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1.
Biomed Pharmacother ; 141: 111838, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34182414

RESUMO

Obesity is known as metabolic syndrome and it affects many tissues including adipose tissue, liver, and central nervous system (CVS). Gambi-jung (GBJ) is a modified prescription of Taeumjowi-tang (TJT), which has been used to treat obesity in Korea. GBJ is composed of 90% Ephedra sinica Stapf (ES). Therefore, the present study was designed to assess the antiobesity effects of GBJ and to compare the effects of GBJ and ES on obesity. GBJ administration remarkably reduced the body weight, Body mass index (BMI), and body fat percentage compared to the ES administration in human subjects. GBJ-treated mice had lower white adipose tissue (WAT) amounts than ES-treated mice. GBJ and ES administration enhanced adenosine monophosphate-activated protein kinase (AMPK) expression in 3T3-L1 adipocytes, epididymal WAT and liver of HFD-induced obese mice. Moreover, GBJ and ES reduced food intake by suppressing the mRNA levels of orexigenic peptides, agouti-related protein (AgRP) and neuropeptide-Y (NPY), as well as AMPK in the brain of HFD-induced obese mice. Furthermore, GBJ-treated mice had dramatically lower expression of macrophage marker F4/80 in epididymal WAT than those of ES-treated mice. Based on these results, we suggest the use of GBJ as a natural drug to control weight gain.


Assuntos
Fármacos Antiobesidade/uso terapêutico , Obesidade/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Células 3T3-L1 , Tecido Adiposo Branco/efeitos dos fármacos , Adulto , Idoso , Animais , Depressores do Apetite/química , Depressores do Apetite/farmacologia , Composição Corporal/efeitos dos fármacos , Índice de Massa Corporal , Ingestão de Alimentos/efeitos dos fármacos , Ephedra sinica/química , Efedrina/química , Efedrina/farmacologia , Feminino , Humanos , Sistema de Sinalização das MAP Quinases , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Pessoa de Meia-Idade , Redução de Peso/efeitos dos fármacos
2.
Sci Rep ; 11(1): 6791, 2021 03 24.
Artigo em Inglês | MEDLINE | ID: mdl-33762661

RESUMO

To examine the effect of a Caralluma Fimbriata extract (CFE) on biomarkers of satiety and body composition in overweight adults. A double-blind, randomised, placebo controlled trial to examine the effect of a Caralluma Fimbriata extract (CFE) on biomarkers of satiety and body composition in overweight adults. Eighty-three men and women aged between 20 and 50 years of age completed 16 weeks of daily supplementation with either CFE or placebo. Plasma cardiometabolic (lipid profile, glucose, insulin) and satiety (ghrelin, leptin, neuropeptideY) biomarkers, body composition, diet history and gastrointenstinal function were assessed at baseline, weeks 4, 8, 12 and 16. Subjects in the CFE and placebo groups were well matched and predominatly female 93% and 87.5%, with a mean age of 40.9 ± 6.7 and 39.5 ± 7.5 years and body mass index (BMI) of 30.0 ± 3.1 and 30.2 ± 2.9 kg/m2 respectively. There was a significant difference in plasma leptin concentration change between groups at week 16 (p = 0.04), with the placebo group increasing concentration (2.27 ± 4.80 ng/mL) while the CFE group (0.05 ± 4.69 ng/mL) remained the same. At week 16, the CFE group had significantly reduced their calorie intake from baseline compared to the placebo group (245 cal vs 15.8 cal respectively p < 0.01). The CFE group also had a significant reduction in waist circumference of 2.7 cm compared to an increase of 0.3 cm in the placebo group (p = 0.02). A weight increase from baseline was seen in the placebo group that was not observed in the CFE group (1.33 kg weight gain vs 0.37 kg weight loss respectively; p = 0.03). The placebo group also had a significant increase in fat mass, android fat mass, BMI and leptin compared to the CFE group (p = 0.04, 0.02, < 0.01 respectively). CFE was effective at maintaining bodyweight during a non-calorie controlled diet compared to a placebo. The mechanism responsible for this action is requiring further research and could be due to an increase in satiety receptor sensitivity.


Assuntos
Apocynaceae/química , Depressores do Apetite/uso terapêutico , Regulação do Apetite/efeitos dos fármacos , Sobrepeso/dietoterapia , Extratos Vegetais/farmacologia , Administração Oral , Adulto , Apocynaceae/metabolismo , Depressores do Apetite/química , Depressores do Apetite/farmacologia , Biomarcadores/sangue , Índice de Massa Corporal , Método Duplo-Cego , Ingestão de Energia/efeitos dos fármacos , Humanos , Leptina/sangue , Pessoa de Meia-Idade , Sobrepeso/patologia , Efeito Placebo , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Circunferência da Cintura/efeitos dos fármacos , Adulto Jovem
3.
Mini Rev Med Chem ; 21(6): 724-730, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33245271

RESUMO

Fenugreek (Trigonella foenum-graecum L.) is a native plant found in the parts of Iran to the North of India, and is presently planted also in other regions of the world. Fenugreek is considered a notable multipurpose medicinal and traditional herb in Iran, India, and China for several centuries. The most important components of fenugreek seeds are protein, neutral detergent fiber, gum, lipids, moisture, ash and starch. Fenugreek seeds and leaves are anti-cholesterolemic, anti-tumor, antiinflammatory, carminative, demulcent, deobstruent, emollient, expectorant, galactogogue, febrifuge, laxative, hypoglycaemic, restorative, parasiticide and uterine tonic and useful in burning sensation. Traditionally, fenugreek seeds being used worldwide are beneficial for bone and muscles, respiratory system, gastro-intestinal system, female reproductive system, cardio-vascular system, endocrinology and hepatic. Fenugreek helps reduce cholesterol, reduce cardiovascular risk, control diabetes, a good consolation for sore throats, a remedy for acid reflux, constipation, colon cancer prevention, appropriate for kidney trouble, skin infection, increase milk production, reduce menstrual discomfort, and reduce menopause symptoms. It is also an appetite suppressant that helps in weight loss. Both modern science and traditional medicine integration with novel technologies and discoveries will secure the cultivation of medicinal herbs and promote sustainability in the long-term and a wide-range.


Assuntos
Medicina Tradicional/história , Extratos Vegetais/química , Trigonella/química , Depressores do Apetite/química , Depressores do Apetite/isolamento & purificação , Depressores do Apetite/farmacologia , Doenças Cardiovasculares/prevenção & controle , História Antiga , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Sementes/química , Sementes/metabolismo , Trigonella/metabolismo , Redução de Peso/efeitos dos fármacos
4.
Forensic Sci Int ; 286: 199-207, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29602147

RESUMO

A novel sibutramine analogue was detected in a slimming formula by high performance liquid chromatography with a photo diode detector array (HPLC-PDA). The unknown compound exhibited an ultraviolet (UV) spectrum that was similar to that of chlorosibutramine, despite having a different HPLC retention time. Further analysis of the slimming formula by LC-quadrupole time-of-flight mass spectrometry (LC-Q-TOF/MS) showed that the unknown compound had the formula C18H27Cl2N. To elucidate the structure of this new sibutramine analogue, the target compound in the slimming formula was isolated on a preparative-LC system equipped with a PDA. After analysis by fourier transform infrared (FT-IR) and nuclear magnetic resonance (NMR) spectroscopy, the unknown compound was identified as a sibutramine analogue in which the iso-butyl group on the side chain is replaced with an iso-pentyl group. This new sibutramine analogue was identified to be 1-(1-(3,4-dichlorophenyl)cyclobutyl)-N,N,4-trimethylpentan-1-amine and has been named as chlorosipentramine.


Assuntos
Depressores do Apetite/química , Ciclobutanos/química , Suplementos Nutricionais , Cromatografia Líquida de Alta Pressão/métodos , Contaminação de Medicamentos , Humanos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas/métodos , Estrutura Molecular , Espectroscopia de Infravermelho com Transformada de Fourier
5.
J Sci Food Agric ; 98(4): 1554-1565, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-28816350

RESUMO

BACKGROUND: Thylakoids, a chloroplast membrane extracted from green leaves, are a promising functional ingredient with appetite-reducing properties via their lipase-inhibiting effect. Thylakoids in powder form have been evaluated in animal and human models, but no comprehensive study has been conducted on powder characteristics. The aim was to investigate the effects of different isolation methods and drying techniques (drum-drying, spray-drying, freeze-drying) on thylakoids' physicochemical and functional properties. RESULTS: Freeze-drying yielded thylakoid powders with the highest lipase-inhibiting capacity. We hypothesize that the specific macromolecular structures involved in lipase inhibition were degraded to different degrees by exposure to heat during spray-drying and drum-drying. We identified lightness (Hunter's L-value), greenness (Hunter's a-value), chlorophyll content and emulsifying capacity to be correlated to lipase-inhibiting capacity. Thus, to optimize the thylakoids functional properties, the internal membrane structure indicated by retained green colour should be preserved. This opens possibilities to use chlorophyll content as a marker for thylakoid functionality in screening processes during process optimization. CONCLUSION: Thylakoids are heat sensitive, and a mild drying technique should be used in industrial production. Strong links between physicochemical parameters and lipase inhibition capacity were found that can be used to predict functionality. The approach from this study can be applied towards production of standardized high-quality functional food ingredients. © 2017 Society of Chemical Industry.


Assuntos
Depressores do Apetite/química , Dessecação/métodos , Liofilização/métodos , Extratos Vegetais/química , Folhas de Planta/química , Spinacia oleracea/química , Tilacoides/química , Depressores do Apetite/isolamento & purificação , Clorofila/química , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Lipase/antagonistas & inibidores , Lipase/química , Extratos Vegetais/isolamento & purificação , Pós/química
6.
Food Chem Toxicol ; 108(Pt A): 63-73, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28713048

RESUMO

Caralluma fimbriata Wall. is currently used as a "natural slimming" food supplement, likely due to its content in pregnane glycosides. In the present study, a commercially available Caralluma fimbriata extract (Slimaluma®; CFE, 100 mg/kg) has been evaluated for its ability to affect the ingestive behaviour in female rats, also with reference to the modulation of the brain neuropeptides NPY and ORX.The interference of CFE with α-amylase and lipase enzymes has been investigated in vitro, as possible peripheral mechanism of action. Also, the chemical composition of CFE has been assessed by NMR and spectrophotometric analysis. Results from in vivo study showed that CFE induced effects neither on blood parameters, nor on liver and gut histomorphology. Interestingly, a reduction in body weight gain with an increase in water intake and hypothalamic levels of NPY and ORX peptides were found. Phytochemical analysis, showed CFE contained about 12% of pregnane glycosides and 1.3% of polyphenols. Present results suggest possible effects of C. fimbriata on ingestive behaviour, likely mediated by central and peripheral mechanisms.


Assuntos
Apocynaceae/química , Depressores do Apetite/farmacologia , Comportamento Alimentar/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Animais , Depressores do Apetite/química , Ingestão de Alimentos/efeitos dos fármacos , Feminino , Compostos Fitoquímicos/química , Extratos Vegetais/química , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley
7.
J Biochem Mol Toxicol ; 31(6)2017 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-28186389

RESUMO

Corticosterone plays an important role in feeding behavior. However, its mechanism remains unclear. Therefore, the present study aimed to investigate the effect of corticosterone on feeding behavior. In this study, cumulative food intake was increased by acute corticosterone administration in a dose-dependent manner. Administration of the 5-HT2c receptor agonist m-chlorophenylpiperazin (mCPP) reversed the effect of corticosterone on food intake. The anorectic effects of mCPP were also blocked by the 5-HT2c receptor antagonist RS102221 in corticosterone-treated mice. Both corticosterone and mCPP increased c-Fos expression in hypothalamic nuclei, but not the nucleus of the solitary tract. RS102221 inhibited c-Fos expression induced by mCPP, but not corticosterone. In addition, mCPP had little effect on TH and POMC levels in the hypothalamus. Furthermore, mCPP antagonized decreasing effect of the leptin produced by corticosterone. Taken together, our findings suggest that 5-HT2c receptors and leptin may be involved in the effects of corticosterone-induced hyperphagia.


Assuntos
Regulação do Apetite/efeitos dos fármacos , Corticosterona/farmacologia , Hipotálamo/efeitos dos fármacos , Leptina/agonistas , Proteínas do Tecido Nervoso/metabolismo , Neurônios/efeitos dos fármacos , Receptor 5-HT2C de Serotonina/metabolismo , Animais , Depressores do Apetite/química , Depressores do Apetite/farmacologia , Estimulantes do Apetite/administração & dosagem , Estimulantes do Apetite/agonistas , Estimulantes do Apetite/antagonistas & inibidores , Estimulantes do Apetite/farmacologia , Comportamento Animal/efeitos dos fármacos , Corticosterona/administração & dosagem , Corticosterona/agonistas , Corticosterona/antagonistas & inibidores , Relação Dose-Resposta a Droga , Ingestão de Energia/efeitos dos fármacos , Hiperfagia/sangue , Hiperfagia/induzido quimicamente , Hiperfagia/metabolismo , Hiperfagia/patologia , Hipotálamo/metabolismo , Hipotálamo/patologia , Leptina/antagonistas & inibidores , Leptina/sangue , Leptina/metabolismo , Camundongos Endogâmicos ICR , Proteínas do Tecido Nervoso/agonistas , Proteínas do Tecido Nervoso/antagonistas & inibidores , Proteínas do Tecido Nervoso/genética , Neurônios/metabolismo , Neurônios/patologia , Especificidade de Órgãos , Piperazinas/antagonistas & inibidores , Piperazinas/farmacologia , Proteínas Proto-Oncogênicas c-fos/agonistas , Proteínas Proto-Oncogênicas c-fos/genética , Proteínas Proto-Oncogênicas c-fos/metabolismo , Receptor 5-HT2C de Serotonina/química , Agonistas do Receptor 5-HT2 de Serotonina/farmacologia , Antagonistas do Receptor 5-HT2 de Serotonina/farmacologia , Compostos de Espiro/farmacologia , Sulfonamidas/farmacologia , Regulação para Cima/efeitos dos fármacos
8.
Artigo em Inglês | MEDLINE | ID: mdl-27092588

RESUMO

In 2013 the Dutch authorities issued a warning against a dietary supplement that was linked to 11 reported adverse reactions, including heart problems and in one case even a cardiac arrest. In the UK a 20-year-old woman, said to have overdosed on this supplement, died. Since according to the label the product was a herbal mixture, initial LC-MS/MS analysis focused on the detection of plant toxins. Yohimbe alkaloids, which are not allowed to be present in herbal preparations according to Dutch legislation, were found at relatively high levels (400-900 mg kg(-1)). However, their presence did not explain the adverse health effects reported. Based on these effects the supplement was screened for the presence of a ß-agonist, using three different biosensor assays, i.e. the validated competitive radioligand ß2-adrenergic receptor binding assay, a validated ß-agonists ELISA and a newly developed multiplex microsphere (bead)-based ß-agonist assay with imaging detection (MAGPIX(®)). The high responses obtained in these three biosensors suggested strongly the presence of a ß-agonist. Inspection of the label indicated the presence of N-isopropyloctopamine. A pure standard of this compound was bought and shown to have a strong activity in the three biosensor assays. Analysis by LC-full-scan high-resolution MS confirmed the presence of this 'unknown known' ß3-agonist N-isopropyloctopamine, reported to lead to heart problems at high doses. A confirmatory quantitative analysis revealed that one dose of the preparation resulted in an intake of 40-60 mg, which is within the therapeutic range of this compound. The case shows the strength of combining bioassays with chemical analytical techniques for identification of illegal pharmacologically active substances in food supplements.


Assuntos
Agonistas de Receptores Adrenérgicos beta 3/intoxicação , Antipirina/análogos & derivados , Depressores do Apetite/efeitos adversos , Suplementos Nutricionais/efeitos adversos , Contaminação de Alimentos , Cardiopatias/etiologia , Preparações de Plantas/efeitos adversos , Agonistas de Receptores Adrenérgicos beta 3/análise , Alcaloides/análise , Alcaloides/toxicidade , Anabolizantes/efeitos adversos , Anabolizantes/química , Anabolizantes/intoxicação , Anabolizantes/normas , Antipirina/análise , Antipirina/intoxicação , Depressores do Apetite/química , Depressores do Apetite/intoxicação , Depressores do Apetite/normas , Técnicas Biossensoriais , Suplementos Nutricionais/análise , Suplementos Nutricionais/intoxicação , Suplementos Nutricionais/normas , Inspeção de Alimentos , Rotulagem de Alimentos , Doenças Transmitidas por Alimentos/etiologia , Doenças Transmitidas por Alimentos/mortalidade , Doenças Transmitidas por Alimentos/terapia , Cardiopatias/mortalidade , Cardiopatias/terapia , Hospitalização , Humanos , Internet , Países Baixos , Nootrópicos/efeitos adversos , Nootrópicos/química , Nootrópicos/intoxicação , Nootrópicos/normas , Pausinystalia/efeitos adversos , Pausinystalia/química , Substâncias para Melhoria do Desempenho/efeitos adversos , Substâncias para Melhoria do Desempenho/química , Substâncias para Melhoria do Desempenho/intoxicação , Substâncias para Melhoria do Desempenho/normas , Preparações de Plantas/química , Preparações de Plantas/intoxicação , Preparações de Plantas/normas
9.
Endocrinology ; 157(1): 233-44, 2016 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-26492472

RESUMO

Body weight loss of Lep(ob/ob) mice in response to leptin is larger than expected from the reduction in energy intake alone, suggesting a thermogenic action of unknown magnitude. We exploited the superior pharmacological properties of a novel long-acting leptin prepared via PASylation to study the contribution of its anorexigenic and thermogenic effects. PASylation, the genetic fusion of leptin with a conformationally disordered polypeptide comprising 600 Pro/Ala/Ser (PAS) residues, provides a superior way to increase the hydrodynamic volume of the fusion protein, thus retarding kidney filtration and extending plasma half-life. Here a single PAS(600)-leptin injection (300 pmol/g) resulted in a maximal weight reduction of 21% 6 days after application. The negative energy balance of 300 kJ/(4 d) was driven by a decrease in energy intake, whereas energy expenditure remained stable. Mice that were food restricted to the same extent showed an energy deficit of only 220 kJ/(4 d) owing to recurring torpor bouts. Therefore, the anorexigenic effect of PAS(600)-leptin contributes 75% to weight loss, whereas the thermogenic action accounts for 25% by preventing hypometabolism. In a second experiment, just four injections of PAS(600)-leptin (100 pmol/g) administered in 5- to 6-day intervals rectified the Lep(ob/ob) phenotype. In total, 16 nmol of PAS(600)-leptin per mouse triggered a weight loss of 43% within 20 days and normalized hypothermia and glucose homeostasis as well as hepatic steatosis. The beneficial properties of PAS(600)-leptin are substantiated by a comparison with previous studies in which approximately 400 nmol (∼25-fold) unmodified leptin was mandatory to achieve similar improvements.


Assuntos
Depressores do Apetite/uso terapêutico , Metabolismo Energético/efeitos dos fármacos , Leptina/análogos & derivados , Obesidade/tratamento farmacológico , Proteínas Recombinantes de Fusão/uso terapêutico , Resposta de Saciedade/efeitos dos fármacos , Motivos de Aminoácidos , Animais , Depressores do Apetite/administração & dosagem , Depressores do Apetite/efeitos adversos , Depressores do Apetite/química , Relação Dose-Resposta a Droga , Ingestão de Energia/efeitos dos fármacos , Feminino , Hipotálamo/efeitos dos fármacos , Hipotálamo/metabolismo , Hipotálamo/patologia , Injeções Subcutâneas , Leptina/administração & dosagem , Leptina/genética , Leptina/uso terapêutico , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Masculino , Camundongos Mutantes , Peso Molecular , Atividade Motora/efeitos dos fármacos , Obesidade/metabolismo , Obesidade/patologia , Peptídeos/metabolismo , Proteínas Recombinantes de Fusão/administração & dosagem , Proteínas Recombinantes de Fusão/efeitos adversos , Proteínas Recombinantes de Fusão/química , Organismos Livres de Patógenos Específicos , Termogênese/efeitos dos fármacos , Redução de Peso/efeitos dos fármacos
10.
Nutr Res ; 35(5): 393-400, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-25823991

RESUMO

We hypothesized that a digestion-resistant maltodextrin, Fibersol-2 (Archer Daniels Midland/Matsutani LLC, Decatur, IL, USA) may impact satiety by decreasing hunger, prolonging satiation, and/or increasing peripheral satiety signals. In a randomized, double-blind, placebo-controlled crossover study, healthy subjects (9 men and 10 women) underwent 3 treatments in which they consumed a standardized meal with a tea containing 0, 5, or 10 g of Fibersol-2. A visual analog scale questionnaire was given in 30-minute intervals to measure subjective appetite and satiety. Blood was drawn just before the meal (time 0) and at 30, 60, 90, 120, 180, and 240 minutes after meal for measurements of plasma ghrelin, cholecystokinin, gastrin, peptide YY, gastric inhibitory polypeptide, and glucagon-like peptide-1, all by enzyme-linked immunosorbent assay. There were significant delays in hunger and increased satiety for 1.5 to 2 hours after treatment with 10 g of Fibersol-2. These delays did not occur after ingesting 0 or 5 g Fibersol-2 at any time. Control and 5 g Fibersol-2 treatments did not suppress increases in hunger postmeal; hunger scores increased and satiety scores decreased significantly (P < .05) at all time points relative to the first postmeal assessment. Plasma peptide YY and glucagon-like peptide-1 were significantly increased by the ingestion of meal with tea containing 10 g Fibersol-2 compared with 0 or 5 g Fibersol-2 (P < .05). This study demonstrated that 10 g Fibersol-2 with a meal stimulated production of satiety hormones and enhanced satiety.


Assuntos
Depressores do Apetite/uso terapêutico , Peptídeo 1 Semelhante ao Glucagon/agonistas , Sobrepeso/dietoterapia , Peptídeo YY/agonistas , Polissacarídeos/uso terapêutico , Prebióticos , Resposta de Saciedade , Adulto , Depressores do Apetite/administração & dosagem , Depressores do Apetite/química , Índice de Massa Corporal , Estudos Cross-Over , Método Duplo-Cego , Células Enteroendócrinas/metabolismo , Feminino , Peptídeo 1 Semelhante ao Glucagon/sangue , Peptídeo 1 Semelhante ao Glucagon/metabolismo , Humanos , Almoço , Masculino , Pessoa de Meia-Idade , Sobrepeso/sangue , Sobrepeso/metabolismo , Peptídeo YY/sangue , Peptídeo YY/metabolismo , Polissacarídeos/administração & dosagem , Polissacarídeos/química , Prebióticos/administração & dosagem , Solubilidade , Chá , Viscosidade , Adulto Jovem
11.
J Ethnopharmacol ; 160: 78-85, 2015 Feb 03.
Artigo em Inglês | MEDLINE | ID: mdl-25435289

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: To understand the role of khat (Catha edulis) use on the aberrations in appetite and weight which are common comorbidities for khat and other amphetamine users. MATERIALS AND METHODS: We provide a comprehensive overview and conceptual summary of the historical cultural use of khat as a natural stimulant and describe the similarities and differences between cathinone (the main psychoactive constituent of khat) and amphetamine highlighting the limited literature on the neurophysiology of appetite and subsequent weight effects of khat. RESULTS: Animal and some human studies indicate that khat produces appetite suppression, although little is known about mechanisms of this effect. Both direct and indirect effects of khat stem from multiple factors including behavioral, chemical and neurophysiological effects on appetite and metabolism. Classic and newly identified appetite hormones have not been explored sufficiently in the study of appetite and khat use. Unique methodological challenges and opportunities are encountered when examining effects of khat and cathinone including khat-specific medical comorbidities, unique route of administration, differential patterns of behavioral effects relative to amphetamines and the nascent state of our understanding of the neurobiology of this drug. CONCLUSION: A considerable amount of work remains in the study of the appetite effects of khat chewing and outline a program of research that could inform our understanding of this natural amphetamine׳s appetite effects and help prepare health care workers for the unique health effects of this drug.


Assuntos
Alcaloides/farmacologia , Anfetamina/farmacologia , Depressores do Apetite/farmacologia , Apetite/efeitos dos fármacos , Catha , Extratos Vegetais/farmacologia , Caules de Planta , Animais , Depressores do Apetite/química , Humanos
12.
Artigo em Inglês | MEDLINE | ID: mdl-24499058

RESUMO

Because of the rapid growth in dietary supplement availability and public concern for weight control, the investigation of foods and various dietary supplements illegally adulterated with weight loss compounds has become increasingly important. A total of 29 weight loss compounds, including sennoside, sibutramine, ephedrine and their analogues, found to be adulterated in foods and dietary supplements were simultaneously examined by LC-MS/MS. The 188 samples were collected between 2009 and 2012 in South Korea, and method validation was performed to determine the adulterants to the weight loss compounds. LODs, LOQs and linearity ranged from 0.03 to 7.5 ng ml⁻¹, from 0.08 to 30.00 ng ml⁻¹, and from 0.990 to 0.999, respectively. The results showed that nine weight loss compounds, namely bisacodyl, desmethylsibutramine, didesmethylsibutramine, ephedrine, fluoxetine, pseudoephedrine, sennoside A, sennoside B and sibutramine, were detected in 62 of all collected samples and were found in order of frequency as follows: sibutramine, 25.7%; sennoside A, 22.9%; sennoside B, 20.0%; fluoxetine, 8.6%; desmethylsibutramine, 7.1%; bisacodyl, ephedrine, and pseudoephedrine, 4.3%; and didesmethylsibutramine, 2.9%. Sibutramine, which was the most frequently found adulterant, ranged in levels from 0.03 to 132.40 mg g⁻¹ (2010), from 0.88 to 76.2 mg g⁻¹ (2011), and from 0.07 to 0.24 mg g⁻¹ (2012). Although the concentrations of most compounds ranged widely, some compounds such as bisacodyl and fluoxetine were found at high concentrations in several samples.


Assuntos
Fármacos Antiobesidade/análise , Suplementos Nutricionais/análise , Contaminação de Alimentos , Inspeção de Alimentos/métodos , Alimentos em Conserva/análise , Fármacos Antiobesidade/química , Depressores do Apetite/análise , Depressores do Apetite/química , Catárticos/análise , Catárticos/química , Estimulantes do Sistema Nervoso Central/análise , Estimulantes do Sistema Nervoso Central/química , Cromatografia Líquida de Alta Pressão , Ciclobutanos/análise , Ciclobutanos/química , Suplementos Nutricionais/economia , Alimentos em Conserva/economia , Limite de Detecção , Reprodutibilidade dos Testes , República da Coreia , Extrato de Senna/análise , Extrato de Senna/química , Senosídeos , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas em Tandem
13.
Phytochemistry ; 93: 144-53, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23602053

RESUMO

In the search for plant alternatives to Hoodia gordonii containing P57, a pregnane glycoside with potential appetite suppressant effect, the roots of Cynanchum auriculatum were investigated. As a result, 15 pregnane glycosides including nine never previously reported were isolated. Their structures were elucidated on the basis of extensive spectroscopic analyses and chemical methods. Appetite suppressant effect and body weight loss were observed when tested with the most abundant pregnane glycoside, wilfoside K1N, in an in vivo test with rats.


Assuntos
Depressores do Apetite/farmacologia , Cynanchum/química , Glicosídeos/farmacologia , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Pregnanos/farmacologia , Redução de Peso/efeitos dos fármacos , Animais , Depressores do Apetite/química , Depressores do Apetite/isolamento & purificação , Feminino , Glicosídeos/química , Glicosídeos/isolamento & purificação , Conformação Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Pregnanos/química , Pregnanos/isolamento & purificação , Ratos , Ratos Wistar
14.
Br J Nutr ; 109(7): 1330-7, 2013 Apr 14.
Artigo em Inglês | MEDLINE | ID: mdl-22850326

RESUMO

The objective was to determine the effects of dietary fibre with bulking, viscous and gel-forming properties on satiation, and to identify the underlying mechanisms. We conducted a randomised crossover study with 121 men and women. Subjects were healthy, non-restrained eaters, aged 18-50 years and with normal BMI (18.5-25 kg/m²). Test products were cookies containing either: no added fibre (control), cellulose (bulking, 5 g/100 g), guar gum (viscous, 1.25 g/100 g and 2.5 g/100 g) or alginate (gel forming, 2.5 g/100 g and 5 g/100 g). Physico-chemical properties of the test products were confirmed in simulated upper gastrointestinal conditions. In a cinema setting, ad libitum intake of the test products was measured concurrently with oral exposure time per cookie by video recording. In a separate study with ten subjects, 4 h gastric emptying rate of a fixed amount of test products was assessed by ¹³C breath tests. Ad libitum energy intake was 22 % lower for the product with 5 g/100 g alginate (3.1 (sd 1.6) MJ) compared to control (4.0 (sd 2.2) MJ, P< 0.001). Intake of the other four products did not differ from control. Oral exposure time for the product with 5 g/100 g alginate (2.3 (sd 1.9) min) was 48 % longer than for control (1.6 (sd 0.9) min, P= 0.01). Gastric emptying of the 5 g/100 g alginate product was faster compared to control (P< 0.05). We concluded that the addition of 5 g/100 g alginate (i.e. gel-forming fibre) to a low-fibre cookie results in earlier satiation. This effect might be due to an increased oral exposure time.


Assuntos
Depressores do Apetite/metabolismo , Fibras na Dieta/metabolismo , Alimentos Fortificados , Trato Gastrointestinal/metabolismo , Resposta de Saciedade , Adolescente , Adulto , Alginatos/química , Alginatos/metabolismo , Depressores do Apetite/química , Celulose/química , Celulose/metabolismo , Estudos Cross-Over , Fibras na Dieta/análise , Feminino , Alimentos Fortificados/análise , Galactanos/química , Galactanos/metabolismo , Esvaziamento Gástrico , Géis , Ácido Glucurônico/química , Ácido Glucurônico/metabolismo , Ácidos Hexurônicos/química , Ácidos Hexurônicos/metabolismo , Humanos , Masculino , Mananas/química , Mananas/metabolismo , Pessoa de Meia-Idade , Países Baixos , Gomas Vegetais/química , Gomas Vegetais/metabolismo , Método Simples-Cego , Inquéritos e Questionários , Viscosidade , Adulto Jovem
15.
Eur J Nutr ; 52(3): 1015-27, 2013 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22752262

RESUMO

PURPOSE: Dietary sesamin (1:1 mixture of sesamin and episesamin) decreases fatty acid synthesis but increases fatty acid oxidation in rat liver. Dietary α-lipoic acid lowers hepatic fatty acid synthesis. These changes can account for the serum lipid-lowering effect of sesamin and α-lipoic acid. It is expected that the combination of these compounds in the diet potentially ameliorates lipid metabolism more than the individual compounds. We therefore studied the combined effect of sesamin and α-lipoic acid on lipid metabolism in rats. METHODS: Male Sprague-Dawley rats were fed diets supplemented with 0 or 2 g/kg sesamin and containing 0 or 2.5 g/kg α-lipoic acid for 22 days. RESULTS AND CONCLUSIONS: Sesamin and α-lipoic acid decreased serum lipid concentrations and the combination of these compounds further decreased the parameters in an additive fashion. These compounds reduced the hepatic concentration of triacylglycerol, the lignan being less effective in decreasing this value. The combination failed to cause a stronger decrease in hepatic triacylglycerol concentration. The combination of sesamin and α-lipoic acid decreased the activity and mRNA levels of hepatic lipogenic enzymes in an additive fashion. Sesamin strongly increased the parameters of hepatic fatty acid oxidation enzymes. α-Lipoic acid antagonized the stimulating effect of sesamin of fatty acid oxidation through reductions in the activity of some fatty acid oxidation enzymes and carnitine concentration in the liver. This may account for the failure to observe strong reductions in hepatic triacylglycerol concentration in rats given a diet containing both sesamin and α-lipoic acid.


Assuntos
Suplementos Nutricionais , Dioxóis/administração & dosagem , Regulação Enzimológica da Expressão Gênica , Hipolipemiantes/administração & dosagem , Lignanas/administração & dosagem , Metabolismo dos Lipídeos , Fígado/metabolismo , Ácido Tióctico/administração & dosagem , Animais , Depressores do Apetite/administração & dosagem , Depressores do Apetite/química , Carnitina/antagonistas & inibidores , Carnitina/metabolismo , Dioxóis/antagonistas & inibidores , Ácidos Graxos/sangue , Ácidos Graxos/metabolismo , Hipolipemiantes/antagonistas & inibidores , Lignanas/antagonistas & inibidores , Lipogênese , Lipólise , Fígado/enzimologia , Fígado/crescimento & desenvolvimento , Masculino , Tamanho do Órgão , RNA Mensageiro/metabolismo , Ratos , Ratos Sprague-Dawley , Ácido Tióctico/antagonistas & inibidores , Triglicerídeos/sangue , Triglicerídeos/metabolismo , Aumento de Peso
16.
Artigo em Inglês | MEDLINE | ID: mdl-22784191

RESUMO

Desorption corona beam ionisation (DCBI), the relatively novel ambient mass spectrometry (MS) technique, was utilised to screen for illicit additives in weight-loss food. The five usually abused chemicals - fenfluramine, N-di-desmethyl sibutramine, N-mono-desmethyl sibutramine, sibutramine and phenolphthalein - were detected with the proposed DCBI-MS method. Fast single-sample and high-throughput analysis was demonstrated. Semi-quantification was accomplished based on peak areas in the ion chromatograms. Four illicit additives were identified and semi-quantified in commercial samples. As there was no tedious sample pre-treatment compared with conventional HPLC methods, high-throughput analysis was achieved with DCBI. The results proved that DCBI-MS is a powerful tool for the rapid screening of illicit additives in weight-loss dietary supplements.


Assuntos
Fármacos Antiobesidade/química , Suplementos Nutricionais/análise , Contaminação de Alimentos , Inspeção de Alimentos/métodos , Depressores do Apetite/análise , Depressores do Apetite/química , China , Cromatografia Líquida de Alta Pressão , Ciclobutanos/análise , Ciclobutanos/química , Fenfluramina/análise , Fenfluramina/química , Indicadores e Reagentes/análise , Indicadores e Reagentes/química , Legislação sobre Alimentos , Espectrometria de Massas , Fenolftaleína/análise , Fenolftaleína/química , Reprodutibilidade dos Testes , Inibidores Seletivos de Recaptação de Serotonina/análise , Inibidores Seletivos de Recaptação de Serotonina/química
17.
Chem Commun (Camb) ; 48(69): 8679-81, 2012 Sep 07.
Artigo em Inglês | MEDLINE | ID: mdl-22825075

RESUMO

Pregnane glycoside P57, the appetite suppressant component from Hoodia, was synthesized expeditiously, featuring preparation of the aglycone Hoodigogenin A from digoxin and assembly of the deoxytrisaccharide with glycosyl o-alkynylbenzoates as donors.


Assuntos
Apocynaceae/química , Depressores do Apetite/síntese química , Extratos Vegetais/síntese química , Saponinas/síntese química , Depressores do Apetite/química , Extratos Vegetais/química , Saponinas/química
18.
Am J Public Health ; 102(9): 1676-86, 2012 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-22813089

RESUMO

The US Food and Drug Administration (FDA) has recently warned consumers about the risks of weight loss supplements adulterated with multiple pharmaceutical agents. Some of these supplements combine potent anorectics, such as amphetamines derivatives, with benzodiazepines, beta-blockers, and other medications to suppress the anorectics' adverse effects. These weight loss supplements represent the most recent generation of rainbow diet pills, named for their bright and varied colors, which date back more than 70 years. Beginning in the 1940s, several US pharmaceutical firms aggressively promoted rainbow pills to physicians and patients. By the 1960s the pills had caused dozens of deaths before the FDA began removing them from the US market. We used a variety of original resources to trace these deadly pills from their origins in the United States to their popularity in Spain and Brazil to their reintroduction to the United States as weight loss dietary supplements.


Assuntos
Anfetaminas/efeitos adversos , Fármacos Antiobesidade/efeitos adversos , Depressores do Apetite/efeitos adversos , Suplementos Nutricionais/efeitos adversos , Contaminação de Medicamentos , Redução de Peso , Anfetaminas/química , Anfetaminas/história , Fármacos Antiobesidade/química , Fármacos Antiobesidade/história , Depressores do Apetite/química , Depressores do Apetite/história , Brasil , Suplementos Nutricionais/história , História do Século XIX , História do Século XX , História do Século XXI , Humanos , Espanha , Estados Unidos
19.
Neuropharmacology ; 63(5): 842-50, 2012 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22732442

RESUMO

Recently, we reported that an initial decrease followed by recovery of food intake was observed during four days of amphetamine (AMPH) treatment and suggested that these changes in response were mediated by changes in neuropeptide Y (NPY) and proopiomelanocortin (POMC). Here we investigated if Y1 receptor (Y1R) and/or Y5 receptor (Y5R) might be involved in this regulation. Rats were treated daily with AMPH for four days. Changes in the expression levels of Y1R, Y5R, melanocortin receptor 3 (MC3R), and NPY were assessed and compared. Results showed that Y1R and MC3R increased, with a maximal increase of about 210% on Day 2 but with a restoration to the normal level on Day 4. In contrast, NPY decreased with a biggest reduction of about 45% on Day 2 and the pattern of expression during AMPH treatment was opposite to those of Y1R and MC3R, while the expression of Y5R was not changed. Central inhibitions of NPY formation or Y1R activity modulated the anorectic response of AMPH and the reciprocal regulation of NPY and MC3R, revealing a crucial role of Y1R in this action. It is suggested that Y1R participates in the reciprocal regulation of NPY- and MC3R-containing neurons in the hypothalamus during the anorectic effect of AMPH. These results may further the understanding of Y1R in the control of eating.


Assuntos
Anfetamina/farmacologia , Depressores do Apetite/farmacologia , Regulação do Apetite/efeitos dos fármacos , Tolerância a Medicamentos , Hipotálamo/efeitos dos fármacos , Neurônios/efeitos dos fármacos , Receptores de Neuropeptídeo Y/metabolismo , Anfetamina/administração & dosagem , Anfetamina/antagonistas & inibidores , Animais , Depressores do Apetite/administração & dosagem , Depressores do Apetite/química , Comportamento Animal/efeitos dos fármacos , Antagonistas de Dopamina/farmacologia , Relação Dose-Resposta a Droga , Ingestão de Alimentos/efeitos dos fármacos , Regulação da Expressão Gênica/efeitos dos fármacos , Haloperidol/farmacologia , Hipotálamo/metabolismo , Masculino , Proteínas do Tecido Nervoso/antagonistas & inibidores , Proteínas do Tecido Nervoso/genética , Proteínas do Tecido Nervoso/metabolismo , Neurônios/metabolismo , Neuropeptídeo Y/antagonistas & inibidores , Neuropeptídeo Y/genética , Neuropeptídeo Y/metabolismo , Oligonucleotídeos Antissenso , Ratos , Ratos Wistar , Receptor Tipo 3 de Melanocortina , Receptores de Melanocortina/metabolismo , Receptores de Neuropeptídeo Y/antagonistas & inibidores
20.
Br J Nutr ; 108(4): 755-8, 2012 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-22313587

RESUMO

Long-chain fatty acids have been shown to suppress appetite and reduce energy intake (EI) by stimulating the release of gastrointestinal hormones such as cholecystokinin (CCK). The effect of NEFA acyl chain length on these parameters is not comprehensively understood. An in vitro screen tested the capacity of individual NEFA (C12 to C22) to trigger CCK release. There was a gradient in CCK release with increasing chain length. DHA (C22) stimulated significantly (P < 0.01) more CCK release than all other NEFA tested. Subsequently, we conducted a randomised, controlled, crossover intervention study using healthy males (n 18). The effects of no treatment (NT) and oral doses of emulsified DHA-rich (DHA) and oleic acid (OA)-rich oils were compared using 24 h EI as the primary endpoint. Participants reported significantly (P = 0.039) lower total daily EI (29 % reduction) with DHA compared to NT. There were no differences between DHA compared to OA and OA compared to NT. There was no between-treatment difference in the time to, or EI of, the first post-intervention eating occasion. It is concluded that NEFA stimulate CCK release in a chain length-dependent manner up to C22. These effects may be extended to the in vivo setting, as a DHA-based emulsion significantly reduced short-term EI.


Assuntos
Depressores do Apetite/metabolismo , Colecistocinina/metabolismo , Suplementos Nutricionais , Ácidos Docosa-Hexaenoicos/metabolismo , Ingestão de Energia , Células Enteroendócrinas/metabolismo , Ácidos Graxos não Esterificados/metabolismo , Adulto , Depressores do Apetite/química , Linhagem Celular Tumoral , Estudos Cross-Over , Ácidos Docosa-Hexaenoicos/química , Emulsões , Ácidos Graxos não Esterificados/química , Humanos , Masculino , Pessoa de Meia-Idade , Peso Molecular , Método Simples-Cego , Adulto Jovem
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