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1.
Einstein (Säo Paulo) ; 18: eAO4876, 2020. tab, graf
Article in English | LILACS | ID: biblio-1039734

ABSTRACT

ABSTRACT Objective To investigate the effects of sericin extracted from silkworm Bombyx mori cocoon on morphophysiological parameters in mice with obesity induced by high-fat diet. Methods Male C57Bl6 mice aged 9 weeks were allocated to one of two groups - Control and Obese, and fed a standard or high-fat diet for 10 weeks, respectively. Mice were then further subdivided into four groups with seven mice each, as follows: Control, Control-Sericin, Obese, and Obese-Sericin. The standard or high fat diet was given for 4 more weeks; sericin (1,000mg/kg body weight) was given orally to mice in the Control-Sericin and Obese-Sericin Groups during this period. Weight gain, food intake, fecal weight, fecal lipid content, gut motility and glucose tolerance were monitored. At the end of experimental period, plasma was collected for biochemical analysis. Samples of white adipose tissue, liver and jejunum were collected and processed for light microscopy analysis; liver fragments were used for lipid content determination. Results Obese mice experienced significantly greater weight gain and fat accumulation and had higher total cholesterol and glucose levels compared to controls. Retroperitoneal and periepididymal adipocyte hypertrophy, development of hepatic steatosis, increased cholesterol and triglyceride levels and morphometric changes in the jejunal wall were observed. Conclusion Physiological changes induced by obesity were not fully reverted by sericin; however, sericin treatment restored jejunal morphometry and increased lipid excretion in feces in obese mice, suggesting potential anti-obesity effects.


RESUMO Objetivo Investigar os efeitos da sericina extraída de casulos de Bombyx mori na morfofisiologia de camundongos com obesidade induzida por dieta hiperlipídica. Métodos Camundongos machos C57Bl6, com 9 semanas de idade, foram distribuídos em Grupos Controle e Obeso, que receberam ração padrão para roedores ou dieta hiperlipídica por 10 semanas, respectivamente. Posteriormente, os animais foram redistribuídos em quatro grupos, com sete animais cada: Controle, Controle-Sericina, Obeso e Obeso-Sericina. Os animais permaneceram recebendo ração padrão ou hiperlipídica por 4 semanas, período no qual a sericina foi administrada oralmente na dose de 1.000mg/kg de massa corporal aos Grupos Controle-Sericina e Obeso-Sericina. Parâmetros fisiológicos, como ganho de peso, consumo alimentar, peso das fezes em análise de lipídios fecais, motilidade intestinal e tolerância à glicose foram monitorados. Ao término do experimento, o plasma foi coletado para dosagens bioquímicas e fragmentos de tecido adiposo branco; fígado e jejuno foram processados para análises histológicas, e amostras hepáticas foram usadas para determinação lipídica. Resultados Camundongos obesos apresentaram ganho de peso e acúmulo de gordura significativamente maior que os controles, aumento do colesterol total e glicemia. Houve hipertrofia dos adipócitos retroperitoneais e periepididimais, instalação de esteatose e aumento do colesterol e triglicerídeos hepáticos, bem como alteração morfométrica da parede jejunal. Conclusão O tratamento com sericina não reverteu todas as alterações fisiológicas promovidas pela obesidade, mas restaurou a morfometria jejunal e aumentou a quantidade de lipídios eliminados nas fezes dos camundongos obesos, apresentando-se como potencial tratamento para a obesidade.


Subject(s)
Animals , Male , Anti-Obesity Agents/therapeutic use , Sericins/therapeutic use , Obesity/drug therapy , Time Factors , Triglycerides/analysis , Body Weight/drug effects , Gastrointestinal Transit/drug effects , Weight Gain/drug effects , Adipose Tissue/pathology , Cholesterol/analysis , Reproducibility of Results , Treatment Outcome , Anti-Obesity Agents/pharmacology , Sericins/pharmacology , Eating/drug effects , Fatty Liver/pathology , Diet, High-Fat/adverse effects , Glucose Tolerance Test , Liver/metabolism , Mice, Inbred C57BL , Mice, Obese , Obesity/etiology , Obesity/physiopathology
2.
RECIIS (Online) ; 11(3): 1-19, jul.-set.2017.
Article in Portuguese | LILACS | ID: biblio-876444

ABSTRACT

Os inibidores de apetite são comercializados no Brasil há mais de 30 anos. Em 2010, a Agência Nacional de Vigilância Sanitária (Anvisa) iniciou um processo de revisão da avaliação de risco desses fármacos e cancelou, em 2011, o registro dos três emagrecedores à base de anfetamina (anfepramona, femproporex,mazindol), permitindo que apenas a sibutramina fosse comercializada. A decisão foi revogada em 2014 pelo Congresso Nacional, que autorizou a volta ao mercado brasileiro dos anorexígenos derivados da anfetamina. Este artigo analisa a construção dos sentidos sobre risco por jornais diários durante a cobertura noticiosa da controvérsia relativa aos emagrecedores, nesses dois momentos antagônicos. Com base na semiologia dos discursos sociais, foram analisadas 25 notícias de 2011 e 2014 que demonstraram que o discurso do risco,embora presente na maioria dos textos, foi minimizado pela cobertura política que privilegia os conflitos de interesses, os embates travados com a autoridade sanitária e as contradições do processo.(AU)


Appetite suppressants are sold in Brazil over 30 years. In 2010, the Agência Nacional de Vigilância Sanitária- Anvisa (National Health Surveillance Agency) began a process to review the risk assessment of these drugs and in 2011 cancelled the register of the three amphetamine-based anorexigenics (anfepramone,fenproporex, mazindol), only allowing to be marketed in Brazil the sibutramine. In 2014, the Congressrevoked the decison-making by Anvisa and authorized the sale of the amphetamine derivatives. This paper analyzes how the meanings of risk were built by daily newspapers during the coverage of the appetite suppressants controversy, considering these two antagonistic moments. Based on the social semiotics, weanalyzed 25 newspaper articles published in 2011 and in 2014, which showed that the discourse of risk doesnot assume the center of the discursive scene, resulting in a political coverage that favours the conflicts ofinterests, as well as the disputes with the Anvisa and the contradictions of the process


Los inhibidores del apetito se venden en Brasil hace más de 30 años. En 2010, la Agência Nacional deVigilância Sanitária ­ Anvisa (Agencia Nacional de Vigilancia Sanitaria) inició un proceso de revisión dela evaluación de riesgos de estos fármacos y ha cancelado, en 2011, la inscripción en el registro de los tresinhibidores del apetito de la familia de las anfetaminas (dietilpropión, fenproporex, mazindol), permitiendoque sólo la sibutramina fuese mantenida en el mercado. La decisión ha sido revocada en 2014 por el Congreso Nacional, que autorizó la comercialización de los inhibidores del apetito derivados de la anfetamina.En este artículo se analiza la construcción del sentido del riesgo en periódicos diarios durante la coberturade la controversia relativa a esos fármacos, en los dos momentos antagónicos. Basado en la teoría de losdiscursos sociales, se analizaron 25 noticias de los años 2011 y 2014, que mostraron que el discurso delriesgo ha sido infravalorado por la cobertura política que privilegia los conflictos de intereses, así como lasdisputas con la autoridad sanitaria, y las contradicciones del proceso.


Subject(s)
Humans , Anti-Obesity Agents/pharmacology , Appetite Depressants , Health Communication , Journalism , Obesity/prevention & control , Appetite Depressants/adverse effects , Brazil , Pharmaceutical Trade , Risk Factors
3.
Braz. j. med. biol. res ; 50(1): e5630, 2017. tab, graf
Article in English | LILACS | ID: biblio-839244

ABSTRACT

Previous studies have reported on the glucose and lipid-lowering effects of ferulic acid (FA) but its anti-obesity potential has not yet been firmly established. This study investigated the possible anti-obesitogenic effects of FA in mice fed a high-fat diet (HFD) for 15 weeks. To assess the antiobesity potential of FA, 32 male Swiss mice, weighing 20–25 g (n=6–8 per group) were fed a normal diet (ND) or HFD, treated orally or not with either FA (10 mg/kg) or sibutramine (10 mg/kg) for 15 weeks and at the end of this period, the body weights of animals, visceral fat accumulation, plasma levels of glucose and insulin hormone, amylase and lipase activities, the satiety hormones ghrelin and leptin, and tumor necrosis factor-α (TNF-α) and monocyte chemoattractant protein-1 (MCH-1) were analyzed. Results revealed that FA could effectively suppress the HFD-associated increase in visceral fat accumulation, adipocyte size and body weight gain, similar to sibutramine, the positive control. FA also significantly (P<0.05) decreased the HFD-induced elevations in serum lipid profiles, amylase and lipase activities, and the levels of blood glucose and insulin hormone. The markedly elevated leptin and decreased ghrelin levels seen in HFD-fed control mice were significantly (P<0.05) reversed by FA treatment, almost reaching the values seen in ND-fed mice. Furthermore, FA demonstrated significant (P<0.05) inhibition of serum levels of inflammatory mediators TNF-α, and MCH-1. These results suggest that FA could be beneficial in lowering the risk of HFD-induced obesity via modulation of enzymatic, hormonal and inflammatory responses.


Subject(s)
Animals , Male , Mice , Anti-Obesity Agents/pharmacology , Coumaric Acids/pharmacology , Cyclobutanes/pharmacology , Intra-Abdominal Fat/drug effects , Obesity/drug therapy , Adipose Tissue/pathology , Diet, High-Fat , Disease Models, Animal , Obesity/pathology
4.
Rio de Janeiro; s.n; 2013. 124 p. ilus, tab.
Thesis in Portuguese | LILACS | ID: lil-719619

ABSTRACT

O extrato aquoso de erva-mate, obtido a partir de folhas secas de Ilex paraguariensis, é uma bebida amplamente consumida na América do Sul. Inicialmente, nosso objetivo foi caracterizar os compostos presentes nas amostras de erva-mate disponíveis no mercado brasileiro (CH: chimarrão; T: chá mate torrado; G: chá mate torrado, comercialmente acondicionado em garrafas ou C: em copos; TS: chá mate torrado solúvel A mutagenicidade, citotoxicidade e antimutagenicidade de todas as amostras também foram avaliadas atavés do Teste de Ames na presença e na ausência de ativação metabólica. Em seguida, analisamos a amostra TS (2,5, 5,0 e 10 mg/mL) quanto a sua atividade antioxidante e antigenotóxica. Além disso, avaliamos também os efeitos da amostra TS sobre a sinalização da leptina e da insulina no hipotálamo e o estresse oxidativo hepático de ratos adultos obesos programados pela superalimentação neonatal (S). Para induzir S, o tamanho da ninhada foi reduzido a três filhotes por lactante e as ninhadas com número padrão de filhotes (dez/lactante) foram utilizadas como controle. Aos 150 dias de vida, as proles S foram subdivididas em: TS - tratados com extrato aquoso de erva-mate (1g/kg de peso corporal/dia, por gavagem) e S - recebendo água por gavagem durante 30 dias. A prole controle (C) também recebeu água nas mesmas condições do grupo S. Em nossos resultados, verificamos a presença de ácido clorogênico, cafeína e teobromina em todas as amostras analisadas. O conteúdo de compostos fenólicos nas infusões estudadas foram CH: 5,14±0,23; T: 4,33±0,01; G: 0,93±0,25; C: 0,80±0,3 e TS: 8,35±0,5 mg/ml. Não observamos efeito mutagênico ou citotóxico nas amostras analisadas. Um efeito antimutagênico significativo foi observado para a cepa TA97 (pré-, co- e pós-tratamento), na presença de ativação metabólica, em todas as amostras testadas. A amostra TS também apresentou um efeito antimutagênico significativo para a TA102 (pré-, co-e e pós-tratamento)...


Yerba mate extract, made from dried leaves of Ilex paraguariensis, is a tea-like beverage consumed in South America. Here, we aim, firstly, to characterize the compounds present in yerba mate beverages available in the Brazilian market (chimarrao –CH; mate tea –T; mate tea commercially packed in bottles –B and cups ready-to-drink –C; and roasted yerba mate soluble tea –TS). We also evaluated its mutagenic, cytotoxic and antimutagenic properties through Ames test in the presence and absence of metabolic activation. Then, we analyzed exclusively TS sample (2.5, 5.0 and 10 mg/mL) as its antioxidant activity, on plasmid DNA cleavages and upon epithelial esophagus primary culture of Wistar rats treated with a genotoxic agent. Futhermore, we evaluated the effects of mate tea (TS) upon the hypothalamic changes of leptin and insulin signaling and hepatic oxidative stress in postnatal early overfeeding (S) rats. To induce S, litter size was reduced to three pups per dam and normal litters (ten pups/dam) were used as control. In postnatal day (PN) 150, S offspring were subdivided into: S and TS groups treated, respectively, with water or mate tea (1g/kg BW/day, by gavage) during 30 days. C offspring received water. Our results showed the presence of chlorogenic acid, caffeine and theobromine in all analyzed samples. The contents of phenolic compounds in the studied infusions were CH:5,14±0,23; T:4,33±0,01; B:0,93±0,25; C:0,80±0,3 and TS:8,35±0,5 mg/mL. No mutagenic or cytotoxic effect was observed for all analyzed samples. A significant antimutagenic effect was observed for S.typhimurium TA97 (CoT, PreT and PosT), in the presence of metabolic activation, for all tested samples. TS sample also exhibited a significant antimutagenic effect for S.typhimurium TA102 (CoT, PreT and PosT) in the presence of metabolic activation. We did not observed an antimutagenic effect using TA98, TA100 and TA102 for CH, T, C and B samples; and no effect for TA98 and TA100 for TS sample...


Subject(s)
Animals , Rats , Antimutagenic Agents/pharmacology , Antioxidants/pharmacology , Anti-Obesity Agents/pharmacology , Ilex paraguariensis/physiology , Ilex paraguariensis/chemistry , DNA Damage , Oxidative Stress , Plant Extracts/pharmacology , Liver , Overnutrition/chemically induced , Obesity/drug therapy , Mutagenicity Tests/methods
5.
Experimental & Molecular Medicine ; : 603-614, 2012.
Article in English | WPRIM | ID: wpr-14962

ABSTRACT

Higher levels of body fat are associated with an increased risk for development numerous adverse health conditions. FTY720 is an immune modulator and a synthetic analogue of sphingosine 1-phosphate (S1P), activated S1P receptors and is effective in experimental models of transplantation and autoimmunity. Whereas immune modulation by FTY720 has been extensively studied, other actions of FTY720 are not well understood. Here we describe a novel role of FTY720 in the prevention of obesity, involving the regulation of adipogenesis and lipolysis in vivo and in vitro. Male C57B/6J mice were fed a standard diet or a high fat diet (HFD) without or with FTY720 (0.04 mg/kg, twice a week) for 6 weeks. The HFD induced an accumulation of large adipocytes, down-regulation of phosphorylated AMP-activated protein kinase alpha (p-AMPKalpha) and Akt (p-Akt); down-regulation of hormone-sensitive lipase (HSL), adipose triglyceride lipase (ATGL) and perilipin mRNA as well as up-regulation of phosphorylated HSL (p-HSL, Ser563) and glycogen synthase kinase 3 alpha/beta (p-GSK3alpha/beta). All these effects were blunted by FTY720 treatment, which inhibited adipogenesis and promoted lipolysis. Also, FTY720 significantly decreased lipid accumulation in maturing preadipocytes. FTY720 down-regulated the transcriptional levels of the PPARgamma, C/EBPalpha and adiponectin, which are markers of adipogenic differentiation. FTY720 significantly increased the release of glycerol and the expression of the HSL, ATGL and perilipin, which are regulators of lipolysis. These results show that FTY720 prevented obesity by modulating adipogenesis and lipolysis, and suggest that FTY720 is used for the treatment of obesity.


Subject(s)
Animals , Male , Mice , 3T3-L1 Cells , AMP-Activated Protein Kinases/metabolism , Adipocytes/drug effects , Adipogenesis/drug effects , Anti-Obesity Agents/pharmacology , Antigens, Differentiation/genetics , Carrier Proteins/genetics , Cell Size , Diet, High-Fat/adverse effects , Disease Models, Animal , Enzyme Activation , Gene Expression Regulation, Enzymologic/drug effects , Glycogen Synthase Kinase 3/genetics , Lipase/genetics , Lipolysis/drug effects , Mice, Inbred C57BL , Obesity/etiology , Phosphoproteins/genetics , Phosphorylation , Propylene Glycols/pharmacology , Protein Processing, Post-Translational , Proto-Oncogene Proteins c-akt/metabolism , Sphingosine/analogs & derivatives , Sterol Esterase/metabolism
6.
Nutrire Rev. Soc. Bras. Aliment. Nutr ; 36(2)ago. 2011. graf, ilus, tab
Article in Portuguese | LILACS | ID: lil-604945

ABSTRACT

Anti-obesity drugs such as mazindol and beta-phenylethylamine derivatives induce their therapeutic effects by inhibiting noradrenaline and dopamine reuptake. In the hypothalamus, noradrenaline and dopamine play an important role in the control of appetite. Sibutramine reduces food intake due to a mechanism of action discretely distinct from beta-phenylethylamine products. In fact, this drug also decreases serotonin reuptake, which is a neurotransmitter quite related to satiety. Rimonabant was considered anovelty on the treatment of obesity, mainly due to its quite new mechanism of action, which is based on the blockade of CB1 receptors. Thus, considering a recent increase in the consumption of such anti-obesity drugs, this study aimed to perform a systematic review about the safety of these drugs. Based on literature, this study concluded that beta-phenylethylaminic drugs and mazindol show many side effects, mainly due to the activation of the sympathetic system (i.e. cardiovascular and gastrointestinal effects, and also central side effects, such as anxiety, and insomnia). Despite sibutramine is well tolerated by patients, clinical studies show that this drugis able to evoke similar sympathetic central and peripheral effects. Regarding rimonabant, the clinical use of this drug was linked to an increase in the incidence of major depression. In conclusion, despite most of the side effects evoked by anti-obesity drugs are classified as of low to moderate intensity, physicians must be aware of such effects upon prescription. In addition, they have to pay attention to the contraindications of such anti-obesity drugs in order to avoid health complications.


Los fármacos antiobesidad tales como el mazindoly los derivados de la beta-feniletilamina actúan inhibiendo la recaptación de la noradrenalinay de la dopamina, neurotransmisores que en el hipotálamo desenvuelven papel importante en el control del apetito. La sibutramina presenta mecanismo de acción discretamente diferente porque disminuye también la recaptación deserotonina, lo cual es positivo porque la activación del sistema serotoninérgico provoca saciedad. El rimonabanto surgió como una novedad para el tratamiento de la obesidad debido a su mecanismo de acción por medio del bloqueo de receptores cannabinoides CB1. Así, considerando el uso creciente y indiscriminado de moduladores del apetito este estudio tiene como principal objetivo realizar una revisión sistemática de la literatura sobre los efectos adversos de estos fármacos. De acuerdo con la literatura, este estudio concluyó que los fármacos beta-feniletilamínicos y el mazindol provocan varios efectos adversos derivados dela activación del sistema simpático, como sonlos efectos gastrointestinales y cardiovasculares, además de algunos efectos secundarios centrales, tales como ansiedad e insomnio. A pesar de la sibutramina ser mejor tolerada por los pacientes, los estudios clínicos muestran que este fármaco es responsable de varios efectos centrales y periféricos simpáticos. Con relación al rimonabanto, a pesar de la expectativa en relación a su mecanismo de acción innovador, su uso clínico demostró efectos adversos graves, como una depresión mayor. Enconclusión, aun cuando la mayor parte de los efectos secundarios provocados por los fármacos anti-obesidad fueron clasificados como de bajao moderada intensidad, los médicos deben estar conscientes de tales efectos secundarios en el momento de la prescripción de un fármaco anorexígeno. Además, deben estar atentos a las contra indicaciones de los tratamientos para la obesidad, a fin de evitar complicaciones mayores.


Fármacos anorexígenos como o mazindole os derivados da beta-feniletilamina ageminibindo a recaptação de noradrenalina edopamina, cujos neuro transmissores estão envolvidos em nível hipotalâmico no controle do apetite. A sibutramina possui mecanismo de ação ligeiramente diverso, pois também inibe a recaptação de serotonina, sendo um ponto positivo, visto que a ativação do sistema serotoninérgico promove a saciedade. O rimonabanto despontou como uma novidade no tratamento da obesidade, graças ao seu mecanismo de ação baseado no bloqueio de receptores canabinoides CB1. Considerando o uso crescente e indiscriminado de moduladores do apetite, o presente estudo visa fazer uma revisão sistemática da literatura sobre os efeitos adversos e as contraindicações do uso desses fármacos. Com base na literatura, este estudo concluiu que os fármacos beta-feniletilamínicos e o mazindol apresentam muitos efeitos adversos decorrentes da ativação do sistema simpático, como distúrbios gastrintestinais e cardiovasculares, além de alguns efeitos centrais, como ansiedade e insônia. Apesar de a sibutramina ser mais bem tolerada, os estudos clínicos mostram que este fármaco é também responsável por sintomas relacionados à ativação simpática periférica e a estimulação do sistema nervoso central. O rimonabanto, apesar das expectativas com relação ao seu mecanismo de ação inovador, mostrou efeitos adversos graves, como depressão maior. Em conclusão, muito embora os efeitos adversos fossem considerados de intensidade leve ou moderada, o médico precisa ter em mente tais situações no momento da prescrição de um fármaco anorexígeno. Além disso, deve estaratento às contraindicações dos tratamentos para obesidade, a fim de evitar maiores complicações.


Subject(s)
Appetite Depressants/analysis , Appetite Depressants/adverse effects , Appetite Depressants/pharmacology , Amphetamines/adverse effects , Anti-Obesity Agents/adverse effects , Anti-Obesity Agents/pharmacology , Obesity , Synaptic Transmission
7.
Arq. bras. endocrinol. metab ; 54(4): 375-380, jun. 2010. ilus, graf
Article in English | LILACS | ID: lil-550707

ABSTRACT

INTRODUSTION: Sibutramine has been described as a drug recommended for treatment of obesity, since it has the ability to inhibit the reuptake of serotonin and noradrenaline in the central nervous system, thereby increasing energy expenditure. OBJECTIVE: Investigate the anxiogenic and anxiolytic effects of acute and chronic treatment with sibutramine in rats submitted to the task of the elevated plus-maze. METHODS: Diazepam was used as a positive control for the anxiolytic effect, and the task of the elevated plus-maze showed sensitivity to detect the effect. In the chronic treatment, sibutramine was ingested for a period of two months. RESULTS: The acute and chronic treatments at the studied dose, which is described to produce a maximum effect of anti-obesity in rats, did not interfere with anxiety. CONCLUSIONS: The acute and chronic administration of sibutramine is not related to anxiolytic or anxiogenic effects.


INTRODUÇÃO: A sibutramina tem sido descrita como um fármaco recomendado para o tratamento da obesidade, uma vez que tem a capacidade de inibir a recaptação de serotonina e noradrenalina no sistema nervoso central, aumentando assim o gasto energético. OBJETIVO: Investigar os efeitos ansiogênico e ansiolítico dos tratamentos agudo e crônico com a sibutramina em ratos Wistar submetidos à tarefa do labirinto em cruz elevado. MÉTODOS: O diazepam foi usado como controle positivo para o efeito ansiolítico, e a tarefa do labirinto em cruz elevado apresentou sensibilidade para detectar o efeito. No tratamento crônico, a sibutramina foi ingerida por um período de dois meses. RESULTADOS: Os tratamentos agudo e crônico, na dose estudada, que é descrita para produzir um efeito de antiobesidade máxima em ratos, não interferem na ansiedade. CONCLUSÕES: As administrações aguda e crônica de sibutramina não estão relacionadas aos efeitos ansiolítico ou ansiogênico.


Subject(s)
Animals , Male , Rats , Anti-Anxiety Agents/pharmacology , Anti-Obesity Agents/pharmacology , Anxiety/drug therapy , Cyclobutanes/pharmacology , Analysis of Variance , Anti-Anxiety Agents/adverse effects , Anti-Obesity Agents/adverse effects , Body Weight/drug effects , Disease Models, Animal , Maze Learning/drug effects , Motor Activity/drug effects , Random Allocation , Rats, Wistar
8.
Arq. bras. endocrinol. metab ; 53(2): 271-280, Mar. 2009. ilus
Article in English | LILACS | ID: lil-513782

ABSTRACT

Central obesity have an important impact on the development of risk factors for coronary heart disease, including dislipidemia, glucose intolerance, insulin resistance and hypertension. These factors contribute to building cardiovascular (CV) disease as a major cause of death. The approach to obesity therapy should be designed to reduce CV risk and mortality. Diet and lifestyle changes remain the cornerstones of therapy for obesity, but the resultant weight loss is often small and long-term success is uncommon and disappointing. Drug therapy is considered for individuals with a body mass index greater than 30 kg/m² or ranging from 25 to 30 kg/m² if they have comorbid conditions. Antiobesity agents can be helpful to some patients in achieving and maintaining meaningful weight loss, but yet our pharmaceutical tools are of limited effectiveness considering the magnitude of the problem. At the present, only two drugs, orlistat and sibutramine, are approved for long-term treatment of obesity and promote no more than 5 to 10 percent of weight loss. Rimonabant, a cannabinoid-1 receptor antagonist, was withdrawn from the market because of concerns about its safety, including risk of suicidal and seizures, although very effective in promoting clinically meaningful weight loss, reduction in waist circumference, and improvements in several metabolic risk factors, rimonabant, a cannabinoid-1 receptor antagonist was withdrawn from the market because it concerns about its safety, including risk of suicidal and seizures. Fortunately, recent fundamental insights into the neuroendocrine mechanisms regulating body weight provide an expanding list of molecular targets for novel, rationally designed antiobesity drugs. In this review, the therapeutic potential of some antiobesity molecules in the development will be analyzed based on an understanding of energy homeostasis.


Obesidade e, particularmente, a obesidade central têm influência importante na predisposição a fatores de risco para doença coronariana, incluindo dislipidemia, intolerância à glicose, resistência à insulina e hipertensão. Tais fatores contribuem para tornar as doenças cardiovasculares (DC) causas frequentes de morte. Os métodos de tratamento da obesidade deveriam ser voltados à redução do risco e da mortalidade devido às doenças cardiovasculares. Dietas e mudanças no estilo de vida continuam sendo fatores-chave no tratamento à obesidade, mas a perda de peso resultante é geralmente pequena e o sucesso em longo prazo costuma ser incomum e frustrante. O tratamento com medicamentos é indicado para indivíduos com índice de massa corpórea superior a 30 kg/m² ou entre 25 e 30 kg/m², se apresentarem comorbidades. Agentes antiobesidade podem ajudar alguns pacientes a alcançar e manter uma perda de peso significativa, mas, ainda assim, os agentes farmacológicos são pouco efetivos considerando-se a magnitude do problema. Atualmente, apenas duas drogas, orlistat e sibutramina, são consideradas efetivas para tratamentos em longo prazo, promovendo não mais do que 5 por cento a 10 por cento de perda de peso. Embora seja muito eficaz ao promover perda de peso significativa do ponto de vista clínico, redução da circunferência da cintura e melhora no perfil metabólico, o rimonabanto, um antagonista do receptor canabinoide 1, foi retirado do mercado por fatores relacionados à segurança, incluindo a ocorrência de suicídios e convulsões. Felizmente, conhecimentos fundamentais recentes sobre mecanismos neuroendócrinos que regulam o peso corporal forneceram uma lista considerável de alvos moleculares para novas drogas antiobesidade produzidas racionalmente. Nesta revisão de literatura, a eficácia terapêutica de algumas moléculas antiobesidade será analisada com base no entendimento da homeostase energética.


Subject(s)
Animals , Humans , Anti-Obesity Agents/therapeutic use , Obesity/drug therapy , Weight Loss , Anti-Obesity Agents/pharmacology , Eating/physiology , Energy Metabolism/drug effects , Energy Metabolism/physiology , Homeostasis/drug effects , Homeostasis/physiology , Neuropeptides/physiology , Obesity/metabolism
9.
Journal of Veterinary Science ; : 189-195, 2009.
Article in English | WPRIM | ID: wpr-151427

ABSTRACT

This study was to investigate the anti-obesity effects of diglyceride (DG)-conjugated linoleic acid (CLA) containing 22% CLA as fatty acids in C57BL/6J ob/ob male mice. There were four experimental groups including vehicle control, DG, CLA, and DG-CLA. The test solutions of 750 mg/kg dose were orally administered to the mice everyday for 5 weeks. CLA treatments significantly decreased mean body weight in the obese mice throughout the experimental period compared to the control (p < 0.01). All test solutions significantly decreased the levels of triglyceride, glucose and free fatty acids in the serum compared with control (p < 0.05). The levels of total cholesterol were also significantly reduced in DG and DG-CLA groups compared with the control group (p < 0.05). CLA significantly decreased weights of renal and epididymal fats compared with the control (p < 0.05). DG and DG-CLA also significantly decreased the epididymal fat weights compared with the control (p < 0.05). A remarkable decrease in the number of lipid droplets and fat globules was observed in the livers of mice treated with DG, CLA, and DG-CLA compared to control. Treatments of DG and CLA actually increased the expression of peroxisome proliferator-activated receptor gamma. These results suggest that DG-CLA containing 22% CLA have a respectable anti-obesity effect by controlling serum lipids and fat metabolism.


Subject(s)
Animals , Male , Mice , Adipose Tissue/drug effects , Anti-Obesity Agents/pharmacology , Blood Chemical Analysis , Body Weight/drug effects , Diglycerides/pharmacology , Disease Models, Animal , Eating/drug effects , Gene Expression Regulation/drug effects , Linoleic Acids, Conjugated/pharmacology , Lipids/blood , Liver/drug effects , Mice, Inbred C57BL , Mice, Obese , Obesity/metabolism , PPAR gamma/metabolism , Time Factors
10.
Arq. bras. endocrinol. metab ; 50(2): 368-376, abr. 2006. ilus, tab
Article in English, Portuguese | LILACS, SES-SP | ID: lil-435164

ABSTRACT

Weight loss improves metabolic abnormalities and reduces cardiovascular risk in obese hypertensive patients. To evaluate the impact of a sustained weight loss on coronary risk, 181 hypertensive patients with metabolic syndrome underwent to orlistat therapy, 120 mg, t.i.d., plus diet for 36 weeks. During therapy, Framingham risk scores (FRS) were calculated for determination of coronary heart disease risk in ten years. Body mass index decreased from 35.0 ± 4.2 to 32.6 ± 4.5 kg/m² (p< 0.0001) and waist circumference from 108.1 ± 10.1 to 100.5 ± 11.1 cm (p< 0.0001), at the end of the study period (week 36). Systolic and diastolic blood pressure showed reductions after the two first weeks, which were maintained up to the end of the study. A clear shift to the left in FRS distribution curve occurred at the end of the study, compared to baseline, indicating a reduction in coronary risk. Over all patients at risk, 49.2 percent moved to a lower risk category. A weight loss > 5 percent occurred in 64.6 percent of all patients, associated with improvement in glucose metabolism. Among those with abnormal glucose metabolism, 38 out 53 patients (71.7 percent) improved their glucose tolerance (p< 0.0005). In conclusion, long-term orlistat therapy helps to reduce and maintain a lower body weight, decreasing risk of coronary disease and improving glucose metabolism, thus protecting against type 2 diabetes.


A perda de peso melhora as anormalidades metabólicas e reduz o risco cardiovascular em pacientes obesos hipertensos. Com o objetivo de avaliar o impacto da perda de peso mantida sobre o risco coronariano, submetemos 181 pacientes hipertensos com síndrome metabólica à terapia com orlistat, 120 mg, três vezes ao dia, mais dieta, por um período de 36 semanas. Durante a terapia, foram calculados os scores de risco de Framingham (FRS) para a determinação do risco de doença cardíaca coronariana em dez anos. Ao final do período de estudo (semana 36), o índice de massa corpóreo diminuiu de 35,0 ± 4,2 para 32,6 ± 4,5 kg/m² (p< 0,0001) e a circunferência da cintura de 108,1 ± 10,1 para 100,5 ± 11,1 cm (p< 0,0001). As pressões sistólica e diastólica mostraram reduções após as primeiras duas semanas, que se mantiveram até o final do estudo. Um deslocamento evidente para a esquerda na curva de distribuição do FRS ocorreu no final do estudo, em comparação com os valores basais, indicando redução no risco coronariano. Do total de pacientes em risco, 49,2 por cento passou para uma categoria de risco menor. Ocorreu perda de peso > 5 por cento em 64,6 por cento de todos os pacientes, associada com melhora no metabolismo da glicose. Entre os 53 pacientes com metabolismo de glicose anormal, 38 (71,7 por cento) melhoraram sua tolerância à glicose (p< 0,0005). Em conclusão, terapia de longa duração com orlistat auxilia a reduzir e manter mais baixo o peso corpóreo, reduzindo o risco de doença coronária e melhorando o metabolismo da glicose e protegendo, dessa maneira, contra o diabetes tipo 2.


Subject(s)
Humans , Male , Female , Middle Aged , Anti-Obesity Agents/therapeutic use , Lactones/therapeutic use , Obesity/drug therapy , Weight Loss/drug effects , Anti-Obesity Agents/pharmacology , Blood Pressure , Body Mass Index , Follow-Up Studies , Hypertension/complications , Lactones/pharmacology , Metabolic Syndrome , Obesity/diet therapy , Waist-Hip Ratio
11.
Experimental & Molecular Medicine ; : 162-172, 2006.
Article in English | WPRIM | ID: wpr-15695

ABSTRACT

People with upper body or visceral obesity have a much higher risk of morbidity and mortality from obesity-related metabolic disorders than those with lower body obesity. In an attempt to develop therapeutic strategies targeting visceral obesity, depot- specific differences in the expression of genes in omental and subcutaneous adipose tissues were investigated by DNA array technology, and their roles in adipocyte differentiation were further examined. We found that levels of metallothionein-II (MT-II) mRNA and protein expression were higher in omental than in subcutaneous adipose tissues. The study demonstrates that MT-II may play an important role in adipocyte differentiation of 3T3L1 preadipocytes, and that N-acetylcysteine (NAC) inhibits the adipocyte differentiation of 3T3L1 cells by repressing MT-II in a time- and dose-dependent manner. Furthermore, the intraperitoneal administration of NAC to rats and mice resulted in a reduction of body weights, and a marked reduction in visceral fat tissues. These results suggest that MT-II plays important roles in adipogenesis, and that NAC may be useful as an anti-obesity drug or supplement.


Subject(s)
Rats , Middle Aged , Mice , Male , Humans , Female , Animals , Aged , Viscera/drug effects , Time Factors , Subcutaneous Fat/drug effects , Rats, Sprague-Dawley , Mice, Inbred C57BL , Metallothionein/genetics , Down-Regulation/drug effects , Dose-Response Relationship, Drug , Cell Differentiation/drug effects , Body Weight/drug effects , Anti-Obesity Agents/pharmacology , Adipose Tissue/cytology , Adipocytes/cytology , Acetylcysteine/pharmacology , 3T3-L1 Cells
12.
Journal of Korean Medical Science ; : 1-6, 2005.
Article in English | WPRIM | ID: wpr-196858

ABSTRACT

This study aimed to evaluate current clinical assessments and management of obesity in the primary care setting in Korea since anti-obesity agents have become available. A questionnaire was sent to eligible primary care physicians selected from a national probability sample in two specialties: family physicians and internists. Of 939 randomly selected physicians, 452 (48.1%) replied. We found that 51.8% of physicians were aware of the definition of obesity, and 33.8% were aware of the definition of abdominal obesity proposed by Asia-Pacific guideline. When evaluating apparently obese patients, 50.0% of respondents measured body mass index (BMI) and 20.4% measured waist circumference. Fewer than 50% of physicians measured blood glucose or lipid profiles, both of which are risk factors for obesity. About 47.3% of physicians prescribed an anti-obesity medication without allowing sufficient time for nonpharmacologic therapy to take effect, and 68.8% of physicians prescribed anti-obesity medications to patients that requested them regardless of obesity status. The majority of respondents did not appropriately evaluate obesity and its risk factors, and were readily susceptible to prescribing anti-obesity medications. Our findings suggest that primary care physicians in Korea need additional education on obesity and its management.


Subject(s)
Adult , Female , Humans , Male , Middle Aged , Age Factors , Anti-Obesity Agents/pharmacology , Blood Glucose/metabolism , Body Mass Index , Family Practice/methods , Health Knowledge, Attitudes, Practice , Korea , Lipids/metabolism , Obesity/metabolism , Practice Patterns, Physicians' , Physicians, Family , Surveys and Questionnaires , Risk Factors , Weight Loss
13.
Medicina (B.Aires) ; 64(4): 332-336, 2004. tab, graf
Article in English | LILACS | ID: lil-401070

ABSTRACT

Rats endocriadas de la línea IIMBeta con obesidad, hipertriacilglicerolemia y diabetes espontáneas fueron tratadas con oleoil-estrona durante 10 días. Un grupo con restricción alimentaria fue incluido en el estudio a fin de aislar algunos efectos de la oleoil-estrona dependientes de la restricción calórica que ésta promueve. Veinticinco ratas Beta macho de 200 dias de edad a los que se suministró 0.2 ml de aceite de girasol por día se dividieron en los seguientes grupos: (1) dosis diaria de 10 nmol/g de oleoil-estrona ; (2) restringido; (3) control. Las variables medidas fueron: proteínas corporales totales, agua y lípidios; pesos de los panículos adiposos retroperitoneal y epididimario; urea, glucosa, insulina, colesterol y triacilgliceroles plasmáticos. Los valores de biomasa y de ingesta de alimentos se registraron diariamente. Los grupos tratados con oleoil-estrona y restringido mostraron variaciones similares en composicíon corporal y disminuciones significativas en peso corporal debidas a reducciones en la ingesta de alimentos. Los tratamientos con oleoil-estrona y restringido disminuyeron significamente los pesos de los panículos adiposos retroperitoneales, pero no de los epididimarios. En los grupos tratados con oleoil-estrona y restringido la hiperglicemia disminuyó y la insulinemia lo hizo en forma significativa. Los valores de colesterol total plasmático normal y la hipertriacilglicerolemia característicos de las ratas Beta disminuyeron fuertemente comparados con los controles, aunque alcanzaron valores significa-tivamente diferentes entre los grupos tratados con oleoil-estrona y restringido. El colesterol total plasmático aparece como más sensible a la restricción calórica que los traicilgliceroles a través de un efecto específico mediado por la oleoil-estrona.


Subject(s)
Animals , Male , Rats , Anti-Obesity Agents/pharmacology , Caloric Restriction , Diabetes Mellitus, Type 2 , Estrone/pharmacology , Obesity/metabolism , Oleic Acids/pharmacology , Anti-Obesity Agents/therapeutic use , Body Weight/drug effects , Cholesterol/metabolism , Diabetes Mellitus, Type 2 , Eating , Estrone/therapeutic use , Obesity/drug therapy , Oleic Acids/therapeutic use , Rats, Inbred Strains , Triglycerides/metabolism , Weight Loss/drug effects
14.
Indian J Exp Biol ; 2001 Jun; 39(6): 551-7
Article in English | IMSEAR | ID: sea-58696

ABSTRACT

Effect of administration of different doses (0.25, 0.5, 1 and 2 g/kg, twice daily, po) of a polyherbal preparation, OB-200G and fluoxetine (10 mg/kg, ip) for 21 days was studied on food intake and body weight in male and female Laka mice. The study further investigated the effect of administration of 0.5 g/kg dose of OB-200G for 40 days on body weight, fat pad weights, locomotor activity and biochemical parameters in monosodium glutamate (MSG)-treated male and female Wistar rat pups. Administration of OB-200G produced dose dependent decrease in body weight in both male and female mice. On the other hand, fluoxetine decreased body weight only in female mice. The food intake was significantly (P < 0.05) increased in both fasted male and female mice after treatment with the lower dose (0.25 g/kg, po) of OB-200G. However, significant (P < 0.05) decrease in food intake was recorded with the administration of higher doses (0.5, 1 and 2 g/kg, po) of OB-200G and fluoxetine in fasted female mice on day 1, 7, 14 and 21. But in male mice differential effect on food intake was recorded at different doses on day 1, 7, 14 and 21. Further, OB-200G administration significantly (P < 0.05) decreased body weight and fat pad weights, increased serum glucose levels and ambulatory activity in MSG-treated female rats but not in MSG-treated male rats. The results suggest that OB-200G involves gender differences in mediating its antiobesity effect and may supplement the current armamentarium for the treatment of obesity.


Subject(s)
Adipose Tissue/drug effects , Animals , Anti-Obesity Agents/pharmacology , Body Weight/drug effects , Feeding Behavior/drug effects , Fluoxetine/pharmacology , Male , Mice , Motor Activity/drug effects , Plant Extracts/pharmacology , Rats , Rats, Wistar , Sodium Glutamate/administration & dosage
16.
Rev. chil. obes ; 5(1): 10-9, 2000. tab, graf
Article in Spanish | LILACS | ID: lil-274577

ABSTRACT

Sibutramine is a drug that recently been accepted for its use in obesity: Here we shall review its actions and its role in the pharmacologic therapy of obesity, its indications and interactions. We shall also see the associations sibutamine has with the patologies most frecuently associated with obesity


Subject(s)
Humans , Anti-Obesity Agents/classification , Obesity/drug therapy , Uric Acid/analysis , Anti-Obesity Agents/pharmacology , Cardiovascular System/drug effects , Diabetes Mellitus/drug therapy , Hypertension/drug therapy
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