RESUMO
OBJECTIVE: The purpose of this study was to explore the clinical benefit and tolerability of IQP-AO-101 in healthy subjects with sleep complaints. METHODS: This double-blind, randomized, placebo-controlled trial involved fifty subjects with sleep complaints. Subjects with a Pittsburgh Sleep Quality Index (PSQI) score between 6 and 15 were randomized to receive either IQP-AO-101 or placebo for 6 weeks, following a run-in period of one week. Sleep parameters were assessed at baseline and after 1, 4, and 6 weeks using the modified Athens Insomnia Scale (mAIS). Subjects were also instructed to wear an activity tracker and keep a sleep diary during the study. Other questionnaires administered were the Frankfurt Attention Inventory (FAIR-2) and the Profile of Mood States (POMS-65). Blood samples for safety laboratory parameters were taken before and at the end of the study. RESULTS: After 6 weeks, subjects who consumed IQP-AO-101 reported significant improvements in mAIS scores compared with placebo, including mAIS total score (11.76 ± 6.85 vs 4.00 ± 4.80; p < 0.001); night parameters composite score (5.20 ± 3.80 vs 2.04 ± 3.16; p = 0.001); and day parameters composite score (6.56 ± 4.10 vs 1.96 ± 2.65; p < 0.001). All individual parameters (Items 1 to 8) were also significantly improved from baseline after 6 weeks of IQP-AO-101 intake. Analysis of variance with baseline values as covariates showed statistically significant improvements across all individual parameters for IQP-AO-101 when compared to placebo. The measurements using the activity tracker, sleep diary, FAIR-2, and POMS did not reveal any significant differences between groups. No adverse effects related to the intake of IQP-AO-101 were reported. Tolerability was rated as very good by all the subjects and by the investigator for all cases. CONCLUSIONS: In this study, IQP-AO-101 was well tolerated and efficacious for promoting sleep and enhancing daytime performance in subjects with moderate sleep disturbances. CLINICAL TRIAL REGISTRATION: This trial is registered with ClinicalTrials.gov, no. NCT03114696.
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Objective: This study was performed to determine the efficacy and tolerability/safety of IQP-AE-103 on body weight reduction in overweight to moderately obese adults. Methods: A double-blind, randomized, placebo-controlled trial involved one hundred and eight subjects (BMI between 25 and 35 kg/m2) that were randomly assigned to either the low-dose or the high-dose IQP-AE-103 group, or the placebo group. Following a 2-week run-in period, subjects received two capsules of investigational product after three daily main meals for 12 weeks. Subjects were instructed to maintain a nutritionally balanced hypocaloric diet according to the individual's energy requirement. Body weight, body fat, and waist and hip circumference were measured at baseline, and after 2, 4, 8, and 12 weeks. Subjects also rated their feelings of hunger and fullness using visual analogue scales, and food craving on a 5-point scale at the same time intervals. Blood samplings for safety laboratory parameters were taken before and at the end of the study. Results: After 12 weeks of intake, the high-dose IQP-AE-103 group had a significantly greater weight loss compared with the placebo (5.03 ± 2.50 kg vs. 0.98 ± 2.06 kg, respectively; p < 0.001) and the low-dose group (3.01 ± 2.19 kg; p=0.001). The high-dose group experienced a decrease in body fat of 3.15 ± 2.41 kg compared with a decrease of 0.23 ± 2.74 kg for the placebo group (p < 0.001). High-dose IQP-AE-103 also decreased the feeling of hunger in 66% subjects. A beneficial effect of IQP-AE-103 on the lipid metabolism was also demonstrated in the subgroup of subjects with baseline total cholesterol levels above 6.2 mmol/L. No side effects related to the intake of IQP-AE-103 were reported. Conclusions: These findings indicate that IQP-AE-103 could be an effective and safe weight loss intervention. This trial is registered with NCT03058367.
Assuntos
Fármacos Antiobesidade/farmacologia , Inulina/farmacologia , Obesidade/tratamento farmacológico , Sobrepeso/tratamento farmacológico , Redução de Peso/efeitos dos fármacos , Abelmoschus/química , Adulto , Peso Corporal/efeitos dos fármacos , Dieta Redutora , Suplementos Nutricionais , Método Duplo-Cego , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Obesidade/fisiopatologia , Sobrepeso/fisiopatologia , Fitoterapia , Resultado do Tratamento , Redução de Peso/fisiologia , Adulto JovemRESUMO
Isolation and identification of the inhibitors of butyrylcholinesterase (BChE), obtained from the extracts of roots and fruits of Angelica archangelica L., are reported. Our results confirmed the weak inhibitory effect of Angelica roots on acetylcholinesterase activity. BChE inhibition was much more pronounced at a concentration of 100 µg/mL for hexane extracts and attained a higher rate than 50%. The TLC bioautography guided fractionation and spectroscopic analysis led to the isolation and identification of imperatorin from the fruit's hexane extract and of heraclenol-2'-O-angelate from the root's hexane extract. Both compounds showed significant BChE inhibition activity with IC(50) = 14.4 ± 3.2 µM and IC(50) = 7.5 ± 1.8 µM, respectively. Only C8-substituted and C5-unsubstituted furanocoumarins were active, which could supply information about the initial structures of specific BChE inhibitors.
Assuntos
Angelica archangelica , Butirilcolinesterase/efeitos dos fármacos , Inibidores da Colinesterase/isolamento & purificação , Frutas/química , Furocumarinas/isolamento & purificação , Raízes de Plantas/química , Fracionamento Químico , Inibidores da Colinesterase/farmacologia , Furocumarinas/farmacologia , Hexanos , Extratos Vegetais/química , Extratos Vegetais/farmacologiaRESUMO
Acetylcholinesterase (AChE) inhibitors are widely used for the symptomatic treatment of Alzheimer's disease (AD) to enhance central cholinergic transmission. On the other hand, butyrylcholinesterase (BuChE) inhibitors were reported to produce a significant increase in brain extracellular AChE without triggering severe peripheral or central side effects. In the present study, we selected twelve plants used in traditional European medicine to treat different central nervous system (CNS) disorders or to improve memory. Methanolic and hexane extracts of these plants were tested for the AChE and BuChE inhibitory activity using Ellman's colorimetric method. The most potent AChE and BuChE inhibition was observed in the hexane extracts of the flowers of Arnica chamissonis Less. subs. foliosa and Ruta graveolens L. herb at a concentration of 400 microg mL(-1). However, methanolic extracts of the flowers of Arnica chamissonis Less. subs. foliosa and the Hypericum perforatum L. herb demonstrated at the same concentration, selective inhibition only against AChE but not against BuChE. The other extracts did not show any significant AChE or BuChE inhibitory activity. Our results show that further investigations of the extracts of arnica, rue and St. John's Wort are needed to identity the compounds responsible for the AChE and BuChE inhibitory activity.