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1.
Bol. latinoam. Caribe plantas med. aromát ; 20(1): 38-50, 2021. tab, ilus
Artigo em Inglês | LILACS | ID: biblio-1284405

RESUMO

This study evaluated the insecticidal activity of Gallesia integrifolia essential oil from fruits, leaves, and flowers against Aedes aegyptilarvae and pupae. The essential oil was obtained by hydrodistillation and characterized by gas chromatography-mass spectrometry. Sulfur compounds represented 95 to 99% of the essential oil from fruits, leaves, and flowers. Essential oil major compounds were 2,8-dithianonane (52.6%) in fruits, 3,5-dithiahexanol-5,5-dioxide (38.9%) in leaves, and methionine ethyl ester (45.3%) in flowers. The essential oils showed high activity against larvae, and low for pupae withLC99.9of 5.87 and 1476.67µg/mL from fruits; 0.0096 and 348.33 µg/mL from leaves and 0.021and 342.84 µg/mL from flowers, respectively. The main compound with insecticide activity is probably n-ethyl-1,3-dithioisoindole, from isoindole organothiophosphate class, found in greater amount in flower and leaf essential oil. The great insecticide activity of G. integrifolia essential oil suggests that this product is a natural insecticide.


Este estudio evaluó la actividad insecticida del aceite esencial de frutos, hojas y flores de Gallesia integrifolia contra larvas y pupas de Aedes aegypti. El aceite esencial se obtuvo por hidrodestilación y se caracterizó por cromatografía de gases acoplada a espectrometría de masas. Los compuestos de azufre representaron del 95 al 99% del aceite esencial de frutas, hojas y flores. Los compuestos principales del aceite esencial fueron 2,8-ditianonano (52,6%) en frutas, 3,5-ditiahexanol-5,5-dióxido (38,9%) en hojas y éster etílico de metionina (45,3%) en flores. Los aceites esenciales mostraron alta actividad contra larvas y baja para pupas con LC99.9de 5.87 y 1476.67µg/mL de frutos; 0,0096 y 348,33 µg/mL de hojas y 0,021 y342,84 µg/mL de flores, respectivamente. El principal compuesto con actividad insecticida es probablemente el n-etil-1,3-ditioisoindol, de la clase de los organotiofosfatos de isoindol, que se encuentra en mayor cantidad en el aceite esencial de flores y hojas. La gran actividad insecticida del aceite esencial de G. integrifolia sugiere que este producto es un insecticida natural.


Assuntos
Animais , Óleos Voláteis/farmacologia , Aedes/efeitos dos fármacos , Phytolaccaceae/química , Inseticidas/farmacologia , Terpenos/análise , Óleos Voláteis/química , Inibidores da Colinesterase , Folhas de Planta/química , Flores/química , Frutas/química , Inseticidas/química , Cromatografia Gasosa-Espectrometria de Massas
2.
Molecules ; 25(6)2020 Mar 19.
Artigo em Inglês | MEDLINE | ID: mdl-32204358

RESUMO

Leishmaniasis affects around 12 million people worldwide and is estimated to cause the ninth-largest disease burden. There are three main forms of the disease, visceral (VL), cutaneous (CL), and mucocutaneous (MCL), leading to more than one million new cases every year and several thousand deaths. Current treatments based on chemically synthesized molecules are far from ideal. In this study, we have tested the in vitro and in vivo efficacy of ursolic acid (UA), a multifunctional triterpenoid with well-known antitumoral, antioxidant, and antimicrobial effects on different Leishmania strains. The in vitro antileishmanial activity against the intracellular forms was six and three-fold higher compared to extracellular forms of L. amazonensis and L. infantum, respectively. UA also showed to be a potent antileishmanial drug against both VL and CL manifestations of the disease in experimental models. UA parenterally administered at 5 mg/kg for seven days significantly reduced the parasite burden in liver and spleen not only in murine acute infection but also in a chronic-infection model against L. infantum. In addition, UA ointment (0.2%) topically administered for four weeks diminished (50%) lesion size progression in a chronic infection model of CL caused by L. amazonensis, which was much greater than the effect of UA formulated as an O/W emulsion. UA played a key role in the immunological response modulating the Th1 response. The exposure of Leishmania-infected macrophages to UA led to a significant different production in the cytokine levels depending on the Leishmania strain causing the infection. In conclusion, UA can be a promising therapy against both CL and VL.


Assuntos
Antiprotozoários/administração & dosagem , Leishmania infantum/efeitos dos fármacos , Leishmania mexicana/efeitos dos fármacos , Leishmaniose Visceral/tratamento farmacológico , Triterpenos/administração & dosagem , Administração Tópica , Animais , Antiprotozoários/farmacologia , Linhagem Celular , Modelos Animais de Doenças , Humanos , Infusões Parenterais , Leishmaniose Visceral/parasitologia , Fígado/efeitos dos fármacos , Fígado/parasitologia , Masculino , Mesocricetus , Camundongos , Phytolaccaceae/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Baço/efeitos dos fármacos , Baço/parasitologia , Triterpenos/farmacologia
3.
Bol. latinoam. Caribe plantas med. aromát ; 18(6): 595-606, nov. 2019. ilus
Artigo em Espanhol | LILACS | ID: biblio-1102648

RESUMO

Petiveria alliacea (PA) have anxiolytic, antidepressant and cognitive effects. In the present paper the effect of PA water infusion and cholinergic drugs on cognitive behavior were studied. For that, 40 male NMRI mice were divided in 4 groups: Control (n=10), Drug Control (n=10), PA (n=10) and PA plus Drug (n=10). PA 1% was administered orally (7.59±1.39 ml/day); while scopolamine (2 mg/Kg), galantamine (1 mg/Kg) and nicotine (0.1 mg/Kg) were administered intraperitoneally. Behavioral tests included: anxiety maze (AM), open field (OF) and marble burying (MB). Habituation cognitive behavior was evaluated in 4 sessions, one week each session. PA had anxiolytic and antidepressant effect effect in AM, combined with nicotine potentiated an anxiogenic effect in AM, galantamine favored habituation in OF. Scopolamine potentiated the habituation in LA and decreased the obsessive-compulsive behavior in OF. In conclusion; PA had an anxiolytic effect and favored deshabituation, combined with nicotine induced an anxiogenic effect, galantamine favored habituation and scopolamine decreased obsessive-compulsive behavior and favored motor habituation indicated a possible anxiolytic effect.


La Petiveria alliacea (PA) está relacionada con efectos ansiolíticos, antidepresivos y cognitivos. El presente trabajo estudió el efecto de la infusión de PA y drogas colinérgicas sobre la habituación. 40 ratones NMRI machos fueron divididos en 4 grupos: Control (n=10), Control Drogas (n=10), PA (n=10) y PA plus Drogas (n=10). La PA (1%) fue administrada vía oral (7.59±1.39 ml/día); escopolamina (2 mg/Kg), galantamina (1 mg/Kg) y nicotina (0.1 mg/Kg) fueron administrados vía intraperitoneal. Los ensayos conductuales incluyeron: laberinto de ansiedad (LA), campo abierto (CA) y enterramiento aversivo (EA). La habituación fue evaluada en 4 sesiones con duración de una semana cada una. PA mostró un efecto ansiolítico en el LA, combinada con nicotina potenció un efecto ansiogénico en el LA. Galantamina favoreció la habituación en CA, y escopolamina potenció el fenómeno de habituación en LA y disminuyó la conducta obsesivo-compulsiva en CA. En conclusión, la PA mostró un efecto ansiolítico y antidepresivo que potencia la deshabituación, combinada con nicotina indujo un efecto ansiogénico, galantamina favoreció la habituación y escopolamina disminuyó la conducta obsesivo­ compulsiva y favoreció la habituación motora indicando un posible efecto ansiolítico.


Assuntos
Animais , Masculino , Camundongos , Colinérgicos/farmacologia , Phytolaccaceae/química , Habituação Psicofisiológica/efeitos dos fármacos , Escopolamina/farmacologia , Galantamina/farmacologia , Nicotina/farmacologia
4.
Chin J Integr Med ; 24(12): 912-919, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30341485

RESUMO

OBJECTIVE: To examine the effect of metanol extract of Petiveria alliacea (PM) on airway inflflammation in a murine model of chronic asthma. METHODS: Two-month-old male BALB/c mice (n=6-8/group) were sensitized on days 0 and 14 by intraperitoneal injection of 20 µg ovalbumin (OVA). On day 25, the mice received an airway challenge with OVA (3%, w/v, in phosphate buffered saline). PM was administered orally by oral gavage to mice at doses of 100, 200 and 400 mg/kg body weight once daily from days 18 to 23. Control mice were orally administered phosphate buffered saline (PBS) to induce a model of asthma. At the end of the test, respiratory reactivity was assayed, the total cell number, interleukin-4 (IL-4), IL-5, IL-13, tumor necrosis factor-alpha (TNF-α) and reactive oxygen species (ROS) in the bronchoalveolar lavage fluid (BALF) were determined and the levels of serum IgE, intercellular cell adhesion molecule 1 (ICAM-1) and eotoxin were measured. In addition, lung tissue was used to qualify the IL-4, IL-5, IL-13, TNF-α and transforming growth factor beta 1 (TGF-ß1). Histologic examination was performed to observe inflammatory cellular infiltration. RESULTS: The administration of PM in comparison with the OVA-only treated group signifificantly attenuated the infifiltration of eosinophils and other inflflammatory cells (P<0.01). Airway resistance (RI) in the OVA-only induced group was significantly higher than that of the PBS control group (P<0.01) when methacholine was added. TNF-α, IgE, TGF-ß1 and cytokine levels IL-4, IL-5, IL-13 in the BALF decreased compared to control mice (P<0.01 or P<0.05). PM treatment also inhibited the production of chemokines, eotaxin and ICAM-1 in BALF (P<0.01), which improved lung function. Histopathological examination revealed that the sensitized treated PM groups had significant lower in inflammatory scores similar to dexamethasone treatments and the untreated group. CONCLUSION: Administration of PM could inhibit airway inflammation, regulate cytokines, chemokines and enhance pulmonary conditions in allergic murine model of asthma.


Assuntos
Alérgenos/imunologia , Asma/tratamento farmacológico , Inflamação/tratamento farmacológico , Pulmão/patologia , Ovalbumina/imunologia , Phytolaccaceae/química , Extratos Vegetais/uso terapêutico , Células Th2/imunologia , Animais , Asma/sangue , Asma/imunologia , Asma/fisiopatologia , Hiper-Reatividade Brônquica/complicações , Hiper-Reatividade Brônquica/tratamento farmacológico , Hiper-Reatividade Brônquica/imunologia , Hiper-Reatividade Brônquica/fisiopatologia , Líquido da Lavagem Broncoalveolar , Quimiocinas/metabolismo , Modelos Animais de Doenças , Imunoglobulina E/sangue , Inflamação/sangue , Inflamação/complicações , Inflamação/imunologia , Pulmão/imunologia , Pulmão/fisiopatologia , Masculino , Metanol , Camundongos Endogâmicos BALB C , Muco/metabolismo , Fitoterapia , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio/metabolismo
5.
Anal Chem ; 90(21): 12802-12809, 2018 11 06.
Artigo em Inglês | MEDLINE | ID: mdl-30222323

RESUMO

Several plants of agricultural and medicinal importance utilize defense chemistry that involves deployment of highly labile, reactive, and lachrymatory organosulfur molecules. However, this chemistry is difficult to investigate because the compounds are often short-lived and prone to degradation under the conditions required for analysis by common analytical techniques. This issue has complicated efforts to study the defense chemistry of plants that exploit the use of sulfur in their defense arsenals. This work illustrates how direct analysis in real time-high resolution mass spectrometry (DART-HRMS) can be used to track organosulfur defense compound chemistry under mild conditions. Petiveria alliacea was used as a model plant that exploits the enzyme alliinase to generate induced organosulfur compounds in response to herbivory. Tracking of the organosulfur compounds it produces and quantifying them by DART-HRMS using isotopically labeled analogues revealed a feedback inhibition loop through which the activities of the alliinase are stymied shortly after their activation. The results show that the downstream thiosulfinate products petivericin (100 µM) and pyruvate (8.4 mM) inhibit alliinase activity by 60% and 29%, respectively, after 1 h, and a mixture of the two inhibited alliinase activity by 65%. By 2 h, alliinase activity in the presence of these alliinase-derived products had ceased completely. Because thiosulfinate, pyruvate, and lachrymatory sulfine compounds are produced via the same alliinase-derived sulfenic acid intermediate, the inhibition of alliinase activity by increasing concentrations of downstream products shows how production of these defense compounds is modulated in real time in response to a tissue breach. These findings provide a framework within which heretofore unexplained phenomena observed in the defense chemistry of P. alliacea, onion, garlic, and other plants can be explained, as well as an approach by which to track labile compounds and enzymatic activity by DART-HRMS.


Assuntos
Liases de Carbono-Enxofre/fisiologia , Espectrometria de Massas/métodos , Phytolaccaceae/fisiologia , Liases de Carbono-Enxofre/antagonistas & inibidores , Liases de Carbono-Enxofre/isolamento & purificação , Cisteína/análogos & derivados , Cisteína/metabolismo , Retroalimentação Fisiológica , Cinética , Phytolaccaceae/enzimologia , Raízes de Plantas/enzimologia , Raízes de Plantas/fisiologia , Ácido Pirúvico/análise , Ácido Pirúvico/metabolismo , Ácidos Sulfínicos/análise , Ácidos Sulfínicos/metabolismo
6.
Braz J Microbiol ; 49 Suppl 1: 229-235, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-29706576

RESUMO

Gallesia integrifolia (Phytolaccaceae) is native to Brazil and has a strong alliaceous odor. The objective of this study was to identify the chemical composition of G. integrifolia fruit essential oil and evaluate fungicidal activity against the main food-borne diseases and food spoilage fungi. The essential oil was extracted by hydrodistillation and identified by GC-MS. From 35 identified compounds, 68% belonged to the organosulfur class. The major compounds were dimethyl trisulfide (15.49%), 2,8-dithianonane (52.63%) and lenthionine (14.69%). The utilized fungi were Aspergillus fumigatus, Aspergillus niger, Aspergillus ochraceus, Aspergillus versicolor, Penicillium funiculosum, Penicillium ochrochloron, Penicillium verrucosum var. cyclopium, and Trichoderma viride. Minimal fungicidal concentration for the essential oil varied from 0.02 to 0.18mg/mL and bifonazole and ketoconazole controls ranged from 0.20 to 3.50mg/mL. The lower concentration of the essential oil was able to control P. ochrochloron, A. fumigatus, A. versicolor, A. ochraceus and T. viride. This study shows a high fungicidal activity of G. integrifolia fruit essential oil and can support future applications by reducing the use of synthetic fungicides.


Assuntos
Fungicidas Industriais/farmacologia , Óleos Voláteis/farmacologia , Phytolaccaceae/química , Óleos Vegetais/farmacologia , Aspergillus/efeitos dos fármacos , Aspergillus/crescimento & desenvolvimento , Brasil , Frutas/química , Fungicidas Industriais/química , Cromatografia Gasosa-Espectrometria de Massas , Testes de Sensibilidade Microbiana , Óleos Voláteis/química , Penicillium/efeitos dos fármacos , Penicillium/crescimento & desenvolvimento , Óleos Vegetais/química
7.
J Ethnopharmacol ; 211: 29-37, 2018 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-28942132

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Petiveria alliacea L. (Phytolaccaceae) is used in folk medicine due to its antispasmodic, diuretic, hypoglycemic, abortive, anti-inflammatory and anticancerogenic properties. Although P. alliacea is considered toxic by people, its toxicity remains a concern since it is strongly dependent on the extraction method and the part of the plant used during tests. Even if some healers prefer to use the aerial parts in a liquefied form or by chewing them, instead of decoctions or infusions, no toxicological studies exist using whole dried stems and leaves. MATERIALS AND METHODS: The toxicity of a suspension of the powder from the leaves and stems of P. alliacea was assessed in Sprague Dawley rats by oral administration using two tests: 1) the acute toxic class method, which allows classification of substances according to their intrinsic toxicity and 2) the repeated dose 28-day method, following the guidelines 423 and 407 respectively from the Organization for the Economic Cooperation and Development. Chemical characterization of this powder was performed by GC-MS, UV-fluorescence, proximate and elemental analysis. RESULTS AND CONCLUSIONS: P. alliacea powder from stems and leaves was classed in the hazard category 5 (LD50 > 2000mg/kg) according to the acute toxicology study. There were no toxicity signs at 1000mg/kg in the repeated dose study, although higher values of total leukocytes were found in the satellite and males of the experimental group, which were attributed to the immunomodulatory properties of this plant. According to GC-MS, the prevailing compounds identified were phytol, (R)-(-)-(Z)-14-methyl-8-hexadecen-1-ol, 1-(2-hydrohyethyl)-1,2,4-triazole and methyl ß-dimethylaminoisobutyrate. In conclusion, the oral administration of the P. alliacea powder to Sprague Dawley rats did not result in deaths and was not associated with adverse effects reflected in the general condition, body weights or histopathological abnormalities.


Assuntos
Compostos Fitoquímicos/toxicidade , Phytolaccaceae , Extratos Vegetais/toxicidade , Folhas de Planta/química , Caules de Planta/química , Animais , Feminino , Contagem de Leucócitos , Masculino , Compostos Fitoquímicos/análise , Extratos Vegetais/análise , Contagem de Plaquetas , Pós , Ratos Sprague-Dawley , Suspensões , Testes de Toxicidade Aguda , Testes de Toxicidade Subaguda
8.
Int Immunopharmacol ; 54: 254-260, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29169044

RESUMO

Esculentoside A (EsA), a saponin isolated from Phytolacca esculenta, is reported as a potent suppressor of pro-inflammatory functions of macrophages. However, little is known about the target proteins of EsA for its anti-inflammatory activity. In the present study, to identify the intracellular target for EsA, affinity resins bearing immobilized EsA were used to capture binding proteins of EsA from RAW264.7 cell lysates. Mass spectrography and Western blot analysis of captured proteins indicated that ribosomal protein S3a preferentially bound to EsA affinity resin. Competition experiment further demonstrated that free EsA can disturb the specific interaction between recombinant RPS3a and affinity resin. Surface Plasmon Resonance analysis confirmed that EsA directly bound to RPS3a. Lentivirus-mediated RNAi RPS3a resulted in suppression of TNF-α and IL-6 production and impediment of signal transduction in LPS-stimulated RAW264.7 cells, indicating that RPS3a is required for LPS-triggered signaling during induction of pro-inflammatory cytokines. In addition, EsA inhibited the expression of inflammatory factors more strongly in the case of RPS3a interference. These results suggest that EsA exerts its anti-inflammatory activity by targeting RPS3a and impairing its signaling function. These new findings not only extended our understanding on the intracellular mechanisms of EsA, but also indicated RPS3a as an essential component for LPS-mediated pro-inflammatory signaling, thus implying RPS3a as a novel therapeutic target for anti-inflammatory therapy.


Assuntos
Anti-Inflamatórios/metabolismo , Macrófagos/imunologia , Ácido Oleanólico/análogos & derivados , Proteínas Ribossômicas/metabolismo , Saponinas/metabolismo , Animais , Humanos , Interleucina-6/metabolismo , Lipopolissacarídeos/imunologia , Camundongos , Ácido Oleanólico/metabolismo , Phytolaccaceae/imunologia , Ligação Proteica , Células RAW 264.7 , RNA Interferente Pequeno/genética , Proteínas Ribossômicas/genética , Transdução de Sinais , Ressonância de Plasmônio de Superfície , Fator de Necrose Tumoral alfa/metabolismo
9.
Braz. j. microbiol ; 49(supl.1): 229-235, 2018. tab, graf
Artigo em Inglês | LILACS | ID: biblio-974342

RESUMO

ABSTRACT Gallesia integrifolia (Phytolaccaceae) is native to Brazil and has a strong alliaceous odor. The objective of this study was to identify the chemical composition of G. integrifolia fruit essential oil and evaluate fungicidal activity against the main food-borne diseases and food spoilage fungi. The essential oil was extracted by hydrodistillation and identified by GC-MS. From 35 identified compounds, 68% belonged to the organosulfur class. The major compounds were dimethyl trisulfide (15.49%), 2,8-dithianonane (52.63%) and lenthionine (14.69%). The utilized fungi were Aspergillus fumigatus, Aspergillus niger, Aspergillus ochraceus, Aspergillus versicolor, Penicillium funiculosum, Penicillium ochrochloron, Penicillium verrucosum var. cyclopium, and Trichoderma viride. Minimal fungicidal concentration for the essential oil varied from 0.02 to 0.18 mg/mL and bifonazole and ketoconazole controls ranged from 0.20 to 3.50 mg/mL. The lower concentration of the essential oil was able to control P. ochrochloron, A. fumigatus, A. versicolor, A. ochraceus and T. viride. This study shows a high fungicidal activity of G. integrifolia fruit essential oil and can support future applications by reducing the use of synthetic fungicides.


Assuntos
Óleos Vegetais/farmacologia , Óleos Voláteis/farmacologia , Phytolaccaceae/química , Fungicidas Industriais/farmacologia , Penicillium/crescimento & desenvolvimento , Penicillium/efeitos dos fármacos , Aspergillus/crescimento & desenvolvimento , Aspergillus/efeitos dos fármacos , Óleos Vegetais/química , Brasil , Óleos Voláteis/química , Testes de Sensibilidade Microbiana , Frutas/química , Fungicidas Industriais/química , Cromatografia Gasosa-Espectrometria de Massas
10.
Vet Parasitol ; 248: 74-79, 2017 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-29173545

RESUMO

Methanol extracts of plant structures are promising alternatives to traditional pharmaceutical anthelminthic treatments. An in vitro evaluation was done of how methanol extracts of Diospyros anisandra bark and leaves, and Petiveria alliacea stems and leaves, collected during the rainy and dry seasons, effected cyathostomin larval development and egg hatching. Seven concentrations (600, 300, 150, 75, 37.5, 18.7 and 9.3µg/ml) were tested using the egg hatch assay. An ANOVA was applied to identify differences between the concentrations and the controls. Fifty percent lethal concentration (LC50) and the 95% confidence interval were calculated with a probit analysis. At and above 37.5µg/ml, the D. anisandra bark extracts from both seasons exhibited ≥95% egg hatch inhibition (EHI), while the D. anisandra leaf extracts had >90% EHI at and above 75µg/ml. For P. alliacea, the extracts from leaves and stems from either season exhibited >97% EHI at and above 300µg/ml, although similar efficacy was also observed at lower concentrations with the rainy season stems (75µg/ml) and leaves (150µg/ml). Values for LC50 were lowest for the rainy season D. anisandra bark (10.2µg/ml) and leaf extracts (18.4µg/ml), followed by the rainy season P. alliacea stems extract (28.2µg/ml). In the D. anisandra extracts, EHI was largely due to its ovicidal activity (≥96% beginning at 37.5µg/ml), whereas in the P. alliacea extracts it was due to L1 larval hatch failure (≥90% beginning at 75µg/ml). Overall, the rainy season D. anisandra bark extracts had a strong in vitro anthelminthic effect against cyathostomins by inhibiting larval development, and the rainy season P. alliacea stem extracts had a strong effect by preventing egg hatching. Both are possible control alternatives for these nematodes.


Assuntos
Anti-Helmínticos/farmacologia , Diospyros/química , Phytolaccaceae/química , Extratos Vegetais/farmacologia , Strongyloidea/efeitos dos fármacos , Animais , Relação Dose-Resposta a Droga , Larva/efeitos dos fármacos , Larva/crescimento & desenvolvimento , Óvulo/efeitos dos fármacos , Óvulo/crescimento & desenvolvimento , Casca de Planta/química , Folhas de Planta/química , Caules de Planta/química , Strongyloidea/crescimento & desenvolvimento
11.
Zhongguo Zhong Yao Za Zhi ; 42(1): 125-129, 2017 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-28945036

RESUMO

This study was to investigate the effect of vinegar processing on esculentosides in n-BuOH fraction and the contents of the main toxic components esculentoside B (EsB) and esculentoside C (EsC) in Phytolaccae Radix pieces. n-BuOH fraction of Phytolaccae Radix pieces was processed with vinegar according to the processing method in Chinese Pharmacopoeia. HPLC-MS-MS was adopted to analyze the esculentosides composition changes in n-BuOH fraction before and after vinegar processing. HPLC-ELSD was used to detect EsC and EsB contents in raw and vinegar processed Phytolaccae Radix pieces, and investigate the content changes before and after vinegar processing. Results showed that the esculentosides contents in n-BuOH fraction were significantly decreased except esculentoside A (EsA); there were significant changes in saponins compositions, but no new compounds were generated in n-BuOH fraction after vinegar processing. The contents of EsC and EsB were 0.12% and 0.20% respectively in raw Phytolaccae Radix, and decreased to 0.048% and 0.094% accordingly after vinegar processing. It showed that vinegar processing could significantly change the composition of esculentosides in n-BuOH fraction from Phytolaccae Radix and reduce the contents of toxic components EsC and EsB, indicating the scientificity of vinegar processing for Phytolaccae Radix.


Assuntos
Ácido Acético/química , Medicamentos de Ervas Chinesas/toxicidade , Ácido Oleanólico/análogos & derivados , Phytolaccaceae/química , Química Farmacêutica , Cromatografia Líquida de Alta Pressão
12.
Drug Dev Ind Pharm ; 43(12): 2011-2015, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28762858

RESUMO

PURPOSE: Petiveria alliacea L. (Phytolaccaceae) is a perennial shrub used by its immunomodulatory, anticancerogenic and anti-inflammatory properties. This study determined the influence of polyvinylpyrrolidone (PVP), colloidal silicon dioxide (CSD) and microcrystalline cellulose (MC) on the technological characteristic of a high-dose P. alliacea tablet prepared by the wet granulation method. METHODOLOGY: The botanical and pharmacognostic analysis of the plant material was firstly performed, followed by a 23 factorial design considering three factors at two levels: (a) the binder (PVP) incorporated in formulation at 10% and 15% (w/w); (b) the compacting agent (CSD) added at 10% and 15% (w/w) and; (c) the diluent (MC) included at 7.33% and 12.46% (w/w). The analysis of pharmaceutical performance and the accelerated and long-term stability of the best prototype were also completed. RESULT AND DISCUSSION: The binder, compacting agent and the interaction binder/diluent had a significant impact on breaking force of high-dose P. alliacea tablet. The optimum formula was found to contain 15% (w/w) of CSD, 7.33% (w/w) of MC and 10% (w/w) of PVP. At these conditions, the tablet shows a breaking force of 77.96 N, a friability of 0.39%, a total phenol content of 1.30 mg/tablet and a maximum disintegration time of 6 min. CONCLUSIONS: The use of adequate amounts of PVP, MC and CSD as per the factorial design allowed the preparation of a tablet suitable for administration, despite the inappropriate flow and compressibility properties of the P. alliacea powder.


Assuntos
Anti-Inflamatórios/administração & dosagem , Celulose/administração & dosagem , Excipientes/química , Phytolaccaceae/química , Povidona/administração & dosagem , Dióxido de Silício/administração & dosagem , Comprimidos/administração & dosagem , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Celulose/química , Química Farmacêutica , Povidona/química , Pós , Dióxido de Silício/química , Comprimidos/química
13.
Int Immunopharmacol ; 51: 148-157, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28843178

RESUMO

Esculentoside A (EsA) is a saponin isolated from the roots of Phytolacca esculenta. This study was designed to evaluate the pharmacological effects of EsA on lipopolysaccharide (LPS)-stimulated BV2 microglia and primary microglia cells. Our results indicated that EsA pretreatment significantly decreased LPS-induced production of Nitric Oxide (NO) and Prostaglandin E2 (PGE2) and impeded LPS-mediated upregulation of pro-inflammatory mediators' expression such as nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), interleukin-1ß (IL-1ß), interleukin-6 (IL-6), interleukin-12 (IL-12) and tumor necrosis factor-a (TNF-α) in both BV2 microglia and primary microglia cells. Moreover, EsA markedly suppressed nuclear factor-κB p65 (NF-κB p65) translocation by blocking IκB-α phosphorylation and degradation in LPS-treated BV2 cells. EsA also decreased phosphorylation level of mitogen-activated protein kinases (MAPKs) and inhibited NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome mediated caspase-1 activation in LPS-stimulated BV2 cells. Additionally, EsA decreased ß-amyloid1-42 (Aß1-42)-induced production of TNF-α, IL-1ß and IL-6 in primary microglia. Thus, EsA might be a promising therapeutic agent for alleviating neuroinflammatory diseases.


Assuntos
Anti-Inflamatórios/farmacologia , Microglia/patologia , Doenças Neurodegenerativas/tratamento farmacológico , Inflamação Neurogênica/tratamento farmacológico , Ácido Oleanólico/análogos & derivados , Saponinas/farmacologia , Peptídeos beta-Amiloides/imunologia , Animais , Apoptose , Linhagem Celular , Dinoprostona/metabolismo , Humanos , Lipopolissacarídeos/imunologia , Microglia/efeitos dos fármacos , NF-kappa B/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Óxido Nítrico/metabolismo , Ácido Oleanólico/farmacologia , Phytolaccaceae/imunologia , Ratos , Transdução de Sinais/efeitos dos fármacos
14.
Biomed Pharmacother ; 94: 292-306, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28763752

RESUMO

Gallesia integrifolia is a Brazilian Amazon tree whose bark decoction is popularly used to treat peptic ulcer. The essential oil from the inner stem bark of G. integrifolia (EOGi) was chemically characterized by GC/MS. The in vitro cytotoxicity and genotoxicity were evaluated in CHO-K1 cells, while the in vivo oral acute toxicity was performed in mice. The gastroprotective effect of EOGi was assessed in acidified ethanol and piroxicam and ulcer healing on acetic acid -induced ulcer models in rodents. Anti-secretory, mucus, K+-ATP channels, prostaglandins (PGs), nitric oxide (NO), TNF-α, IL-1ß, IL-10, catalase (CAT) and myeloperoxidase (MPO) activities and in vitro Helicobacter pylori action by EOGi were evaluated. EOGi exhibited cytotoxic effects only at 72h and no acute toxicity. EOGi showed gastroprotective and ulcer healing effects. EOGi gastroprotection was attenuated by indomethacin pre-treatment. Gastric volume and total acidity were reduced, while gastric pH was elevated. EOGi increased mucus and NO productions and CAT activity, and inhibited MPO activity, TNF-α and IL-1ß concentrations and augmented IL-10. EOGi was not active against H. pylori. These results indicated that EOGi is safe and exerts preventive and curative gastric ulcer effects by multitarget actions. Twenty compounds were identified and (-)-alpha-santalene was the main compound.


Assuntos
Antiulcerosos/uso terapêutico , Óleos Voláteis/uso terapêutico , Phytolaccaceae/química , Úlcera Gástrica/tratamento farmacológico , Animais , Antiulcerosos/química , Antiulcerosos/toxicidade , Células CHO , Sobrevivência Celular/efeitos dos fármacos , Cricetulus , Modelos Animais de Doenças , Feminino , Mucosa Gástrica/efeitos dos fármacos , Helicobacter pylori/efeitos dos fármacos , Masculino , Camundongos , Testes de Sensibilidade Microbiana , Testes para Micronúcleos , Óleos Voláteis/química , Óleos Voláteis/toxicidade , Casca de Planta/química , Ratos , Testes de Toxicidade Aguda
15.
J Microbiol Biotechnol ; 27(8): 1401-1408, 2017 Aug 28.
Artigo em Inglês | MEDLINE | ID: mdl-28621111

RESUMO

Petiveria alliacea L. (Phytolacaceae) is a medicinal plant with a broad range of traditional therapeutic properties, including the treatment of dysentery and intestinal infections caused by protozoan parasites. However, its effects against Entamoeba histolytica have not been reported yet. We investigated the antiamoebic activity present in the leaves of P. alliacea Antiamoebic activity was evaluated in methanolic and aqueous extracts, as well as in the hexanic, methanolic, and EtOAc fractions. The P. alliacea methanolic extract showed a better antiamoebic activity than the aqueous extract with an IC50 = 0.51 mg/ml. Likewise, the hexanic fraction was the most effective fraction, showing a dose-dependent activity against E. histolytica, with an IC50 = 0.68 mg/ml. Hexanic subfraction 12-19 showed the highest antiamoebic activity at 0.8 mg/ml, producing 74.3% growth inhibition without any toxicity in mammal cells. A major component in subfraction 12-19 was identified as isoarborinol, which produced 51.4% E. histolytica growth inhibition at 0.05 mg/ml without affecting mammal cells. The P. alliacea leaf extract has antiamoebic activity that can be attributed to a major metabolite known as isoarborinol.


Assuntos
Antiprotozoários/farmacologia , Entamoeba histolytica/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Phytolaccaceae/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Triterpenos/farmacologia , Antiprotozoários/isolamento & purificação , Concentração Inibidora 50 , Testes de Sensibilidade Parasitária , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Triterpenos/isolamento & purificação
16.
Molecules ; 22(7)2017 Jun 29.
Artigo em Inglês | MEDLINE | ID: mdl-28661449

RESUMO

The quality and the efficacy of herbal medicine are of great concern especially with the increase in their global use. Medicinal plants of different species or collected from different geographical regions have shown variations in both their contents and pharmacological activities due to the differences in the environmental conditions of the collected sites. In this study, roots of Phytolacca acinosa found in different provinces in south China (Sichuan and Shandong) and a species of Phytolacca americana were investigated. To ensure a maximum yield of the major compounds, the extraction method and conditions were optimized. The preeminent method of extraction in this analysis was determined to be the ultrasound-assisted method with specific conditions as follows: ethanol-H2O (1:1, v/v), with a solvent: sample ratio of 1:8, and extraction was performed 3 times, each for 30 min. Under these conditions, samples from the different regions varied both in quantity and quality via the LC-MS analysis. A total of 60 triterpenoid saponins were detected within the three samples, among which 22 were identified as common in the three samples. The amounts of these common triterpenoid saponin identified varied across the samples. Moreover, the analysis led to the detection of some novel compounds that have not yet been reported in this family, while other compounds differ in their fragmentation pathways compared to previous literature. To further divulge the correlations between the bioactivities in these three samples and the quantity and quality of their bioactive components, a cytotoxic analysis was thus carried out with two cancer cell lines, and SGC-7901 and Hep G2, which evidently showed remarkable differences in their anti-proliferative activities with respect to the IC50 value. Samples of P. acinosa from Sichuan showed higher values in both cell lines (27.20 ± 1.60 and 25.59 ± 1.63 µg/mL) compared to those of Shandong and P. americana. For the first time, analysis and comparison of both interspecies and of different species in this family were carried out. This study will significantly contribute to the quality insurance of herbal medicine, especially in the Phytolaccaceae family.


Assuntos
Phytolaccaceae/química , Saponinas/análise , Saponinas/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cromatografia Líquida , Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Estrutura Molecular , Extratos Vegetais/análise , Extratos Vegetais/farmacologia , Espectrometria de Massas em Tandem
17.
Vet Parasitol ; 228: 121-125, 2016 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-27692312

RESUMO

Six compounds in a methanolic extract of Petiveria alliacea stem (cis-stilbene; benzyl disulphide; benzyl trisulphide; and methyl esters of hexadecanoic acid, octadecadienoic acid and octadecenoic acid) are known to exercise acaricide activity against cattle tick Rhipicephalus microplus larvae and adults. The synergistic effect of 57 combinations of these six compounds on acaricide activity against R. microplus was evaluated. Larvae immersion tests produced the lethal concentrations needed to kill 50% (LC50) and 99% (LC99) of the population. Adult immersion tests produced rates (%) for mortality, oviposition inhibition and eclosion inhibition. Individually, none of the compounds (1% concentration) exhibited acaricide activity (mortality ≤2.3%). When combined, however, nine mixtures exhibited a synergistic increase in activity, with high mortality rates (≥92%) in larvae. Values for LC50 ranged from 0.07 to 0.51% and those for LC99 from 0.66 to 5.16%. Thirty six compound mixtures had no significant activity (mortality ≤30%) against larvae. Two mixtures exhibited synergism against adults, with high rates (≥92%) of oviposition inhibition. The mixtures based on the benzyl disulphide+benzyl trisulphide pairing produced a synergistic effect against acaricide-resistant R. microplus larva and adults, and are therefore the most promising combination for controlling this ubiquitous ectoparasite.


Assuntos
Ácidos Graxos/farmacologia , Phytolaccaceae/química , Rhipicephalus/efeitos dos fármacos , Estilbenos/farmacologia , Sulfetos/farmacologia , Acaricidas/farmacologia , Animais , Bovinos , Doenças dos Bovinos/tratamento farmacológico , Doenças dos Bovinos/parasitologia , Resistência a Medicamentos , Sinergismo Farmacológico , Quimioterapia Combinada , Feminino , Larva/efeitos dos fármacos , Oviposição/efeitos dos fármacos , Extratos Vegetais/farmacologia , Caules de Planta/química , Infestações por Carrapato/parasitologia , Infestações por Carrapato/prevenção & controle , Infestações por Carrapato/veterinária
18.
Fitoterapia ; 111: 138-46, 2016 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-27105957

RESUMO

Dibenzyl trisulfide (DTS) is the major active ingredient expressed in Petiveria alliacea L., a shrub widely used for a range of conditions, such as, arthritis, asthma and cancer. Given its use alone and concomitantly with prescription medicines, we undertook to investigate its impact on the activities of important drug metabolizing enzymes, the cytochromes P450 (CYP), a key family of enzymes involved in many adverse drug reactions. DTS and seven standardized extracts from the plant were assessed for their impact on the activities of CYPs 1A2, 2C19, 2C9, 2D6 and 3A4 on a fluorometric assay. DTS revealed significant impact against the activities of CYPs 1A2, 2C19 and 3A4 with IC50 values of 1.9, 4.0 and 3.2µM, respectively, which are equivalent to known standard inhibitors of these enzymes (furafylline, and tranylcypromine), and the most potent interaction with CYP1A2 displayed irreversible enzyme kinetics. The root extract, drawn with 96% ethanol (containing 2.4% DTS), displayed IC50 values of 5.6, 3.9 and 4.2µg/mL respectively, against the same isoforms, CYPs 1A2, 2C19 and 3A4. These investigations identify DTS as a valuable CYP inhibitor and P. alliacea as a candidate plant worthy of clinical trials to confirm the conclusions that extracts yielding high DTS may lead to clinically relevant drug interactions, whilst extracts yielding low levels of DTS, such as aqueous extracts, are unlikely to cause adverse herb-drug interactions.


Assuntos
Compostos de Benzil/farmacologia , Inibidores das Enzimas do Citocromo P-450/farmacologia , Interações Ervas-Drogas , Phytolaccaceae/química , Extratos Vegetais/farmacologia , Sulfetos/farmacologia , Humanos
19.
J Ethnopharmacol ; 184: 128-37, 2016 May 26.
Artigo em Inglês | MEDLINE | ID: mdl-26945980

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Gallesia integrifolia (Phytolaccaceae) is commonly known as "pau-d'alho" in Brazil or "garlic plant" due to the strong scent of garlic peculiar to all parts of the plant. The bark decoction is used for the treatment of microbial infections among other diseases by different ethnic groups in Brazil, Peruvian Amazonians, Bolivia and Mosetene Indians. This study aimed to advance in the antibacterial activity and characterize the mode of action of the hydroethanolic extract of the inner stem bark of G. integrifolia (HEGi) using in vivo and in vitro experimental models. MATERIALS AND METHODS: The qualitative and quantitative phytochemical analyzes of HEGi were carried out using colorimetric and HPLC technique. The cytotoxic potential of HEGi was evaluated against CHO-K1 cells by Alamar blue assay and its acute toxicity was assessed by the Hippocratic screening test using Swiss-Webster mice. The antibacterial activity was evaluated by micro- dilution method against ten strains of Gram-positive and Gram-negative bacteria. The mode of action of HEGi was investigated by outer membrane permeability, nucleotide leakage and potassium efflux assays. In vivo infection model was established by using Staphylococcus aureus infection model Wistar rats. RESULTS: Qualitative phytochemical analysis of HEGi revealed the presence of saponins, alkaloids, phenolic compounds and flavonoids. Phytochemical quantification of HEGi showed that higher total phenolic (80.10±0.62mg GAE/g) and flavonoid (16.10±0.03mg RE/g) contents. HPLC fingerprint analysis revealed the presence of gallic acid, rutin, and morin. In the Alamar blue assay no cytotoxic effect of HEGi in CHO-K1 cells was observed up to 200µg/mL, and no signs or symptoms of acute toxicity were observed in mice of both sexes at higher doses of up to 2000mg/kg, p.o. HEGi demonstrated bacteriostatic effect against selected Gram positive and Gram negative bacterial pathogens. Its mode of action is associated, at least partly, with changes in the permeability of bacterial membranes, evidenced by the increased entry of hydrophobic antibiotic in Pseudomonas aeruginosa, intense K(+) efflux and nucleotides leakage in Shigella flexneri, Streptococcus pyogenes and S. aureus. HEGi attenuated the experimental blood borne S. aureus infection in rats at all the tested doses levels (10, 50 and 250mg/kg). CONCLUSION: HEGi is safe at the dose tested when used acutely, and it presented broad antibacterial effect, which support its traditional use in the treatment of bacterial infections. It contains well known important phytochemicals, recognized to be active against bacterial pathogens in vitro and might be collectively responsible for the antibacterial activity of HEGi. It is bacteriostatic in nature, with membrane perturbation being one of it mode of action. HEGi represent a potential phytotherapic antibacterial agent.


Assuntos
Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Phytolaccaceae , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Infecções Estafilocócicas/tratamento farmacológico , Animais , Comportamento Animal/efeitos dos fármacos , Células CHO , Sobrevivência Celular/efeitos dos fármacos , Cricetulus , Feminino , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/crescimento & desenvolvimento , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/crescimento & desenvolvimento , Masculino , Camundongos , Testes de Sensibilidade Microbiana , Fitoterapia , Casca de Planta , Ratos Wistar , Infecções Estafilocócicas/microbiologia
20.
J Ethnopharmacol ; 185: 182-201, 2016 Jun 05.
Artigo em Inglês | MEDLINE | ID: mdl-26944236

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Petiveria alliacea L. commonly grows in the tropical regions of the Americas such as the Amazon forest, Central America, Caribbean islands and Mexico, as well as specific regions of Africa. Popularly known by several different names including 'mucuracaá', 'guiné' and 'pipi', P. alliacea has been used in traditional medicine for the treatment of various central nervous system (CNS) disorders, such as anxiety, pain, memory deficits and seizures, as well as for its anaesthetic and sedative properties. Furthermore, the use of this species for religious ceremonies has been reported since the era of slavery in the Americas. Therefore, the present review aims to provide a critical and comprehensive overview of the ethnobotany, phytochemistry and pharmacological properties of P. alliacea, focusing on CNS pharmacological effects, in order to identify scientific lacunae and to open new perspectives for future research. MATERIALS AND METHODS: A literature search was performed on P. alliacea using ethnobotanical textbooks, published articles in peer-reviewed journals, unpublished materials, government survey reports and scientific databases such as PubMed, Scopus, Web of Science, Science Direct and Google Scholar. The Plant List, International Plant Name Index and Kew Botanical Garden Plant name databases were used to validate the scientific names. RESULTS AND DISCUSSION: Crude extracts, fractions and phytochemical constituents isolated from various parts of P. alliacea show a wide spectrum of neuropharmacological activities including anxiolytic, antidepressant, antinociceptive and anti-seizure, and as cognitive enhancers. Phytochemistry studies of P. alliacea indicate that this plant contains a diversity of biologically active compounds, with qualitative and quantitative variations of the major compounds depending on the region of collection and the harvest season, such as essential oil (Petiverina), saponinic glycosides, isoarborinol-triterpene, isoarborinol-acetate, isoarborinol-cinnamate, steroids, alkaloids, flavonoids and tannins. Root chemical analyses have revealed coumarins, benzyl-hydroxy-ethyl-trisulphide, benzaldehyde, benzoic acid, dibenzyl trisulphide, potassium nitrate, b-sitosterol, isoarborinol, isoarborinol-acetate, isoarborinol-cinnamate, polyphenols, trithiolaniacine, glucose and glycine. CONCLUSIONS: Many traditional uses of P. alliacea have now been validated by modern pharmacology research. The available data reviewed here support the emergence of P. alliacea as a potential source for the treatment of different CNS disorders including anxiety, depression, pain, epilepsy and memory impairments. However, further studies are certainly required to improve the knowledge about the mechanisms of action, toxicity and efficacy of the plant as well as about its bioactive compounds before it can be approved in terms of its safety for therapeutic applications.


Assuntos
Sistema Nervoso Central/efeitos dos fármacos , Etnobotânica , Compostos Fitoquímicos/química , Phytolaccaceae/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Plantas Medicinais
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