções por Salmonella/microbiologia , Infecções por Salmonella/patologia
20.
PLoS Negl Trop Dis ; 13(8): e0007626, 2019 08.
Artigo em Inglês | MEDLINE | ID: mdl-31449534

RESUMO

Visceral leishmaniasis (VL) is a zoonosis caused by the protozoan Leishmania infantum and in Brazil is transmitted mainly by the bite of Lutzomuyia longipalpis sand flies. Data about the presence, distribution, natural infection rate, seasonal and monthly dynamics of the vector population are important for optimizing the measures to control VL in endemic areas. This study aimed to identify sand fly fauna in an endemic area for VL to detect the prevalence of L. infantum infection in the Lu. longipalpis population and to elucidate the influence of bioclimatic factors on the monthly fluctuations of this vector. HP light traps were monthly set in the intradomicile and peridomicile of residences located in the central and beachfront areas of Camaçari, a VL endemic area. The sand fly collection was conducted in two periods: i) period 1-between December 2011 and November 2012 and ii) period 2-August 2014 and July 2015. Sand fly species were identified and detection of L. infantum infection by qPCR was performed in pools of female Lu. longipalpis. For the first time, the parasite load of positive pools was correlated with the number of Lu. longipalpis captured per month in both periods. Correlation analyses between the monthly fluctuation of the sand fly population and bioclimatic indices of the municipality in both collection periods were also performed. In both evaluated periods, more than 98% of the collected sand flies were Lu. longipalpis, confirming the predominance of this species in the region. It was captured mostly in the beachfront area in all months evaluated (99%). For the period 1, Leishmania DNA was detected in 81% of tested pools representing a minimal infection rate of 9.6%. In the period 2, 40% of the pools were positive with a minimal infection rate of 10.2%. Infected sand flies were only detected in the beachfront area in both periods. The parasite load was low and did not vary in the evaluated months despite the number of collected sand flies. No correlation was observed for climatic factors in both areas of Camaçari. These findings emphasize the high risk of Leishmania transmission in Camaçari regardless of the season and that other factors, aside from bioclimatic elements, are influencing the sand fly population monthly fluctuation.


Assuntos
Leishmaniose Visceral/epidemiologia , Leishmaniose Visceral/parasitologia , Psychodidae/parasitologia , Animais , Brasil/epidemiologia , Feminino , Leishmania infantum/genética , Leishmania infantum/parasitologia , Leishmaniose Visceral/transmissão , Carga Parasitária , Prevalência , Estações do Ano
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