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1.
Braz. j. biol ; 83: e251219, 2023. graf
Article in English | LILACS, VETINDEX | ID: biblio-1345535

ABSTRACT

Abstract The most common form of psycho-social dysfunction is anxiety with depression being related closely without any age bar. They are present with combined state of sadness, confusion, stress, fear etc. Glyoxalase system contains enzyme named glyoxalase 1 (GLO1).It is a metabolic pathway which detoxifies alpha-oxo-aldehydes, particularly methylglyoxal (MG). Methylglyoxal is mainly made by the breakdown of the glycolytic intermediates, glyceraldehyde-3-phosphates and dihydroxyacetone phosphate. Glyoxylase-1 expression is also related with anxiety behavior. A casual role or GLO-1 in anxiety behavior by using viral vectors for over expression in the anterior cingulate cortex was found and it was found that local GLO-1 over expression increased anxiety behavior. The present study deals with the molecular mechanism of protective activity of eugenol against anxiolytic disorder. A pre-clinical animal study was performed on 42 BALB/c mice. Animals were given stress through conventional restrain model. The mRNA expression of GLO-1 was analyzed by real time RT-PCR. Moreover, the GLO-1 protein expression was also examined by immunohistochemistry in whole brain and mean density was calculated. The mRNA and protein expressions were found to be increased in animals given anxiety as compared to the normal control. Whereas, the expressions were decreased in the animals treated with eugenol and its liposome-based nanocarriers in a dose dependent manner. However, the results were better in animals treated with nanocarriers as compared to the compound alone. It is concluded that the eugenol and its liposome-based nanocarriers exert anxiolytic activity by down-regulating GLO-1 protein expression in mice.


Resumo A forma mais comum de disfunção psicossocial é a ansiedade intimamente relacionada com a depressão, sem qualquer barreira de idade. Elas estão presentes em um estado combinado de tristeza, confusão, estresse, medo etc. O sistema de glioxalase contém uma enzima chamada glioxalase 1 (GLO1). É uma via metabólica que desintoxica alfa-oxo-aldeídos, particularmente metilglioxal (MG). O metilglioxal é produzido principalmente pela quebra dos intermediários glicolíticos, gliceraldeído-3-fosfatos e fosfato de diidroxiacetona. A expressão da glioxalase 1 também está relacionada ao comportamento de ansiedade. Um papel casual ou GLO1 no comportamento de ansiedade usando vetores virais para superexpressão no córtex cingulado anterior foi encontrado e descobriu-se que a superexpressão local de GLO1 aumentava o comportamento de ansiedade. O presente estudo trata do mecanismo molecular da atividade protetora do eugenol contra o transtorno ansiolítico. Um estudo pré-clínico em animais foi realizado em 42 camundongos BALB / c. Os animais foram submetidos ao estresse por meio do modelo de contenção convencional. A expressão de mRNA de GLO1 foi analisada por RT-PCR em tempo real. Além disso, a expressão da proteína GLO1 também foi examinada por imuno-histoquímica em todo o cérebro e a densidade média foi calculada. Verificou-se que as expressões de mRNA e proteínas estavam aumentadas em animais que receberam ansiedade em comparação com o controle normal. Considerando que as expressões foram diminuídas nos animais tratados com eugenol e seus nanocarreadores baseados em lipossomas de forma dependente da dose. No entanto, os resultados foram melhores em animais tratados com nanocarreadores em comparação com o composto sozinho. Conclui-se que o eugenol e seus nanocarreadores baseados em lipossomas exercem atividade ansiolítica por regulação negativa da expressão da proteína GLO1 em camundongos.


Subject(s)
Animals , Rabbits , Eugenol/therapeutic use , Eugenol/pharmacology , Lactoylglutathione Lyase/antagonists & inhibitors , Anxiety/drug therapy , Liposomes , Mice, Inbred BALB C
2.
China Journal of Chinese Materia Medica ; (24): 6502-6510, 2021.
Article in Chinese | WPRIM | ID: wpr-921810

ABSTRACT

This study aimed to investigate the effect of methyl eugenol(ME) on hypoxia/reoxygenation(H/R)-induced injury of human renal tubular epithelial HK-2 cells and its mechanism. The viability of HK-2 cells cultured with different concentrations of ME and exposed to H/R was detected by cell counting kit-8(CCK-8) assay. The effect of ME on the morphology of HK-2 cells was observed under an inverted microscope. The content of intracellular reactive oxygen species in different groups was detected after 2',7'-dichlorodihydrofluorescein diacetate(DCFH-DA) fluorescence staining. Cell apoptosis was determined by flow cytometry. Changes in mitochondrial membrane potential were monitored by JC-1 dye. The concentrations of nuclear factor erythroid 2 related factor 2(Nrf2), heme oxygenase-1(HO-1), and nicotinamide adenine dinucleotide phosphatase oxidase 4(Nox4) were measured by Western blot, followed by the assay of Nrf2 concentration changes in cytoplasm and nucleus by confocal fluorescence staining. The results showed that when the concentration of ME was 0-40 μmol·L~(-1), the activity of HK-2 cells was not affected. Compared with the model group, ME enhanced the activity of HK-2 cells and the cell morphology was normal. As revealed by further experiments, ME inhibited the release of reactive oxygen species and the decline in mitochondrial membrane potential of HK-2 cells after H/R injury, promoted Nrf2/HO-1 expression and Nrf2 translocation to the nucleus, and down-regulated the expression of Nox4, thereby significantly reducing apoptosis. This protective effect of ME could be reversed by the specific Nrf2 inhibitor ML385. These findings have preliminarily proved that ME effectively protected HK-2 cells against H/R injury, which might be related to its promotion of Nrf2/HO-1 signaling pathway and inhibition of Nox4. Such exploration on the possible mechanism of ME in the treatment of renal ischemia-reperfusion injury(IRI) and protection of organ function from the perspective of antioxidant stress has provided reference for related research on the treatment of acute kidney injury with traditional Chinese medicine.


Subject(s)
Humans , Apoptosis , Epithelial Cells/metabolism , Eugenol/pharmacology , Heme Oxygenase-1/metabolism , Hypoxia , NF-E2-Related Factor 2/metabolism , Oxidative Stress , Reactive Oxygen Species , Reperfusion Injury/drug therapy
3.
Bol. latinoam. Caribe plantas med. aromát ; 19(1): 65-76, ene. 2020. tab, ilus
Article in English | LILACS | ID: biblio-1102867

ABSTRACT

Due to the biological activities of Syzygium aromaticum essential oil, its incorporation in methacrylate polymeric (Eudragit E100) nanoparticles (NP), physical characterization, and antimicrobial essays were evaluated. The clove bears great potential for applications in dentistry. The oil was obtained by hydrodistillation and oil loaded NP using the nanoprecipitation method. Particle size and polydispersity index were determined by photon correlation spectroscopy, and physical morphology by electron microscopy. Loading capacity and in vitro eugenol release were evaluated by gas mass chromatography, and the antimicrobial activity of oil loaded-NP was calculated against Streptococcus mutans. Different chemical ingredients were characterized, and eugenol was the principal compound with 51.55%. Polymer content was directly related to NP homogenous size, which was around 150 nm with spherical morphology. A 73.2% loading capacity of eugenol was obtained. Oil loaded NP presented a fickian-type release mechanism of eugenol. Antimicrobial activity to 300 µg/mL was obtained after 24 h.


Debido a las actividades biológicas del aceite esencial de Syzygium aromaticum, se evaluó su incorporación en nanopartículas (NP) de metacrilato polimérico (Eudragit E100), su caracterización y ensayos antimicrobianos. El clavo tiene un gran potencial para aplicaciones en odontología. El aceite se obtuvo por hidrodestilación y las NP cargado de aceite utilizando el método de nanoprecipitación. El tamaño de partícula y el índice de polidispersidad se determinaron mediante espectroscopia de correlación fotónica y su morfología por microscopía electrónica. La capacidad de carga y la liberación de eugenol in vitro se evaluaron mediante cromatografía de gases en masa, y la actividad antimicrobiana se evaluó contra Streptococcus mutans. Se caracterizaron diferentes ingredientes químicos, siendo el eugenol el principal compuesto con 51.55%. El contenido de polímero se relacionó directamente con el tamaño homogéneo de NP, que fue de alrededor de 150 nm con morfología esférica. Se obtuvo un 73,2% de capacidad de carga de eugenol. El aceite cargado en NP presentó un mecanismo de liberación de eugenol de tipo fickiano. La actividad antimicrobiana a 300 µg/mL se obtuvo después de 24 h.


Subject(s)
Polymers/chemistry , Oils, Volatile/administration & dosage , Syzygium/chemistry , Nanoparticles/chemistry , Anti-Bacterial Agents/administration & dosage , Streptococcus mutans/drug effects , Eugenol/pharmacology , Oils, Volatile/pharmacology , Administration, Oral , Chromatography, Thin Layer , Drug Delivery Systems , Gas Chromatography-Mass Spectrometry , Anti-Bacterial Agents/pharmacology
4.
Bol. latinoam. Caribe plantas med. aromát ; 17(6): 610-618, nov. 2018. ilus, tab
Article in English | LILACS | ID: biblio-1007367

ABSTRACT

Peperomia hispidula (Sw.) A. Dietr. is used in Mexican traditional medicine for treating respiratory illnesses such as asthma. The latter disorder results from an excessive and inappropriate constriction of airway smooth muscle. The aim of the present study was to evaluate the relaxant activity of P. hispidula on isolated rat tracheal rings contracted with carbachol. The methyleugenol was identified as the main active constituent in the dichloromethane extract. To explore the possible mechanism of action, concentration-response curves were constructed in the presence and absence of propranolol (3 µM), indomethacin (10 µM), glibenclamide (1 µM), and L-NAME (300 µM), finding that neither reduced methyleugenol-induced smooth muscle relaxation. In conclusion, P. hispidula herein displayed relaxant activity on rat tracheal rings. The effect of methyleugenol, was probably not related to the activation of ß2-adrenoceptors, prostaglandins, K+ATP channels or nitric oxide.


Peperomia hispidula (Sw.) A. Dietr. es utilizada en la medicina tradicional mexicana para tratar enfermedades respiratorias como el asma. Este último trastorno es el resultado de una contracción excesiva e inapropiada del músculo liso de las vías respiratorias. El objetivo del presente estudio fue evaluar la actividad relajante de P. hispidula sobre anillos aislados de tráquea de rata contraídos con carbacol. El metileugenol fue identificado como el principal constituyente activo en el extracto de diclorometano. Para explorar el posible mecanismo de acción, se construyeron curvas concentración-respuesta en presencia y ausencia de propranolol (3 µM), indometacina (10 µM), glibenclamida (1 µM), y L-NAME (300 µM), encontrando que ninguno redujo la relajación del músculo liso inducida por metileugenol. En conclusión, P. hispidula muestra actividad relajante en anillos de tráquea de rata. El efecto de metileugenol, al parecer no está implicado con la activación de los receptores ß2-adrenérgicos, prostaglandinas, canales de K+ATP u óxido nítrico.


Subject(s)
Animals , Male , Rats , Trachea/drug effects , Eugenol/analogs & derivatives , Eugenol/pharmacology , Plant Extracts/pharmacology , Peperomia , Asthma/metabolism , Tracheal Stenosis/chemically induced , Eugenol/isolation & purification , Chromatography, High Pressure Liquid , Tandem Mass Spectrometry , Methylene Chloride/chemistry , Muscle Relaxation/drug effects
5.
Braz. j. biol ; 77(4): 696-702, Nov. 2017. tab, graf
Article in English | LILACS | ID: biblio-888807

ABSTRACT

Abstract The transport of live fish is a routine practice in aquaculture and constitutes a considerable source of stress to the animals. The addition of anesthetic to the water used for fish transport can prevent or mitigate the deleterious effects of transport stress. This study investigated the effects of the addition of eugenol (EUG) (1.5 or 3.0 µL L-1) and essential oil of Lippia alba (EOL) (10 or 20 µL L-1) on metabolic parameters (glycogen, lactate and total protein levels) in liver and muscle, acetylcholinesterase activity (AChE) in muscle and brain, and the levels of protein carbonyl (PC), thiobarbituric acid reactive substances (TBARS) and nonprotein thiol groups (NPSH) and activity of glutathione-S-transferase in the liver of silver catfish (Rhamdia quelen; Quoy and Gaimard, 1824) transported for four hours in plastic bags (loading density of 169.2 g L-1). The addition of various concentrations of EUG (1.5 or 3.0 µL L-1) and EOL (10 or 20 µL L-1) to the transport water is advisable for the transportation of silver catfish, since both concentrations of these substances increased the levels of NPSH antioxidant and decreased the TBARS levels in the liver. In addition, the lower liver levels of glycogen and lactate in these groups and lower AChE activity in the brain (EOL 10 or 20 µL L-1) compared to the control group indicate that the energetic metabolism and neurotransmission were lower after administration of anesthetics, contributing to the maintenance of homeostasis and sedation status.


Resumo O transporte de peixes vivos é uma prática rotineira na aquicultura e constitui uma fonte considerável de estresse para os animais. A adição de anestésicos na água utilizada para o transporte de peixes pode prevenir ou mitigar os efeitos nocivos do estresse de transporte. Este estudo investigou os efeitos da adição de eugenol (EUG) (1,5 ou 3,0 mL L-1) e óleo essencial de Lippia alba (OEL) (10 ou 20 mL L-1) em parâmetros metabólicos (níveis de glicogênio, lactato e proteína total) no fígado e músculos, a atividade da acetilcolinesterase (AChE) no músculo e no cérebro, e os níveis de proteína carbonil (PC), ácido tiobarbitúrico (TBARS) e grupos tióis não proteicos (NPSH) e atividade da glutationa-S-transferase no fígado de jundiás (Rhamdia quelen; Quoy e Gaimard, 1824) transportados por quatro horas em sacos plásticos (densidade de carga de 169,2 g L-1). A adição de várias concentrações de EUG (1,5 ou 3,0 mL L-1) e OEL (10 ou 20 mL L-1) na água de transporte é aconselhável para o transporte do jundiá, uma vez que ambas concentrações destas substâncias aumentaram os níveis do antioxidante NPSH e diminuíram os níveis de TBARS no fígado. Além disso, os níveis mais baixos de glicogénio e lactato no fígado destes grupos e menor atividade de AChE no cérebro (EOL 10 ou 20 mL L-1) em comparação com o grupo controle indicam que o metabolismo energético e neurotransmissão foram menores após a administração dos anestésicos, contribuindo para a manutenção do estado de homeostase e sedação.


Subject(s)
Animals , Catfishes/physiology , Eugenol/pharmacology , Oils, Volatile/pharmacology , Aquaculture , Lippia/chemistry , Anesthetics/pharmacology , Transportation
6.
Braz. j. biol ; 77(2): 367-371, Apr.-June 2017. graf
Article in English | LILACS | ID: biblio-888737

ABSTRACT

Abstract The present study evaluates the influence of anesthesia on the parasitic fauna of monogenea fish parasites, as its intensity and viability. Two experiments were conducted: Evaluation of an anesthetic method by sprinkling eugenol directly on gills and evaluation of monogenea motility and viability; Comparison of immersion and directly sprinkling on the gills with benzocaine and eugenol followed by evaluation on parasite intensity. The results suggest that the anesthetic sprinkling didn't interfere in the parasite motility, morphology and body surface integrity analyzed by fluorescence method. The monogenean intensity in the gills was lower in fish anesthetized by immersion method compared to the sprinkling method and the control group. This method of anesthesia can be used in parasitological studies.


Resumo O presente estudo avalia a influência da anestesia sobre a fauna parasitária de monogeneas em peixes, sua intensidade e sua viabilidade. Dois experimentos foram realizados: Avaliação de um método anestésico por aspersão eugenol diretamente nas brânquias e avaliação da motilidade das monogeneas e sua viabilidade; e Comparação entre imersão e aspersão diretamente nas brânquias com benzocaína e eugenol, seguido de avaliação sobre a intensidade parasitária. Os resultados sugerem que a aspersão do anestésico não interferiu na motilidade, morfologia, superfície corporal e integridade do parasita, analisadas pelo método de fluorescência. A intensidade de monogenéticos nas brânquias foi menor nos peixes anestesiados pelo método de imersão em comparação com o método de aspersão e o grupo controle. O método de anestesia por aspersão nas brânquias pode ser utilizado em estudos parasitológicos.


Subject(s)
Animals , Platyhelminths/drug effects , Benzocaine/pharmacology , Eugenol/pharmacology , Characiformes/physiology , Characiformes/parasitology , Anesthetics/pharmacology , Gills/drug effects , Gills/physiology , Gills/parasitology , Anesthesia/veterinary
7.
Rev. Soc. Bras. Med. Trop ; 50(1): 75-79, Jan.-Feb. 2017. tab
Article in English | LILACS | ID: biblio-842827

ABSTRACT

ABSTRACT INTRODUCTION: This study evaluated the susceptibilities of oral candidiasis-derived Candida albicans, fluconazole-resistant (FR) Candida dubliniensis, and fluconazole-susceptible (FS) C. dubliniensis to synthetic antiseptics [chlorhexidine gluconate (CHX), cetylpyridinium chloride (CPC), and triclosan (TRC)] and natural compounds (carvacrol, eugenol and thymol). METHODS: Susceptibility tests were performed based on the M27-A3 reference method. The fluconazole-resistant C. dubliniensis strains were obtained after prolonged in vitro exposure to increasing fluconazole concentrations. The geometric mean values for minimum inhibitory concentrations and minimum fungicidal concentrations were compared among the groups. RESULTS: Fluconazole-susceptible C. dubliniensis was more sensitive to CPC and TRC than FR C. dubliniensis and C. albicans were. However, eugenol and thymol were more active against FR C. dubliniensis. The fungicidal activities of CHX and TRC were similar for the three groups, and FR C. dubliniensis and C. albicans had similar sensitivities to CPC. CONCLUSIONS: The resistance of C. dubliniensis to fluconazole affects its sensitivity the synthetic antiseptics and natural compounds that were tested.


Subject(s)
Humans , Candida/drug effects , Fluconazole/pharmacology , Anti-Infective Agents, Local/pharmacology , Antifungal Agents/pharmacology , Thymol/pharmacology , Triclosan/pharmacology , Candida/isolation & purification , Candida/classification , Candida albicans/drug effects , Eugenol/pharmacology , Microbial Sensitivity Tests , Cetylpyridinium/pharmacology , Chlorhexidine/pharmacology
8.
J. oral res. (Impresa) ; 3(4): 218-224, dic. 2014. tab, ilus, graf
Article in English | LILACS | ID: lil-776884

ABSTRACT

Dental caries is a disease which affects the human oral cavity. Currently, the search for active principles of plants with antimicrobial effect seems promising for dental therapy. In this article the activity of the essential oil of Syzygium aromaticum (clove) was evaluated with an emphasis on its antimicrobial properties. The oil was obtained by hydrodistillation, characterized by thin layer chromatography and chemical tests. The main compound was identified in the oil obtained from the flower buds and its antibacterial activity against plank¬tonic cells Streptcoccus mutans ATCC700611 was assessed by performing serial dilutions, from 15 up to 1000 ug/mL, compared with 0.12 percent chlorhexidine and dimethylsulfoxide. MIC was also determined. Subsequently, UFC was analyzed and compared with CMR Test Ivoclar Vivadent. The efficiency in obtaining the oil was 2.20 percent. By using the CCD technique, a fraction was revealed by UV light, corresponding to eugenol. It had a good response for triterpenoids and flavonoids. It showed greater antimicrobial activity at concentrations of 1000, 500 and 250ug/ ml. The MIC and MBC of the oil was 125 to 250ug/mL, respectively. Eugenol was found as an active principle in the oil obtained. Currently, the impact of using plant extracts has favored the evaluation of alternative, effective and biocompatible antibacterial agents for the formulations of oral hygiene products applied to the prevention or treatment of oral diseases.


La caries dental es una enfermedad que afecta la cavidad oral en los humanos. Actualmente la búsqueda de principios activos de plantas con efecto antimicrobiano representa una promesa en la terapia Odontológica. El presente trabajo, evaluó la actividad, del aceite esencial de Syzygium aromaticum (clavo) con énfasis en su propiedad antimicrobiana. El aceite fue obtenido por hidrodestilación, caracterizado por cromatografía en capa delgada y pruebas químicas. Se iden¬tificó el compuesto principal en el aceite obtenido de los botones florales y se evaluó su actividad antibacteriana contra células plantónicas de Streptcoccus mutans ATCC (700611) realizándose diluciones seriadas; desde 15 hasta 1000ug/mL, comparándose con clorhexidina al 0.12 por ciento y dimetilsulfóxido, además se determinó la CMI. Posteriormente, se analizó las UFC, comparándose con el Test CMR® Ivoclar Vivadent. La eficiencia en la obtención del aceite fue de 2.20 por ciento. Por la técnica de CCD se identificó una fracción al revelado UV, corres¬pondiente al eugenol. Presentó respuesta positiva para flavonoides y triterpenos. Mostró mayor actividad antimicrobiana a las concentraciones de 1000, 500 y 250 ug/mL. La CMI y CMB del aceite, resultó a 125 y 250 ug/mL respectivamente. Se comprobó la presencia del eugenol como principio activo en el aceite obtenido. Actualmente la proyección del uso de extractos de plantas ha favorecido la evaluación de agentes antibacterianos alternos, eficaces y biocompatibles para su empleo en las formulaciones de productos de higiene bucal aplicados a la prevención o tratamiento de enfermedades orales.


Subject(s)
Anti-Bacterial Agents/pharmacology , Dental Caries/drug therapy , Eugenia/chemistry , Eugenol/pharmacology , Streptococcus mutans , Oils, Volatile/pharmacology , Chromatography , Microbial Sensitivity Tests
9.
Bol. latinoam. Caribe plantas med. aromát ; 13(4): 336-343, jul. 2014. ilus, tab
Article in Spanish | LILACS | ID: lil-785451

ABSTRACT

Croton malambo is a plant used in traditional medicine, in Colombia. The aim of this research was to characterize the essential oils (EO) from leaves and branches by GC-MS, NMR and determine the antiradical capacities and the in vitro and in vivo cytotoxic properties of the EO, methyleugenol (ME) and eugenol (EU). The EO of leaves and branches of C. malambo presented to ME as the main constituent (68.5 percent and 85.1 percent, respectively) and their structure was confirmed by NMR. On the other hands, the antiradical capacities (ABTS+. method) of the EO and ME were very low, obtaining only inhibition values at a fixed concentration: to 2045 ug/mL – 50 +/- 2 percent (leaves EO) and 28 +/- 1 percent (branches EO); and, 2218 ug/mL - 2.0 +/- 0.2 percent (ME). While EU had the highest value of TAA (14003 +/- 719 mmol Trolox®/kg SE). According to lymphocytes citotoxicity test, all tested substances were classified as “moderately toxic”, with values of LC50 between 310 +/- 17 – 897 +/- 11 ug/mL, being the EO the most toxic. The assessment of the toxicity in Zebra fish embryos indicated that LC50 of the branches EO, ME and EU were between 16 +/- 9 – 43 +/- 9 ug/mL, being the EU the most toxic.


Croton malambo es una planta empleada en medicina tradicional, en Colombia. El objetivo de esta investigación fue caracterizar los aceites esenciales (AE) de hojas y ramas por GC-MS, RMN y determinar las capacidades antiradicalarias y las propiedades citotóxicas in vitro e in vivo de los AE, metileugenol (ME) y eugenol (EU). Los AE de hojas y ramas de Croton malambo presentaron a ME como el constituyente principal (68.5 por ciento y 85.1 por ciento, respectivamente) y su estructura fue confirmada por RMN. Por otro lado, las capacidades antiradicalarias (método ABTS+.) de los AE y ME fueron muy bajas, obteniéndose sólo valores de inhibición a una concentración fija: a 2045 ug/mL – 50 +/- 2 por ciento (AE de hojas) y 28 +/- 1 por ciento (AE de ramas); y, 2218 ug/mL - 2.0 +/- 0.2 por ciento (ME). Mientras que, EU tuvo el mayor valor de TAA (14003 +/- 719 mmol Trolox®/kg SE). Según el ensayo de citotoxicidad en linfocitos, todas las sustancias evaluadas se catalogaron como “moderadamente tóxicas”, con valores de CL50 entre 310 +/- 17 – 897 +/- 11 ug/mL, siendo los AE los más tóxicos. La estimación de la toxicidad en embriones del pez Cebra indicó que las CL50 del AE ramas, ME y EU estuvieron entre 16 +/- 9 – 43 +/- 9 ug/mL, siendo el EU el más tóxico.


Subject(s)
Oils, Volatile/pharmacology , Croton/chemistry , Eugenol/pharmacology , Plant Leaves/chemistry , Antioxidants , Oils, Volatile/chemistry , Gas Chromatography-Mass Spectrometry
10.
Braz. j. med. biol. res ; 47(4): 328-333, 8/4/2014. graf
Article in English | LILACS | ID: lil-705768

ABSTRACT

In cardiac and skeletal muscle, eugenol (μM range) blocks excitation-contraction coupling. In skeletal muscle, however, larger doses of eugenol (mM range) induce calcium release from the sarcoplasmic reticulum. The effects of eugenol are therefore dependent on its concentration. In this study, we evaluated the effects of eugenol on the contractility of isolated, quiescent atrial trabeculae from male Wistar rats (250-300 g; n=131) and measured atrial ATP content. Eugenol (1, 3, 5, 7, and 10 mM) increased resting tension in a dose-dependent manner. Ryanodine [100 µM; a specific ryanodine receptor (RyR) blocker] and procaine (30 mM; a nonspecific RyR blocker) did not block the increased resting tension induced by eugenol regardless of whether extracellular calcium was present. The myosin-specific inhibitor 2,3-butanedione monoxime (BDM), however, reversed the increase in resting tension induced by eugenol. In Triton-skinned atrial trabeculae, in which all membranes were solubilized, eugenol did not change resting tension, maximum force produced, or the force vs pCa relationship (pCa=-log [Ca2+]). Given that eugenol reduced ATP concentration, the increase in resting tension observed in this study may have resulted from cooperative activation of cardiac thin filaments by strongly attached cross-bridges (rigor state).


Subject(s)
Animals , Male , Calcium/physiology , Eugenol/pharmacology , Excitation Contraction Coupling/drug effects , Heart Atria/drug effects , Muscle Strength/drug effects , Myocardial Contraction/drug effects , Adenosine Triphosphate/analysis , Anesthetics, Local/pharmacology , Eugenol/administration & dosage , In Vitro Techniques , Luciferases , Muscle, Skeletal/drug effects , Procaine/pharmacology , Rats, Wistar , Ryanodine/pharmacology
11.
Braz. dent. j ; 23(6): 635-644, 2012. ilus, tab
Article in English | LILACS | ID: lil-662420

ABSTRACT

This study aimed to evaluate by the intra-osseous implant technique the most commonly used materials for pulp therapy in pediatric dentistry: calcium hydroxide (CH), Guedes Pinto paste and CTZ paste, according to FDI (1980) and ANSI/ADA (1982) recommendations. Thirty guinea pigs, 10 for each material, divided into experimental periods of 4 and 12 weeks received one implant on each side of the lower jaw symphysis. The external lateral tube wall served as control for the technique. At the end of the observation periods, the animals were euthanized and specimens were prepared for routine histological examination. It was observed that CH and CTZ paste induced severe inflammation, a large amount of necrotic tissue, lymphocytes, foreign body cells and bone resorption, while Guedes Pinto Paste induced little or no inflammation in the 4-week observation period. After 12 weeks, the reactions to CH and Guedes Pinto paste were also absent/mild, presenting a general pattern of replacement by recently formed bone tissue while a moderate to severe inflammatory response was observed with CTZ paste. Guedes Pinto paste presented acceptable biocompatibility levels in both analyzed periods; CH only showed acceptable biocompatibility in the 12-week period while CTZ paste showed no biocompatibility in both periods. Among the tested materials, only Guedes Pinto paste presented an acceptable biocompatibility.


A pesquisa teve como objetivo avaliar a biocompatibilidade através da técnica de implantes intra-ósseos dos materiais utilizados em odontopediatria para tratamento pulpar: hidróxido de cálcio, pastas Guedes Pinto e CTZ, de acordo com as recomendações da FDI (1980) e ANSI/ADA(1982). Trinta guinea pigs, dez para cada material, divididos em períodos experimentais de 4 e 12 semanas receberam um implante em cada lado da sínfise mandibular. A parede lateral externa do copo serviu como controle para a técnica. No final dos períodos experimentais, os animais foram sacrificados e os espécimes preparados para o exame histológico de rotina. Observou-se que o hidróxido de cálcio e a pasta CTZ mostraram reação inflamatória severa, grande quantidade de tecido necrosado, linfócitos, células de corpo estranho e reabsorção óssea; enquanto a pasta Guedes Pinto induziu pouca ou nenhuma inflamação no período de 4 semanas. Após 12 semanas as reações para o hidróxido de cálcio e pasta Guedes Pinto foram ausentes/suaves apresentando um padrão geral de substituição por tecido ósseo neoformado, enquanto uma resposta inflamatória de moderada a severa foi observada para a pasta CTZ. A pasta Guedes Pinto apresentou níveis aceitáveis de biocompatibilidade nos dois períodos analisados; hidróxido de cálcio apresentou biocompatibilidade aceitável somente no período de 12 semanas e a pasta CTZ não mostrou biocompatibilidade em ambos os períodos. Entre estes, apenas a pasta Guedes Pinto apresentou níveis de biocompatibilidade nos dois períodos analisados.


Subject(s)
Animals , Guinea Pigs , Biocompatible Materials/pharmacology , Mandible/drug effects , Root Canal Filling Materials/pharmacology , Anti-Bacterial Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Bone Resorption/chemically induced , Calcium Hydroxide/pharmacology , Chloramphenicol/pharmacology , Drug Combinations , Eugenol/pharmacology , Giant Cells, Foreign-Body/drug effects , Hydrocarbons, Iodinated/pharmacology , Lymphocytes/drug effects , Macrophages/drug effects , Necrosis , Neutrophils/drug effects , Osteitis/chemically induced , Osteogenesis/drug effects , Prednisolone/analogs & derivatives , Prednisolone/pharmacology , Rifamycins/pharmacology , Time Factors , Tetracycline/pharmacology , Zinc Oxide/pharmacology
12.
Rev. Inst. Med. Trop. Säo Paulo ; 53(5): 271-275, Sept.-Oct. 2011. tab
Article in English | LILACS | ID: lil-602363

ABSTRACT

The effect of sub-lethal feeding of bait formulations containing molluscicidal component of Ferula asafoetida (ferulic acid, umbelliferone), Syzygium aromaticum (eugenol) and Carum carvi (limonene) on biochemical changes in the ovotestis of snail Lymnaea acuminata were studied. Bait formulations feeding to L. acuminata were studied in clear glass aquaria having diameter of 30 cm. Baits were prepared from different binary combinations of attractant amino acid (valine, aspartic acid, lysine and alanine 10 mM) in 100 mL of 2 percent agar solution + sub-lethal (20 percent and 60 percent of 24h LC50) doses of different molluscicides (ferulic acid, umbelliferone, eugenol and limonene). These baits caused maximum significant reduction in free amino acid, protein, DNA, RNA levels i.e. 41.37, 23.56, 48.36 and 14.29 percent of control in the ovotestis of the snail, respectively. Discontinuation of feeding after treatment of 60 percent of 96h LC50 of molluscicide containing bait for next 72h caused a significant recovery in free amino acid, protein, DNA and RNA levels in the ovotestis of L. acuminata.


Foi estudado o efeito subletal das iscas usadas para alimentação contendo componentes moluscicidas de Ferula asafoetida (ácido ferúlico, umbeliferone), Syzygium aromaticum (eugenol) e Carum carvi (limonene) nas alterações bioquímicas do ovoteste do caramujo Lymnaea acuminata. A formulação das iscas usadas para alimentar L. acuminata foi estudada em aquários de vidros transparentes de diâmetro de 30 cm. As iscas foram preparadas por combinações diferentes binárias de aminoácidos (valina, ácido aspártico, lisina e alanina 10 mM) em 100 mL de solução de agar a 2 por cento + doses subletais (20 por cento e 60 por cento durante 24 horas LC50) de diferentes moluscicidas (ácido ferúlico, umbeliferone, eugenol e limonene). Estas iscas causaram redução significante máxima em aminoácidos livres, proteínas, níveis de DNA e RNA isto é 41,37 por cento, 23,56 por cento, 48,36 por cento e 14,29 por cento de controle no ovoteste do caramujo, respectivamente. Discontinuação da alimentação depois do tratamento de 60 por cento de 96 horas de LC50 do moluscicida contendo a isca para as subsequentes 72 horas causou significante recuperação dos níveis de aminoácidos livres, proteína, DNA e RNA no ovoteste da L. acuminata.


Subject(s)
Animals , Female , Male , Coumaric Acids/pharmacology , Cyclohexenes/pharmacology , Eugenol/pharmacology , Lymnaea/drug effects , Molluscacides/pharmacology , Plant Extracts/pharmacology , Terpenes/pharmacology , Amino Acids , DNA , Ovary/drug effects , RNA , Time Factors , Testis/drug effects
13.
Indian J Exp Biol ; 2009 Jan; 47(1): 63-67
Article in English | IMSEAR | ID: sea-58787

ABSTRACT

Methyleugenol is naturally occurring substance in oils and fruits and in various foods as flavoring agent. Effect of this methyleugenol in inhibiting A. flavus colonization and aflatoxin production on peanut pods and kernels has been studied. Spray of methyleugenol (0.5%) on peanut pods and kernels checked the colonization of A. flavus and aflatoxin synthesis. This chemical can be used as both prophylactic or post infection spray on peanut pods before storage. It is the first report on the inhibition of A. flavus by methyleugenol on peanut.


Subject(s)
Aflatoxin B1/biosynthesis , Antifungal Agents/pharmacology , Arachis/drug effects , Arachis/microbiology , Aspergillus flavus/drug effects , Aspergillus flavus/growth & development , Biological Assay , Colony Count, Microbial , Eugenol/analogs & derivatives , Eugenol/pharmacology , Microbial Sensitivity Tests
14.
RBCF, Rev. bras. ciênc. farm. (Impr.) ; 43(1): 121-126, jan.-mar. 2007. ilus, tab, graf
Article in English | LILACS | ID: lil-451938

ABSTRACT

This study was led with the purpose of evaluating the effectiveness of eugenol, beta-pinene and alpha-pinene in inhibiting the growth of potential infectious endocarditis causing gram-positive bacteria. The phytochemicals Minimum Inhibitory Concentration-MIC was determined by solid medium diffusion procedure, while the interference of the MIC values on the bacterial cell viability was performed by viable cells count. Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae and S. pyogenes strains were used as test microorganisms. The assayed phytochemicals showed effectiveness in inhibiting all assayed bacteria strains presenting MIC values between 2.5 and 40 µL/mL. Eugenol showed the lowest MIC values which were between 2.5 and 5 µL/mL for the most bacteria strains. MIC values found to the phytochemicals were able to inhibit the cell viability of S. aureus providing a total elimination of the bacteria inoculum in a maximum time of 24 hours of exposure. These data showed the interesting antibacterial property of the assayed phytochemicals and support their possible and rational use in the antimicrobial therapy.


Este estudo foi conduzido com a proposta de avaliar a efetividade de eugenol, beta-pineno e alfa-pineno em inibir o crescimento de cepas de bactérias Gram-positivas potencialmente causadoras de endocardite infecciosa. A Concentração Inibitória Mínima-CIM dos fitoconstituintes foi determinada através do método de difusão em meio sólido, enquanto a interferência da CIM sobre a viabilidade celular bacteriana foi avaliada através da contagem de células viáveis. Cepas de Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae e S. pyogenes foram utilizadas como microrganismos teste nos ensaios antimicrobianos. Os fitoconstituintes ensaiados mostraram efetividade em inibir todas as cepas bacterianas utilizadas como microrganismos testes apresentando valores de CIM entre 2.5 e 40 µL/mL. Eugenol apresentou os menores valores de CIM, os quais estiveram entre 2,5 e 5 µL/mL para a maioria das cepas bacterianas. Os valores de CIM encontrados para os fitoconstituintes foram capazes de inibir a viabilidade celular de S. aureus causando uma total eliminação do inóculo bacteriano em um tempo máximo de 24 horas de exposição. Estes dados mostram o intenso potencial antibacteriano dos fitoconstituintes ensaiados e suportam sua possível e racional aplicação na terapia antimicrobiana.


Subject(s)
Endocarditis/metabolism , Eugenol/pharmacology , Gram-Positive Bacteria , Technology, Pharmaceutical
15.
J Environ Biol ; 2007 Jan; 28(1): 39-43
Article in English | IMSEAR | ID: sea-113357

ABSTRACT

Screening of test chemicals or formulations for antifouling (AF) activity is important to get first hand information on their nontoxic repelling activities. Especially spores of a fouling alga, Ulva pertusa were used in this study to test the AF efficiency of five organic chemicals. Coatings made with 100 microg cm2 of citral and eugenol significantly inhibited the spore attachment. A low concentration (1 microg cm2) of solanesol exhibited effective AF activity against spore attachment. Spore germination was sensitive to different AF candidates screened in this study. Based on the attachment and germination response of Ulva pertusa spores, AF efficiency of five organic AF candidates is discussed.


Subject(s)
Acetates/pharmacology , Eugenol/pharmacology , Germination/drug effects , Monoterpenes/pharmacology , Spores/drug effects , Terpenes/pharmacology , Ulva/drug effects
16.
Indian J Physiol Pharmacol ; 2005 Apr; 49(2): 125-31
Article in English | IMSEAR | ID: sea-106258

ABSTRACT

The medicinal plants are widely used by the traditional medical practitioners for curing various diseases in their day to day practice. In traditional systems of medicine, different parts (leaves, stem, flower, root, seeds and even whole plant) of Ocimum sanctum Linn (known as Tulsi in Hindi), a small herb seen throughout India, have been recommended for the treatment of bronchitis, bronchial asthma, malaria, diarrhea, dysentery, skin diseases, arthritis, painful eye diseases, chronic fever, insect bite etc. The Ocimum sanctum L. has also been suggested to possess antifertility, anticancer, antidiabetic, antifungal, antimicrobial, hepatoprotective, cardioprotective, antiemetic, antispasmodic, analgesic, adaptogenic and diaphoretic actions. Eugenol (1-hydroxy-2-methoxy-4-allylbenzene), the active constituent present in Ocimum sanctum L., has been found to be largely responsible for the therapeutic potentials of Tulsi. Although because of its great therapeutic potentials and wide occurrence in India the practitioners of traditional systems of medicine have been using Ocimum sanctum L. for curing various ailments, a rational approach to this traditional medical practice with modern system of medicine is, however, not much available. In order to establish the therapeutic uses of Ocimum sanctum L. in modern medicine, in last few decades several Indian scientists and researchers have studied the pharmacological effects of steam distilled, petroleum ether and benzene extracts of various parts of Tulsi plant and eugenol on immune system, reproductive system, central nervous system, cardiovascular system, gastric system, urinary system and blood biochemistry and have described the therapeutic significance of Tulsi in management of various ailments. These pharmacological studies have established a scientific basis for therapeutic uses of this plant.


Subject(s)
Animals , Eugenol/pharmacology , Humans , Medicine, Ayurvedic , Medicine, Traditional , Ocimum , Phytotherapy , Plant Extracts/pharmacology , Plant Leaves/chemistry , Plants, Medicinal
17.
Braz. dent. j ; 16(1): 9-16, Jan.-Apr. 2005.
Article in English | LILACS | ID: lil-415737

ABSTRACT

Foi propósito deste trabalho observar o processo de reparo de dentes de cães após obturação dos canais com dois cimentos diferentes, fazendo ou não a patência apical. Após uma sobreinstrumentação, os canais receberam um curativo de uma solução de corticosteróide-antibiótico por 7 dias, com o objetivo de obter invaginação de tecido conjuntivo para dentro dos canais. Após esse período, esse tecido foi totalmente removido em metade dos casos (grupos com patência apical) e preservados no restante dos casos (grupos sem patência apical). Os canais foram obturados pela técnica da condensação lateral empregando um cimento a base de hidróxido de cálcio (Sealer Plus) ou um cimento de Grossman (Fill Canal). Os animais foram sacrificados por overdose anestésica 60 dias após o tratamento endodôntico e as peças anatômicas foram obtidas e preparadas para análise histológica. Os dados obtidos foram analisados com base em diversos parâmetros histomorfológicos. Os resultados foram melhores nos grupos sem patência apical (p=0,01) do que nos grupos com patência. Dentre os cimentos estudados, os melhores resultados foram observados com o cimento Sealer Plus (p=0,01). Em conclusão, tanto a patência apical (presença ou ausência) quanto o tipo de material obturador de canal influíram no processo de reparo apical de dentes de cães com polpas vitais após tratamento endodôntico. O emprego de um cimento a base de hidróxido de cálcio em dentes sem patência apical promoveu os melhores resultados, dentre as condições experimentais propostas.


Subject(s)
Animals , Dogs , Root Canal Filling Materials/pharmacology , Root Canal Obturation/methods , Tooth Apex/physiology , Analysis of Variance , Barium Sulfate/pharmacology , Bismuth/pharmacology , Borates/pharmacology , Calcium Hydroxide/pharmacology , Drug Combinations , Dental Cementum/drug effects , Dental Pulp/physiology , Eugenol/pharmacology , Periodontal Ligament/drug effects , Resins, Synthetic/pharmacology , Statistics, Nonparametric , Wound Healing/drug effects , Zinc Oxide/pharmacology
18.
Rev. cuba. estomatol ; 39(2)mayo-ago. 2002.
Article in Spanish | LILACS, CUMED | ID: lil-351649

ABSTRACT

El Eugenol es un derivado fenólico conocido comúnmente como esencia de clavo, que es utilizado desde hace varios siglos en la práctica odontológica. Por sus propiedades farmacológicas tiene diferentes usos. Sus efectos farmacológicos son complejos y dependen de la concentración del Eugenol libre a la cual el tejido se expone. En este trabajo se presentan sus características farmacológicas y toxicológicas; se mencionan algunos de los mecanismos de acción propuestos para ambos efectos, y se exponen algunos de los nuevos materiales que se utilizan actualmente en estomatología; se presentan sus usos y sus ventajas sobre las formulaciones de Eugenol ya existentes(AU)


Eugenol is a phenolic derivative, commonly known as "esencia de clavo", which has been used in dental practice for centuries. Its pharmacological properties determined different uses. Its pharmacological effects are complex and depend on the concentration of free Eugenol to which the tissue is exposed. This paper presents the pharmacological and toxicological characteristics of Eugenol; it mentions some of the mechanisms of action proposed for both effects and also presents some of the new materials used in dentistry nowadays. Their uses and advantages over already existing Eugenol formulations are set forth(AU)


Subject(s)
Humans , Eugenol/pharmacology , Risk Assessment/methods , Dental Materials/therapeutic use
19.
Indian J Exp Biol ; 2000 May; 38(5): 509-11
Article in English | IMSEAR | ID: sea-57173

ABSTRACT

The present study was carried out to study the effect of antioxidants on oxidised LDL + VLDL and found that vitamin E, eugenol and tincture of crataegus (antioxidants) inhibited oxidation of (LDL + VLDL) similar to standard antioxidant (butylated hydroxy toluene). Vitamin C acted as an antioxidant at lower concentration, and prooxidant at higher concentration.


Subject(s)
Antioxidants/pharmacology , Crataegus , Diabetes Mellitus, Type 2/blood , Eugenol/pharmacology , Humans , Lipoproteins, LDL/blood , Lipoproteins, VLDL/blood , Oxidation-Reduction , Plant Extracts/pharmacology , Thiobarbituric Acid Reactive Substances/metabolism
20.
Indian J Exp Biol ; 1999 Dec; 37(12): 1192-5
Article in English | IMSEAR | ID: sea-61483

ABSTRACT

The effect of eugenol on the antioxidant status of the rat intestine after short and long term (15 days and 90 days respectively) oral administration of 1000 mg/kg.b.wt (a dosage which has been reported to be highly hepatoprotective) was studied. The level of lipid peroxidation products (TBARS) and the activities of glutathione peroxidase (GPx), glutathione reductase (GR), superoxide dismutase (SOD) and catalase (CAT) were found to be near normal on eugenol treatment. The level of glutathione (GSH) did not show any change on 15 days of eugenol treatment, but it was increased significantly on 90 day eugenol treatment. The activity of glutathione-S-transferases (GSTs) was increased significantly in both 15 day eugenol treated and 90-day eugenol treated groups. The results suggest that eugenol is nontoxic, protective and induces glutathione-S-transferases (GSTs) and thereby it may facilitate the removal of toxic substances from the intestine.


Subject(s)
Animals , Antioxidants/pharmacology , Catalase/metabolism , Eugenol/pharmacology , Glutathione/metabolism , Glutathione Transferase/metabolism , Intestines/drug effects , Male , Rats , Rats, Wistar , Superoxide Dismutase/metabolism , Thiobarbituric Acid Reactive Substances/metabolism
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