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1.
Article in English | LILACS | ID: biblio-915344

ABSTRACT

The chemical composition of the seasonal essential oils (2015-2016) from the leaves and flowers of Zaluzania montagnifolia is presented. The chemical content of those oils showed quantitative and qualitative differences. Germacrene D (19.9-29.8%), camphor (12.4- 19.4%) and ß-caryophyllene (13.7-18.5%) were the most abundant volatiles in the leaves. The essential oils from the flowers contained high amounts of camphor (32.7-37.2%) limonene (19.8-24.9%) and germacrene D (3.2-7.3%). All the seasonal essential oils showed a potent in vitro inhibition against HMG-CoA reductase. The essential oils from flowers (IC50, 40.5-55.1 µg mL-1) showed better inhibition properties than those of leaves (IC50, 84.4-123.5 µg mL-1). Camphor (IC50, 72.5 µg mL-1) and borneol (IC50, 84.4 µg mL-1) exerted a non-competitive inhibition on the enzyme. Additionally, the hydrodistillates exhibited antibacterial activity against the phytopathogenic Pseudomonas syringae pv. tabaci TBR2004 (MIC, 62.7-76.5 µg mL-1) P. syringae pv. tomato DC3000 (MIC, 45.4-50.4 µg mL-1) and P. syringae pv. phaseolicola NPS3121 (MIC, 26.7-31.9 µg mL-1). Germacrene D (MIC, 35.4-66.2 µg mL-1) and ß-caryophyllene (MIC, 36.5-54.2 µg mL-1) were the strongest anti-Pseudomonas syringae agents.


Se presenta la composición química de los aceites esenciales estacionales (2015-2016) provenientes de hojas y flores de Zaluzania montagnifolia. El contenido químico de los aceites esenciales mostró diferencias cualitativas y cuantitativas. El germacreno D (19.9-29.8%), alcanfor (12.4-19.4%) y ß-cariofileno (13.7-18.5%) fueron los volátiles más abundantes en las hojas. Los aceites esenciales de las flores contuvieron altas concentraciones de alcanfor (32.7-37.2%), limoneno (19.8-24.9%) y germacreno D (3.2-7.3%). Todos los aceites esenciales estacionales mostraron una potente inhibición in vitro contra la HMG-CoA reductasa. Los aceites esenciales de las flores (IC50, 40.5-55.1 µg mL-1) mostraron mejores propiedades inhibitorias que aquellos de las hojas (IC50, 84.4-123.5 µg mL-1). El alcanfor (IC50, 72.5 µg mL-1) y el borneol (IC50, 84.4 µg mL-1) ejercieron una inhibición no competitiva sobre la enzima. Adicionalmente, los hidrodestilados exhibieron una actividad antibacterial contra los fitopatógenos Pseudomonas syringae pv. tabaci TBR2004 (MIC, 62.7-76.5 µg mL-1) P. syringae pv. tomato DC3000 (MIC, 45.4-50.4 µg mL-1) y P. syringae pv. phaseolicola NPS3121 (MIC, 26.7-31.9 µg mL-1). El germacreno D (MIC, 35.4-66.2 µg mL-1) y ß-cariofileno (MIC, 36.5-54.2 µg mL-1) fueron los agentes más fuertes contra los patovares de Pseudomonas syringae.


Subject(s)
Oils, Volatile/chemistry , Hydroxymethylglutaryl-CoA Reductase Inhibitors/chemistry , Asteraceae , Terpenes/analysis , Oils, Volatile/pharmacology , Chromatography, Gas/methods , Hydroxymethylglutaryl-CoA Reductase Inhibitors/pharmacology , Hydroxymethylglutaryl CoA Reductases/drug effects , Anti-Bacterial Agents/pharmacology
2.
Cad. saúde pública ; 31(3): 607-619, 03/2015. tab
Article in Portuguese | LILACS | ID: lil-744832

ABSTRACT

Este estudo analisa as conexões entre saúde, direitos, legislação e políticas públicas a partir da pesquisa documental realizada no âmbito federal e nos estados do Rio Grande do Sul, Mato Grosso, Paraná e São Paulo, acerca das garantias legais das mulheres e seus filhos que vivem no cárcere. Busca instrumentalizar uma atuação garantista dos agentes públicos e dar visibilidade à problemática, diante das extremas vulnerabilidades e invisibilidade jurídica e administrativa da questão. Foram identificadas 33 normas legais, com pontos de tensão, como a possibilidade de prisão domiciliar e as disparidades quanto a prazos e condições de permanência das crianças no sistema penitenciário. A garantia legal constitucional do direito à amamentação é refletida nas regulamentações identificadas. Mas constatam-se ausências de outros aspectos relativos à maternidade na prisão, que se traduzem em dupla penalidade às mulheres, arbitrariamente estendida aos seus filhos. É necessária a ampliação e efetivação da regulamentação existente para prevenir e coibir as violações de direitos apontadas.


This study analyzes the links between health, rights, legislation, and public policies based on document research on legal safeguards for women and their children residing in prison. The research was conducted at the Federal level and in four States of Brazil: Rio Grande do Sul, Mato Grosso, Paraná, and São Paulo. The study aims to back measures by public agencies to guarantee such rights and to raise awareness of the problem, given the extreme vulnerability of women inmates and their children and the issue's legal and administrative invisibility. The authors identified 33 different legal provisions as points of tension, such as the possibility of house arrest and disparities in the terms and conditions for children to remain inside the prison system. Various provisions cite the Constitutional guarantee of women inmates' right to breastfeed in prison. Meanwhile, the study found gaps in other issues pertaining to motherhood in prison, expressed as dual incarceration (imprisonment arbitrarily extended to their children). It is necessary to expand and enforce the existing legislation to prevent such violations of rights.


Este estudio analiza las conexiones entre la salud, derechos humanos, legislación y políticas públicas, partiendo de una investigación documental, realizada a nivel federal y en los estados de Río Grande do Sul, Mato Grosso, Paraná y São Paulo, sobre las garantías jurídicas de las mujeres presas y sus hijos. El estudio pretende instrumentalizar una actuación garantista de los agentes públicos y dar visibilidad a esta problemática, frente a la extrema vulnerabilidad e invisibilidad jurídica y administrativa existente. Se identificaron 33 normas legales, con puntos de tensión, como la posibilidad de arresto domiciliario y disparidades en cuanto a los términos y condiciones de la estancia de los niños en el sistema penitenciario. La garantía constitucional del derecho a la lactancia materna se refleja en las regulaciones identificadas. No obstante, hay ausencias de otros aspectos de la maternidad en la cárcel, que se traduce en una doble pena para las mujeres, extendida arbitrariamente a sus hijos. Es necesaria la ampliación y ejecución efectiva de las regulación existente para prevenir y frenar las violaciones de los derechos.


Subject(s)
Animals , Humans , Mice , Endothelium, Vascular/metabolism , Heme Oxygenase-1/chemistry , Hydroxymethylglutaryl-CoA Reductase Inhibitors/pharmacology , Adenoviridae/metabolism , Biomechanical Phenomena , Endothelium, Vascular/cytology , Heme Oxygenase-1/metabolism , Hydrogen Peroxide/chemistry , Hydroxymethylglutaryl-CoA Reductase Inhibitors/chemistry , /metabolism , Oxidative Stress , Phosphorylation , RNA, Small Interfering/metabolism , Stress, Mechanical
3.
Rev. Soc. Cardiol. Estado de Säo Paulo ; 23(4): 40-44, out.-dez.2013.
Article in Portuguese | LILACS | ID: lil-742383

ABSTRACT

o benefício em longo prazo do tratamento com estatinas naprevenção de eventos coronarianos primários e secundários éindiscutível. Embora uma parte deste benefício esteja ligadaao efeito sobre a redução da circulação de lipoproteínasaterogênicas, outros mecanismos, como a modulação datrombogênese, a redução da inflamação e melhora da funçãoendotelial, têm sido investigados. O efeito da estatina sobrea função endotelial está ligado à sua inibição da produçãode superóxido e sua regulação positiva da síntese do óxidonítrico (NOS) no endotélio. Na prática clínica, o benefíciona função do endotélio depois do tratamento com estatinatem sido observado em uma ampla variedade de condiçõesque incluem a hipertensão arterial sistêmica, doença arterialcrônica e síndrome coronariana aguda. Esta breve revisãoincidirá sobre as principais conclusões relacionadas à terapiacom estatina sobre o tônus arterial sistêmico e doença arterialcoronariana aguda e crônica...


The long-term benefit of statin treatment on the prevention of primary and secondary coronary events is undisputed. Although a proportion of this effect has been linked to its reduction of circulating atherogenic lipoproteins, other mechanisms have been studied such as modulation of thrombogenesis, reduction of inflammation, and improvement of endothelia! function. Its favorable effect on endothelial function is tied to its inhibition of superoxide production and its positive regulation of nitric oxide synthase (NOS) in the endothelium. In the clinica! setting, the gain in endothelia! function after statin treatment has been observed in a wide range of conditions that include systernic hypertension, chronic arterial disease, and acute coronary syndrome. This brief review will focus on the main findings related to statin therapy on the systernic arterial tone and both acute and chronic coronary artery disease...


Subject(s)
Humans , Coronary Disease/therapy , Endothelium/chemistry , Hydroxymethylglutaryl-CoA Reductase Inhibitors/chemistry , Exercise Test , Pravastatin/administration & dosage , Simvastatin/administration & dosage
4.
Assiut Medical Journal. 2012; 36 (3): 201-210
in English | IMEMR | ID: emr-170187

ABSTRACT

Statins and fenofibrate are the most effective pharmacological agents used to treat hyperlipidemia. Better understanding of various pleotropic effects of statins and fenofibrate have prompted a new surge of interest in their use to treat or prevent a wide range of chronic and life-threatening disorders. Male Swiss albino mice were treated with either heat killed E. coli or saline. They were classified into 14 groups. The effects of simvastatin and fenofibrate ill with a low and a high triton dose [200 and 400 mg/kg /three times weekly for 3 weeks] on the levels of interferon-gamma [IFN-gamma], total immunoglobulins and total antioxidant activity were examined in both normal and immunized mice. Simvatatin and fenofibrate administration together with the low or high triton dose or triton alone, induced a significant rise in the level of interferon-gamma [IFN- gamma] and total immunoglobulins in immunized animals as compared to non-immunized ones. Moreover, there was all in the total antioxidant activity upon treatment with either simvastatin or fenofibrate in non-immunized and immunized hyperlipidemic mice. In conclusion, these findings revealed that treatment with low or high dose triton in combination with either simvastatin or fenofibrate increased the acquired immunity by increasing the level of interferon- gamma and total immunoglobulins. In addition, these combinations also increased the antioxidant activity during infection


Subject(s)
Male , Animals, Laboratory , Hydroxymethylglutaryl-CoA Reductase Inhibitors/chemistry , Fenofibrate/chemistry , Fenofibrate , Antioxidants , Adjuvants, Immunologic , Mice
5.
Arq. bras. cardiol ; 85(supl.5): 9-14, out. 2005. tab, graf
Article in Portuguese | LILACS | ID: lil-418867

ABSTRACT

As estatinas são agentes hipolipemiantes que exercem os seus efeitos através da inibição da HMG-CoA redutase, enzima fundamental na síntese do colesterol, levando a uma redução do colesterol tecidual e um conseqüente aumento na expressão dos receptores de LDL. Existem consideráveis diferenças entre as estatinas, no que tange às propriedades farmacocinéticas, bem como ao coeficiente de hidrofilicidade, via hepática de metabolização (especialmente, do citocromo P450 e isoenzimas), meia-vida plasmática e eficácia na redução lipídica. As estatinas também podem diferir na capacidade de interação com outras drogas que utilizam a mesma via de metabolização. Recentemente, muitos efeitos pleiotrópicos têm sido relatados com estas drogas, bem como propriedades antiinflamatórias, melhora na função endotelial e benefícios na hemostasia.


Subject(s)
Humans , Hydroxymethylglutaryl-CoA Reductase Inhibitors/pharmacokinetics , Cholesterol, LDL/metabolism , Drug Interactions , Muscular Diseases/chemically induced , Liver Diseases/chemically induced , Aryl Hydrocarbon Hydroxylases/metabolism , Hydroxymethylglutaryl-CoA Reductase Inhibitors/adverse effects , Hydroxymethylglutaryl-CoA Reductase Inhibitors/chemistry , Rhabdomyolysis/chemically induced
6.
Article in English | IMSEAR | ID: sea-124247

ABSTRACT

Previous publications have clearly demonstrated that hydroxymethylglutaryl coenzyme A [HMG-CoA] reductase activity of Schistosoma mansoni is vital for parasite reproductive activity and that drugs which inhibit this enzyme have been found to be effective antischistosomal agents. In this report we describe the expression and purification of enzymatically active schistosome HMG-CoA reductase enzyme. The recombinant protein was tested, in parallel with the mammalian enzyme, against well-known mammalian HMG-CoA reductase inhibitors obtained from various pharmaceutical companies. We demonstrated that there were significant differences in the response of the two proteins to an array of HMG-CoA reductase inhibitors. The difference in the characteristics between mammalian and schistosome enzyme could be exploited for rational drug design.


Subject(s)
Animals , Catalytic Domain , Humans , Hydroxymethylglutaryl CoA Reductases/drug effects , Hydroxymethylglutaryl-CoA Reductase Inhibitors/chemistry , Recombinant Proteins , Schistosoma mansoni/enzymology
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