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Introduction and aims: Obesity is a multifactorial condition with high health risk, associated with important chronic disorders such as diabetes, dyslipidemia, and cardiovascular dysfunction. Citrus aurantium L. (C. aurantium) is a medicinal plant, and its active component, synephrine, a ß-3 adrenergic agonist, can be used for weight loss. We investigated the effects of C. aurantium and synephrine in obese adolescent mice programmed by early postnatal overfeeding. Methods: Three days after birth, male Swiss mice were divided into a small litter (SL) group (3 pups) and a normal litter (NL) group (9 pups). At 30 days old, SL and NL mice were treated with C. aurantium standardized to 6% synephrine, C. aurantium with 30% synephrine, isolated synephrine, or vehicle for 19 days. Results: The SL group had a higher body weight than the NL group. Heart rate and blood pressure were not elevated. The SL group had hyperleptinemia and central obesity that were normalized by C. aurantium and synephrine. In brown adipose tissue, the SL group showed a higher lipid droplet sectional area, less nuclei, a reduction in thermogenesis markers related to thermogenesis (UCP-1, PRDM16, PGC-1α and PPARg), and mitochondrial disfunction. C. aurantium and synephrine treatment normalized these parameters. Conclusion: Our data indicates that the treatment with C. aurantium and synephrine could be a promising alternative for the control of some obesity dysfunction, such as improvement of brown adipose tissue dysfunction and leptinemia.

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Background: There are still no studies of the cardiovascular safety of the isolated use of Citrus aurantium in aerobic submaximal exercise. Objective: To evaluate the effect of C. aurantium supplementation on the recovery of cardiorespiratory and autonomic parameters following a session of submaximal aerobic exercise. Methods: Twelve healthy male adults achieved a crossover, randomized, double-blind, and placebo-controlled trial. C. aurantium (600 mg, p-synephrine at 30% amount [180 mg]) or placebo (600 mg of starch) were ingested 90 min before evaluation in randomized days. We evaluated systolic blood pressure (SBP), diastolic blood pressure (DBP), pulse pressure (PP), mean arterial pressure (MAP), heart rate (HR) and, HR variability indexes at Rest and during 60 min of recovery from exercise. Results: Citrus aurantium ingestion accelerated the reduction in SBP after exercise, anticipated the return of vagal modulation of the heart after exercise via the HF (ms2), pNN50 (%), and 2 UV% indices. Moreover, rushed the output of sympathetic modulation after exercise via the 0V% index. No unfavorable cardiovascular effects were achieved for HR, DBP, PP, and MAP parameters. Conclusions: Citrus aurantium was shown to be safe for the cardiovascular and autonomic systems alongside submaximal aerobic exercise in healthy males.

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A LC-MS/MS method for synephrine as a biomarker for orange honey authenticity was developed and validated. The sample was extracted with 5% TCA and cleaned up with Florisil providing 83.7% recoveries. Ions transitions for quantification and identification were 168→135.0 and 168→107.0, respectively. The limits of detection and quantification were 0.66 and 1.0ng/g, respectively. Synephrine was detected in orange honey at levels from 79.2 to 432.2ng/g, but not in other monofloral honeys. It was also present in some wildflower honeys (9.4-236.5ng/g), showing contribution of citrus to this polyfloral honey. Results were confirmed by qualitative pollen analysis. No citrus pollen was detected in honey containing synephrine levels ≤43.8ng/g, suggesting that synephrine in honey is more sensitive compared to pollen analysis. Synephrine was found in citrus but not in other apiculture flowers. Therefore, synephrine is a botanical marker to differentiate and attest authenticity of orange honey.

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ABSTRACT The association of p-synephrine, ephedrine, salicin, and caffeine in dietary supplements and weight loss products is very common worldwide, even though ephedrine has been prohibited in many countries. The aim of this study was to evaluate a 28-day oral exposure toxicity profile of p-synephrine, ephedrine, salicin, and caffeine mixture (10:4:6:80 w/w respectively) in male and female Wistar rats. Body weight and signs of toxicity, morbidity, and mortality were observed daily. After 28 days, animals were euthanized and blood collected for hematological, biochemical, and oxidative stress evaluation. No clinical signs of toxicity, significant weight loss or deaths occurred, nor were there any significant alterations in hematological parameters. Biochemical and oxidative stress biomarkers showed lipid peroxidation, and hepatic and renal damage (p < 0.05; ANOVA/Bonferroni) in male rats (100 and 150 mg/kg) and a reduction (p < 0.05; ANOVA/Bonferroni) in glutathione (GSH) levels in all male groups. Female groups displayed no indications of oxidative stress or biochemical alterations. The different toxicity profile displayed by male and female rats suggests a hormonal influence on mixture effects. Results demonstrated that the tested mixture can alter oxidative status and promote renal and hepatic damages.

RESUMO A associação de p-sinefrina, efedrina, salicina, e cafeína em suplementos alimentares e produtos para perda de peso é muito utilizada em todo o mundo, embora a efedrina tenha sido proibida em muitos países. O objetivo deste estudo foi avaliar o perfil de toxicidade à exposição oral de 28 dias à associação de p-sinefrina, efedrina, salicina e cafeína (na proporção de 10:4:6:80 m/m respectivamente) em ratos Wistar machos e fêmeas. Diariamente, os animais foram observados quanto ao peso corporal, sinais de toxicidade, morbidade e mortalidade. Após 28 dias, os animais foram sacrificados e o sangue coletado para avaliações hematológicas, bioquímicas e de estresse oxidativo. Não se observaram sinais clínicos de toxicidade, tampouco perda significativa de peso, mortes, ou quaisquer alterações significativas nos parâmetros hematológicos. Biomarcadores do estresse oxidativo e bioquímicos mostraram peroxidação lipídica, danos renais e hepáticos (p < 0,05; ANOVA/Bonferroni) em ratos machos (100 e 150 mg/kg) e a redução (p < 0,05; ANOVA/Bonferroni) nos níveis de glutationa reduzida (GSH) em todos os grupos de machos tratados. Nas fêmeas, não houve indícios de estresse oxidativo, nem alterações bioquímicas. O diferente perfil de toxicidade entre os gêneros sugere influência hormonal nos efeitos de mistura administrada. A associação testada pode alterar o estado oxidativo e promover danos renais e hepáticos.

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Atualmente a obesidade tem sido uma doença de grande expansão na população. Dentre as alternativas terapêuticas, o uso de plantas com propriedade termogênica tem sido comumente adotado pela população. A Citrus aurantium L., conhecida como Laranja amarga tem sido uma alternativa para o emagrecimento, porém postula-se que seu uso possa acarretar danos toxicológicos ao fígado, taquicardia e aumento da pressão arterial. Objetivo: avaliar a variação ponderal, o consumo de ração e o perfil bioquímico lipídico. Metodologia: utilizou 20 camundongos suíços, fêmeas e adultas divididas em: Grupo Controle (n=10) tratadas com água e Grupo Laranja (n=10) tratadas com extrato aquoso da Laranja amarga na dosagem diária de 1,2g/dia. A administração foi feita por gavagem durante 30 dias. Ambos os grupos foram submetidos à natação, três vezes por semanas e pesados semanalmente. A ração consumida também foi mensurada diariamente. Após a eutanásia foi feita a coleta de sangue por punção cardíaca para os exames bioquímicos. Resultados: quanto à variação ponderal, os dois grupos apresentaram perda significativa (Grupo Controle: p=0,003/ Grupo Laranja: p=0,027) de peso, o que possivelmente foi proporcionado pela natação e não pelo extrato da planta (diferença entre os grupos controle e laranja não foi significativa, tendo como p=0,308). Não foram evidenciadas alterações no perfil lipídico e no consumo de ração de ambos os grupos. Conclusão: de acordo com os dados obtidos, o extrato aquoso Citrus aurantium L. não mostrou potencial termogênico e não alterou o perfil lipídico dos animais tratados por 30 dias...

Currently obesity has been a disease of great expansion in the population. Among the therapeutic alternatives, the use of plants with thermogenic property has been commonly adopted by population. The Citrus aurantium L., known as bitter orange has been an alternative to weight loss, however it is postulated that its use may cause toxicological liver damage, tachycardia and increased blood pressure. Objective: evaluate the changes in body weight, food intake and lipid biochemical profile. Methodology: 20 swiss mice, females and adults divided into: Control Group (n = 10) treated with water and Orange Group (n = 10) treated with aqueous extract of bitter orange in a daily dosage of 1.2g/day. The administration was by gavage for 30 days. Both groups were submitted to swimming three times per week and weighted weekly. Food consumption was also measured daily. After euthanasia, blood was collected by cardiac puncture for biochemical exams. Results: as for weighted variation, the two groups showed significant loss (Control Group: p = 0.003 / Orange Group: p = 0.027) in weight, which was possibly due to swimming and not by the plant extract (difference between the Control Group and Orange Group was not significant, with p = 0.308). No changes were observed in the lipid profile and food intake in both groups. Conclusion: according to data obtained, the aqueous extract Citrus aurantium L. did not show thermogenic potential and did not affect the lipid profile of the treated animals in 30 days...

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Citrus aurantium (bitter orange) is characterized by the presence of p-synephrine, an amine structurally and pharmacologically related to ephedrine. Besides the same adverse effects as ephedrine, nowadays it is believed that altered levels of p-synephrine can be associated to the occurrence of migraine and cluster headaches. Leaves and fruits of this species are highly commercialized in form of teas and herbal preparations, but without taking into account the risks associated with its use. This work describes a survey of teas and herbal preparations containing C. aurantium, commercialized in Porto Alegre (RS/Brazil), in order to verify the presence of p-synephrine. Comparing with the mean amount available in the supermarkets, around 20 percent of the teas and 10 percent of the herbal preparations declared the presence of C. aurantium in their labels. In a sampling of 15 teas and 2 herbal preparations selected for the analysis, the presence of p-synephrine was characterized in all samples, with levels between 0.0040 to 0.2308 percent, leading to a caution that even being natural products, they are not free of adverse effects.

Citrus aurantium (laranjeira-azeda) é caracterizada pela presença de p-sinefrina, amina estrutural e farmacologicamente similar à efedrina. Além de poder causar efeitos adversos similares aos da efedrina, atualmente acredita-se que níveis endógenos alterados de p-sinefrina possam estar associados à causa da enxaqueca. Folhas e frutos desta espécie são largamente comercializados na forma de chá e em preparados de erva-mate, sem que sejam considerados os riscos associados ao seu uso. Neste sentido, este trabalho descreve uma pesquisa em chás e preparados de erva-mate comercializados em Porto Alegre, para verificar a presença de C. aurantium e p-sinefrina. Comparando com a quantidade média disponível nas prateleiras dos supermercados, cerca de 20 por cento dos chás e 10 por cento dos preparados de erva-mate declaravam nos rótulos conter C. aurantium. De uma amostragem de 15 chás e 2 preparados de erva-mate selecionados para análise, em todos foi caracterizada a presença de p-sinefrina com níveis variando de 0,0040 a 0,2308 por cento, levando ao alerta de que mesmo sendo naturais, estes produtos podem não ser destituídos de reações adversas.

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