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Covering: up to the end of 2022The area of scalemic natural products is often enigmatic from a mechanistic standpoint, since low optical purity is observed in compounds having multiple contiguous stereogenic centers resulting from mechanistically distinct biogenetic steps. A scalemic state is rarely the result of a sloppy enzymatic activity, rather resulting from the expression of antipodal enzymes/directing proteins or from the erosion of optical purity by enzymatic or spontaneous reactions. Evidence for these processes is critically reviewed, identifying the mechanisms most often associated to the enzymatic generation of scalemic natural products and also discussing analytical exploitations of natural products' scalemicity.
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Produtos Biológicos , EstereoisomerismoRESUMO
Bergamot has been traditionally used for the relief of diseases related to oxidative stress. Our aim was to investigate the effect of bergamot phytosome on visceral adipose tissue (VAT) and on metabolic profile, in overweight and obese subjects with mild hypercholesterolemia. A total of 64 participants were randomized into two groups for 12 weeks: a supplemented group (33 individuals, BMI 27 ± 3 kg/m2 receiving 500 mg of bergamot phytosome, two daily tablets) and placebo group (31 subjects, BMI 28 ± 3 kg/m2 , two daily tablets). As to the within differences, the parameters of VAT, total and LDL-cholesterol were significantly decreased in the bergamot phytosome group, but not in the placebo group. As to between-group differences, a statistically significant interaction between time and group, that is, the change in score over time differs between the two groups was observed 30 days after supplementation for VAT (p-value = .005), total cholesterol (p-value <.0002), and LDL (p = .004) in respect to placebo. The other parameters (glucose, insulin, Homeostasis Model Assessment, high-density lipoprotein cholesterol, triglycerides, fat free mass, fat mass) were not significant. In conclusion, this clinical study gives evidence that bergamot phytosome provides beneficial effects, such as decrease of VAT and modulation of metabolic alterations, after just 30 days of supplementation, resulting a very promising protection of cardiovascular health.
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Hipercolesterolemia/tratamento farmacológico , Gordura Intra-Abdominal/efeitos dos fármacos , Metabolismo dos Lipídeos/efeitos dos fármacos , Obesidade/tratamento farmacológico , Sobrepeso/tratamento farmacológico , Óleos de Plantas/uso terapêutico , Adolescente , Adulto , Método Duplo-Cego , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Óleos de Plantas/farmacologia , Adulto JovemRESUMO
Turmeric (Curcuma longa L.) is the only edible plant recognized as a dietary source of curcuminoids, among which curcumin, demethoxycurcumin (DMC) and bis-demethoxycurcumin (Bis-DMC) are the most representative ones. Curcumin shows a very low systemic bioavailability and for this reason, several technologies have been adopted to improve it. These technologies generally improve curcuminoid absorption in the small intestine, however, no data are available about the effect of curcuminoid formulation on colonic biotransformation. The present study aims at investigating the human colonic metabolism of curcuminoids, prepared with two different technologies, using an in vitro model. Unformulated curcuminoid and lecithin-curcuminoid botanical extracts were fermented using an in vitro fecal model and colonic catabolites were identified and quantified by uHPLC-MSn. Native compounds, mainly curcumin, DMC and bis-DMC, were metabolized by colonic microbiota within the 24-h incubation. The degradation of curcuminoids led to the formation of specific curcuminoid metabolites, among which higher concentrations of bis(demethyl)-tetrahydrocurcumin and bis(demethyl)-hexahydrocurcumin were found after lecithin-extract fermentation compared to the concentration detected after unformulated extract. In conclusion, both curcumin-based botanical extracts can be considered important sources of curcuminoids, although the lecithin-formulated extract led to a higher production of curcuminoid catabolites. Moreover, a new curcuminoid catabolite, namely bis(demethyl)-hexahydrocurcumin, has been putatively identified, opening new perspectives in the investigation of curcuminoid bioavailability and their potential metabolite bioactivity.
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Colo/microbiologia , Curcuma/química , Diarileptanoides/metabolismo , Microbioma Gastrointestinal , Diarileptanoides/química , HumanosRESUMO
The scientific literature has demonstrated that glutamine is one of the main beneficial amino acids. It plays an important role in gut microbiota and immunity. This paper provides a critical overview of experimental studies (in vitro, in vivo, and clinical) investigating the efficacy of glutamine and its effect on gut microbiota. As a result of this review, we have summarized that glutamine could affect gut microbiota via different mechanisms including the reduction in the ratio of Firmicutes to Bacteroidetes, with the activation of NF-κB and PI3K-Akt pathways, reducing the intestinal colonization (Eimeria lesions) and bacterial overgrowth or bacterial translocation, increasing the production of secretory immunoglobulin A (SIgA) and immunoglobulin A+ (IgA+) cells in the intestinal lumen, and decreasing asparagine levels. The potential applications of glutamine on gut microbiota include, but are not limited to, the management of obesity, bacterial translocation and community, cytokines profiles, and the management of side effects during post-chemotherapy and constipation periods. Further studies and reviews are needed regarding the effects of glutamine supplementation on other conditions in humans.
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Microbioma Gastrointestinal , Glutamina/metabolismo , Distúrbios Nutricionais/microbiologia , Animais , Dieta , Humanos , Distúrbios Nutricionais/metabolismoRESUMO
This study examined the relationship between TAS2R38 gene polymorphism (RS713598), G/G, C/G or C/C genotype, and sensory responsiveness, food preferences, biochemical parameters and body composition in a cross-sectional study in 118 adults (24 men and 94 women). The frequencies of C/C, G/G and C/G were respectively 20.3%, 29.7% and 50.0%. As regards taste responsiveness, subjects with G-allele had a higher perception threshold than the C/C genotype for 6-n-propyl-2-thiouracil (PROP) (p < .05), and caffeine (p < .05). The G-alleles had higher preferences for beer (OR: 6.25; p < .05), but lower for butter (OR: 0.64; p < .05) and cured meat (OR: 0.55; p < .05). Biochemical parameters and body composition markers did not differ between genotypes. Subjects with RS713598 polymorphism had a higher bitter taste perception threshold and higher or lower preferences for selected nutrient/energy dense foods, such as beer, butter and cured meat.
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Adiposidade , Preferências Alimentares , Predisposição Genética para Doença , Sobrepeso/genética , Polimorfismo de Nucleotídeo Único , Receptores Acoplados a Proteínas G/genética , Limiar Gustativo , Absorciometria de Fóton , Adulto , Substituição de Aminoácidos , Biomarcadores/sangue , Índice de Massa Corporal , Estudos de Coortes , Estudos Transversais , Feminino , Estudos de Associação Genética , Humanos , Itália , Masculino , Pessoa de Meia-Idade , Sobrepeso/sangue , Sobrepeso/diagnóstico por imagem , Sobrepeso/metabolismo , Estudos Prospectivos , Receptores Acoplados a Proteínas G/metabolismo , Adulto JovemRESUMO
BACKGROUND: The aim of this study was to evaluate the performance of Edmonton Frail Scale (EFS) on frailty assessment in association with multi-dimensional conditions assessed with specific screening tools and to explore the prevalence of frailty by gender. METHODS: We enrolled 366 hospitalised patients (women\men: 251\115), mean age 81.5 years. The EFS was given to the patients to evaluate their frailty. Then we collected data concerning cognitive status through Mini-Mental State Examination (MMSE), health status (evaluated with the number of diseases), functional independence (Barthel Index and Activities Daily Living; BI, ADL, IADL), use of drugs (counting of drugs taken every day), Mini Nutritional Assessment (MNA), Geriatric Depression Scale (GDS), Skeletal Muscle Index of sarcopenia (SMI), osteoporosis and functionality (Handgrip strength). RESULTS: According with the EFS, the 19.7% of subjects were classified as non frail, 66.4% as apparently vulnerable and 13.9% with severe frailty. The EFS scores were associated with cognition (MMSE: ß = 0.980; p < 0.01), functional independence (ADL: ß = -0.512; p < 0.00); (IADL: ß = -0.338; p < 0.01); use of medications (ß = 0.110; p < 0.01); nutrition (MNA: ß = -0.413; p < 0.01); mood (GDS: ß = -0.324; p < 0.01); functional performance (Handgrip: ß = -0.114, p < 0.01) (BI: ß = -0.037; p < 0.01), but not with number of comorbidities (ß = 0.108; p = 0.052). In osteoporotic patients versus not-osteoporotic patients the mean EFS score did not differ between groups (women: p = 0.365; men: p = 0.088), whereas in Sarcopenic versus not-Sarcopenic patients, there was a significant differences in women: p < 0.05. CONCLUSIONS: This study suggests that measuring frailty with EFS is helpful and performance tool for stratifying the state of fragility in a group of institutionalized elderly. As matter of facts the EFS has been shown to be associated with several geriatric conditions such independence, drugs assumption, mood, mental, functional and nutritional status.
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Doença Crônica/epidemiologia , Idoso Fragilizado/estatística & dados numéricos , Avaliação Geriátrica/métodos , Atividades Cotidianas , Idoso , Idoso de 80 Anos ou mais , Cognição , Comorbidade , Feminino , Indicadores Básicos de Saúde , Humanos , Itália , Masculino , Estado Nutricional , PrevalênciaRESUMO
A scalable synthesis of 7-hydroxy cannabidiol (7-OH CBD), a primary metabolite of (-)-cannabidiol (CBD), is highly desirable, from an industrial point of view, to enable future clinical trials. A Piers-Rubinsztajn reaction was key to enable a mild deprotection and a concise synthesis of 7-OH CBD from commercially available CBD, in 31% overall yield.
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In this preliminary pilot registry study, we investigated the effects of the oral supplementation of a standardized cranberry extract (Anthocran® Phytosome®, Indena) delivered by a lecithin-based system, for the prophylactic management of recurrent-urinary tract infections (R-UTIs). We included 64 otherwise healthy subjects who underwent a surgical procedure and required post-surgical urinary catheterization for high-risk UTIs or a previous history of R-UTIs. Patients were given supplementation with the standardized cranberry extract at the dose of either 120 mg/day (n = 12) or 240 mg/day (n = 12) or assigned to a control group consisting of standard management (SM; n = 18) or nitrofurantoin administration (n = 22) for 4 weeks. After 4 weeks, patients receiving the standardized cranberry supplementation reported to have a more effective reduction in UTI symptoms, as assessed on the visual analogue scale, compared with patients in the SM or nitrofurantoin groups. The occurrence of hematuria and urine bacterial contamination were decreased among patients treated with the supplement compared with controls (p < 0.05). The cranberry extract was also superior to the control management in terms of recurrence of signs/symptoms, with none of the patients in this group suffering from a R-UTI in the 3 months following the study end (p < 0.05). The supplementation showed an optimal safety profile, with no significant adverse events and no drop-outs in the supplement group. This registry shows that this cranberry extract is effective as a supplementary, preventive management in preventing post-operative, post-catheter UTIs; the product has a good tolerability profile.
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Infecções Urinárias , Vaccinium macrocarpon , Humanos , Fitoterapia/métodos , Fitossomas , Nitrofurantoína/uso terapêutico , Extratos Vegetais/uso terapêutico , Infecções Urinárias/etiologia , Infecções Urinárias/prevenção & controle , Infecções Urinárias/tratamento farmacológico , CateterismoRESUMO
The stability of molecular curcumin (purcumin, 1a) in solution is strongly light-dependent. Under laboratory artificial light, a relative stability is observed only at neutral pH, while more intense light and/or solar light can trigger degradation via a combination of hydrolytic and oxidative fragmentation of the heptadiendione moiety. Minor curcuminoids in commercial curcumin (purcuminoids) can improve the stability of molecular curcumin, but only under conditions of low irradiation. While confirming earlier observations alerting to the instability of purcumin, our results provide new rationales for unexplained differences between previous studies, question the biological relevance of a non-enzymatic degradation for the bioactivity profiles that have been reported for purcumin, and highlight the need of a better characterization of the degradation of purcuminoids under visible light irradiation.
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Curcumina/metabolismo , Cromatografia Líquida de Alta Pressão , Curcumina/química , Estabilidade de Medicamentos , Concentração de Íons de Hidrogênio , SoluçõesRESUMO
Acute diarrhea is a frequent problem worldwide, mostly due to gastrointestinal infections or food poisoning. Boswellia serrata could be active in the treatment of acute diarrhea due to its anti-inflammatory, antispasmodic, and antimicrobial activity. In this randomized, double-blind, placebo-controlled clinical study, 49 adults with acute diarrhea were randomly allocated to receive 250 mg of a lecithin-based delivery form of Boswellia serrata (CASP) or placebo for 5 days. The time it took to become healthy with stoppage of diarrhea (primary end point) was significantly shorter in the intervention group (3.08 vs. 4.44 days: p-value < 0.0001). The probability of subjects treated with CASP to recover sooner was equal to 80.2%. A significantly lower number of stools was observed in the CASP group over time (ß = −0.17, p-value < 0.0001). A significant difference was observed between the two groups for abdominal pain, nausea, and GAE (global assessment of efficacy). In conclusion, the lecithin-based delivery form of Boswellia serrata extract could be a useful addition to the treatment of acute diarrhea in adults. CASP is safe and reduces the time it takes to become healthy, the frequency of stools, the abdominal pain and nausea of subjects with acute diarrhea. Further studies are needed to confirm these promising results.
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Boswellia , Dor Abdominal/tratamento farmacológico , Adulto , Diarreia/tratamento farmacológico , Humanos , Fatores Imunológicos , Lecitinas , Náusea/tratamento farmacológico , Extratos Vegetais/uso terapêuticoRESUMO
Bloating is a symptom frequently reported by subjects with irritable bowel syndrome (IBS) and small bowel dysbiosis, and Low FODMAP's diet (LFD) has been used to treat them. Extracts of Curcumalonga and Boswelliaserrata share anti-inflammatory and antimicrobial effects that could be useful in the management of these clinical conditions. The aim of this study was to evaluate the efficacy of curcumin and boswellia extracts (as Curcumin Boswellia Phytosome, CBP) and LFD on the relief of abdominal bloating in IBS subjects with small bowel dysbiosis, in comparison to LFD alone, in a 30-day supplementation, randomized trial. IBS participants were randomized to either the intervention (500 mg bid of CBP and LFD) or control arm (LFD). Small bowel dysbiosis has been defined by an increase of urinary indican with normal urinary skatole. A total of 67 subjects were recruited. The intervention group (33 subjects) showed a significant decrease (p < 0.0001) of bloating, abdominal pain, and indican values at the end of the study, when compared to the control group (34 subjects). Moreover, the subjects of the intervention group showed a significantly better (p < 0.0001) global assessment of efficacy (GAE) as compared to controls. In conclusion, in subjects with IBS and small bowel dysbiosis, abdominal bloating can be successfully reduced with a supplementation with CBP and LFD.
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Boswellia , Curcuma , Disbiose , Síndrome do Intestino Irritável , Extratos Vegetais , Boswellia/química , Curcuma/química , Disbiose/tratamento farmacológico , Humanos , Síndrome do Intestino Irritável/tratamento farmacológico , Extratos Vegetais/uso terapêuticoRESUMO
BACKGROUND: Cancer is an irregular proliferation of cells that starts with a gene mutation that alters cellular function, is triggered by several factors, and can be inherited or acquired. The aim of this review is to discuss the anticancer activity of basil and its components' strength, focusing on its implication in cancer prevention and treatment. METHODS: This systematic review involves all of the studies published from 1 January 2010 through 1 January 2022. RESULTS: In this review, 16 research articles are included to discuss the potential anticancer ability of the extracts of various Ocimum basilicum varieties at various dosages, applied to different cancer cells. Of those 16 articles, 2 were in vivo studies, 13 were in vitro studies, and 1 study conducted both in vivo and in vitro experiments. Antioxidants and other bioactive compounds in basil leaves show important potential anticancer activity at dosage of 4 mg/mL as aqueous extract or essential oil up to 200 µg/mL could slow-down tumor growth and progression with regards to cell death and viability inhibition. At dosages from 50 to 500 µg/mL is effective as anti-proliferative activities. cytotoxicity, inducing apoptosis, slowing down tumor growth, and especially cell cycle arrest, both in vivo and in vitro. Human studies show effects at dosages from 1 to 2.5 mg/daily on general vital activities and on reducing cytokines activity. CONCLUSIONS: Based on 16 published studies, basil demonstrates important anticancer activities in vivo and vitro models, and it could act as a potential cancer.
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BACKGROUND: Exercise-induced gastrointestinal (GI) symptoms are frequently reported by athletes during training and competitions. A standardized combination of artichoke leaves and ginger root extracts has shown beneficial effects in managing GI discomfort in otherwise healthy subjects. METHODS: In this pilot study, we assessed the effectiveness of artichoke leaves and ginger root extracts combination associated with simethicone in reducing exercise-related GI symptoms in endurance athletes. The effects of the combination on upper/lower GI and systemic symptoms were assessed at baseline and after 4 weeks through a questionnaire. RESULTS: Fifty endurance athletes took the extracts' combination 320 mg + simethicone 40 mg chewable pills. The extracts combination and simethicone were effective in reducing the mean intensity of upper GI (86.6%) lower GI (85.9%) and systemic symptoms (81.9%), with superior results compared to placebo. The most remarkable effects were reported in the lower GI tract, with a significant decrease in flatulence, intestinal cramps, loose stools and diarrhea. Athletes also benefited from a reduction in belching and bloating and in dizziness, headache and muscle cramps, although the decrease in systemic symptoms was not significant. CONCLUSIONS: The supplementation of standardized artichoke and ginger extracts, combined with simethicone, may be effective in decreasing digestive discomfort and alteration of gastric motility not only in healthy subjects but also in endurance athletes.
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Cynara scolymus , Zingiber officinale , Atletas , Humanos , Projetos Piloto , Extratos Vegetais/uso terapêutico , Simeticone/uso terapêuticoRESUMO
Quercetin, for its crucial properties, fulfills the need for a multifactor action that is useful for the potential counterbalance of a COVID-19 infection. Given this background, the aim of the study was to evaluate the potential effect of 3 months' supplementation with Quercetin Phytosome® (250 mg twice a day) as prevention against symptomatic COVID-19. In total, 120 subjects were enrolled (males, 63; females, 57; age 49 ± 12), with 60 in the supplementation group and 60 in the placebo group. No significant differences were detected between groups in terms of gender, smoking, and chronic disease. Subjects underwent rapid COVID-19 diagnostic tests every 3 weeks. During our study, 5 subjects had COVID-19, 1 out of 60 subjects in the quercetin group and 4 out of 60 in the control group. Complete clinical remission was recorded at 7 and 15 days in the quercetin and placebo groups, respectively. Analysis showed that, at 5 months, the COVID free survival function (risk of infection) was 99.8% in subjects under quercetin supplementation and 96.5% in control group. As shown by the value of EXP(B), those who had taken the supplement had a protection factor of 14% more to not contract the COVID-19 infection than that of those who had taken a placebo. Obtained results are encouraging, but further studies are required to add quercetin as regular prophylaxis.
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Background: Quercetin, a natural polyphenol with demonstrated broad-spectrum antiviral, anti-inflammatory, and antioxidant properties, has been proposed as an adjuvant for early-stage coronavirus disease 2019 (COVID-19) infection. Objective: To explore the possible therapeutic effect of quercetin in outpatients with early-stage mild to moderate symptoms of COVID-19. Methods: This was an open-label randomized controlled clinical trial conducted at the department of medicine, King Edward Medical University, Lahore, PK. Patients were randomized to receive either standard of care (SC) plus an oral quercetin supplement (500 mg Quercetin Phytosome®, 1st week, TDS: 2nd week, BDS) (n = 50, quercetin group) or SC alone (n = 50, control group). Results: After one week of treatment, patients in the quercetin group showed a speedy recovery from COVID-19 as compared to the control group, i.e., 34 patients (vs. 12 in the control group) tested negative for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) (p = 0.0004), and 26 patients (vs. 12 in the control group) had their COVID-19-associated acute symptoms resolved (p = 0.0051). Patients in the quercetin group also showed a significant fall in the serum lactate dehydrogenase (LDH) mean values i.e., from 406.56 ± 183.92 to 257.74 ± 110.73 U/L, p = 0.0001. Quercetin was well-tolerated by all the 50 patients, and no side effects were reported. Conclusion: Our results, suggest the possible therapeutic role of quercetin in early-stage COVID-19, including speedy clearance of SARS-CoV-2, early resolution of the acute symptoms and modulation of the host's hyperinflammatory response. Clinical Trial Registration: clinicaltrials.gov, identifier NCT04861298.
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Menopause is characterized by weight gain and increased visceral fat, which acts as an endocrine organ secreting proinflammatory adipocytokines, with consequent increased risk of metabolic disorders. The aim of this double-blind, placebo-controlled randomized trial was to evaluate the effects of a 60-day dietary supplementation using Camellia sinensis leaf extract on adipose tissue dysfunction in overweight or class I obese post-menopausal, sedentary women. Primary endpoints were the respiratory quotient (RQ), the percentage of carbohydrates (%CHO), the percentage of fat oxidation (%FAT), and the resting energy expenditure (REE) measured by indirect calorimetry. Secondary endpoints included body composition, by dual x-ray absorptiometry (DXA), glucose profile, lipid profile, inflammatory state, liver and kidney function, hormonal status regarding satiety, and status of catecholamines. Twenty-eight women were randomized into two groups: 14 (BMI 31.1 ± 3.5) were supplemented and 14 (BMI 31.9 ± 2.2) received placebo. In regards to the between-group differences over time (ß), a statistically significant difference between the supplemented and placebo group was observed for: RQ (ß = -0.04, p = 0.009), % fat oxidation (ß = 11.04, p = 0.0006), insulin (ß = -1.74, p = 0.009), HOMA (ß = -0.31, p = 0.02), waist circumference (ß = -1.07, p = 0.007), REE (ß = 83.21, p = 0.009), and CRP (ß = -0.14, p = 0.02). These results demonstrate that a 60-day green tea extract supplementation counteracts the dysfunction of adipose tissue in overweight post-menopausal and class I obese women.
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Sobrepeso , Pós-Menopausa , Humanos , Feminino , Sobrepeso/metabolismo , Obesidade/metabolismo , Antioxidantes/metabolismo , Tecido Adiposo/metabolismo , Suplementos Nutricionais , Chá/química , Extratos Vegetais/uso terapêuticoRESUMO
There are currently no standardized therapies for Parkinson disease (PD). Curcumin shows anti-amyloidogenic properties in vitro and may be a promising treatment for PD. We evaluated the effects of curcumin supplementation on clinical scales and misfolded, phosphorylated α-synuclein (p-syn) accumulation in skin biopsies in 19 PD patients who received curcumin supplementation for 12 months and 14 PD patients to treated with curcumin. The patients underwent autonomic (COMPASS-31), motor (MDS-UPDRS and H&Y) and nonmotor (NMSS) questionnaires and skin biopsies to evaluate clinical involvement and p-syn load in skin nerves at the beginning and the end of study. Curcumin and curcuminoid levels were assayed in plasma and CSF. Supplemented patients showed detectable CSF curcuminoid levels that were lower than those in plasma. They showed a decrease of COMPASS-31 and NMSS scores, and a slight p-syn load decrease versus untreated patients who displayed a worsening of these parameters despite increased levodopa doses. Multiple regression models showed a significant effect of curcumin supplementation in decreasing the worsening of the clinical parameters and p-syn load at after curcumin treatment. These data suggest that curcumin can cross the blood-brain barrier, that it is effective in ameliorating clinical parameters and that it shows a tendency to decrease skin p-syn accumulation in PD patients.
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Curcumina , Doença de Parkinson , Biópsia , Curcumina/uso terapêutico , Humanos , Doença de Parkinson/tratamento farmacológico , Doença de Parkinson/patologia , Pele/patologiaRESUMO
It is well established that maintaining healthy blood pressure is fundamental in order to avoid disorders to the heart and blood vessels. In prevention, and alongside pharmacological therapy, the use of natural substances has been proven to be extremely helpful for pre- and mild hypertensive subjects. Our study was therefore focused on the effects, both in vitro and in humans, of a grape seed extract, Enovita (GSEe), a highly standardized extract in polyphenols of Vitis vinifera L. The in vitro human umbilical vein endothelial cells (HUVEC) model was chosen to explore the extract properties related to vascular inflammation/vasodilation. A significant reduction of both soluble Inter-Cellular Adhesion Molecule-1 (sICAM) and endothelin-1 secretion/release was induced by GSEe in HUVEC cells. A randomized, double-blind, placebo-controlled clinical study in healthy volunteers was further performed to investigate GSEe benefits. In healthy volunteers, both supplementations significantly modulated blood pressure, with a pronounced effect after GSEe tablets (300 mg/day for 16 weeks) in respect to placebo. In the male gender subgroup, no placebo effect was observed as it was for the female group. As an additional outcome, an overall GSEe positive modulation emerged on mood related to stress perception. Thus, GSEe resulted in a benefit of modulating endothelial functionality and blood pressure. It was noteworthy that GSEe relieved the perceived stress, promising new future perspectives on mood comfort.
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Pressão Sanguínea/efeitos dos fármacos , Extrato de Sementes de Uva/farmacologia , Voluntários Saudáveis , Estresse Psicológico/tratamento farmacológico , Adulto , Idoso , Suplementos Nutricionais , Método Duplo-Cego , Feminino , Extrato de Sementes de Uva/química , Humanos , Masculino , Pessoa de Meia-IdadeRESUMO
OBJECTIVE: To evaluate in vitro solubility, bioaccessibility, and cytotoxic profile, together with a pharmacokinetic profile by oral administration to healthy volunteers of a novel food-grade berberine formulation (BBR-PP, i.e., berberine Phytosome®). RESULTS: An in vitro increase of solubility in simulated gastric and intestinal fluids and an improved bioaccessibility at intestinal level along with a lower cytotoxicity with respect to berberine were observed with BBR-PP. The pharmacokinetic profile of the oral administration to healthy volunteers confirmed that berberine Phytosome® significantly ameliorated berberine absorption, in comparison to unformulated berberine, without any observed side effects. The berberine plasma concentrations observed with both doses of BBR-PP were significantly higher than those seen after unformulated berberine administration, starting from 45 min (free berberine) and 30 min (total berberine). Furthermore, BBR-PP improved berberine bioavailability (AUC) was significantly higher, around 10 times on molar basis and with observed dose linearity, compared to the unformulated berberine. CONCLUSION: These findings open new perspectives on the use of this healthy berberine formulation in metabolic discomforts.
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Polycystic Ovary Syndrome (PCOS) is the most frequent endocrine disease in females of reproductive age and is characterized by multifactorial unhealthy conditions related to hormonal unbalance and also to dysmetabolism and inflammation. Recently, increasing evidence has shown that natural plant-based products may play a role in PCOS management. The aim of this one-group pretest-post-test explanatory study was to evaluate, in normal-overweight PCOS women with normal menses, the effectiveness of berberine on: Insulin resistance (IR) by Homeostasis Model Assessment (HOMA); Inflammation by C-Reactive Protein (CRP), Tumor Necrosis Factor α (TNF-α); Lipid metabolism; Sex hormone profile and symptoms correlated to hyperandrogenism, such as acne, by Global Acne Grading System (GAGS) and Cardiff Acne Disability Index (CADI); Body composition by DXA. Finally, adverse effects were assessed by liver and kidney functions and creatine phosphokinase (CPK). All these parameters were collected at baseline and 60 days after supplementation with a new bioavailable and safe berberine formulation. Twelve females (aged 26.6 ± 4.9, BMI 25.3 ± 3.6) were supplied for 60 days with two tablets/day (550 mg/table) of the bioavailable berberine. Results showed a statistically significant decrease in HOMA, CRP, TNF-α, Triglycerides, testosterone, Body Mass Index (BMI), Visceral Adipose Tissue (VAT), fat mass, GAGS and CADI scores, and a statistically significant increase in sex hormone-binding globulin (SHBG). Liver and kidney functions and CPK are not statistically significantly different. Therefore, berberine can represent a safe novel dietary supplement, helpful in treatment strategy for PCOS.