42 research outputs found

    Effects of a healthy meal course on spontaneous energy intake, satiety and palatability

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    Many food components can influence satiety or energy intake. Combined together, these food components could represent an interesting dietary strategy in the prevention and treatment of obesity. The aims of this study were: 1) to determine the effect of a functional food in the form of a healthy meal course on subsequent energy intake and satiety; 2) to verify if it is possible to maintain palatability while preserving the satiating effects of the test meal. Thirteen subjects were invited to eat two lunch sessions: healthy and control meal courses (2090 kJ/meal). Anthropometric and ad libitum food intake measurements, and visual analogue scales (VAS) were performed during the two lunch sessions. The healthy main course acutely decreased energy intake during the rest of the meal ( − 744 kJ, P ≀ 0·0001) and lipid ( − 6 %, P ≀ 0·0001) compared with the control meal. VAS ratings during the course of the testing showed a meal effect for hunger, desire to eat and prospective food consumption (P ≀ 0·05) and a time effect for all appetite sensations (P ≀ 0·0001). VAS scores on hunger ratings were lower for the healthy meal (P ≀ 0·05), whereas fullness ratings were higher shortly after the healthy main course (P ≀ 0·05). The healthy meal produced a slightly higher palatability rating but this effect was not statistically significant. These results suggest that it is possible to design a healthy meal that decreases spontaneous energy intake and hunger without compromising palatability

    Design, synthesis, cytocidal activity and estrogen receptor a affinity of doxorubicin conjugates at 16α-position of estrogen for site-specific treatment of estrogen receptor-positive breast cancers

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    Doxorubicin (DOX) is an important medicine for the treatment of breast cancer, which is the most frequently diagnosed and the most lethal cancer in women worldwide. However, the clinical use of DOX is impeded by serious toxic effects such as cardiomyopathy and congestive heart failure. Covalently linking DOX to estrogen to selectively deliver the drug to estrogen receptor-positive (ER+) cancer tissues is one of the strategies under investigation for improving the efficacy and decreasing the cardiac toxicity of DOX. However, conjugation of drug performed until now was at 3- or 17-position of estrogen, which is not ideal since the hydroxyl groups at this position are important for receptor binding affinity. In this study, we designed, prepared and evaluated in vitro the first estrogen–doxorubicin conjugates at 16α-position of estradiol termed E-DOXs (8a–d). DOX was conjugated using a 3–9 carbon atoms alkylamide linking arm. E-DOXs were prepared from estrone using a seven-step procedure to afford the desired conjugates in low to moderate yields. The antiproliferative activities of the E-DOX 8a conjugate through a 3-carbon spacer chain on ER+ MCF7 and HT-29 are in the micromolar range while inactive on M21 and the ER− MDA-MB-231 cells (>50 ÎŒM). Compound 8a exhibits a selectivity ratio (ER+/ER− cell lines) of >3.5. Compounds 8b–8d bearing alkylamide linking arms ranging from 5 to 9 carbon atoms were inactive at the concentrations tested (>50 ÎŒM). Interestingly, compounds 8a–8c exhibited affinity for the estrogen receptor α (ERα) in the nanomolar range (72–100 nM) whereas compound 8d exhibited no affinity at concentrations up to 215 nM. These results indicate that a short alkylamide spacer is required to maintain both antiproliferative activity toward ER+ MCF7 and affinity for the ERα of the E-DOX conjugates. Compound 8a is potentially a promising conjugate to target ER+ breast cancer and might be useful also for the design of more potent E-DOX conjugates

    The effect of psychological interventions on the prevention of chronic pain in adults: a systematic review protocol

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    Abstract Background Numerous psychological risk and protective factors have been identified as contributing to or preventing the development of the prevalent issue of chronic pain. Systematic reviews of studies on psychological interventions that tackle these factors have shown limited effects on chronic pain. Therefore, implementing psychological interventions before pain becomes chronic has been put forward. However, the efficacy of such interventions in preventing the transition from acute to chronic pain has not yet been systematically assessed. Methods The aims of this systematic review are to assess the effects of psychological interventions applied in the acute pain phase on pain severity as well as on physical, psychological, and social functions at 3 months and beyond. Randomized controlled trials including psychological intervention as a treatment of primary interest and participants with pain of less than 3 months duration will be considered. The following comparisons will be undertaken: psychological interventions with (1) standard treatment, (2) information, (3) waiting-list, and (4) active treatment. The primary outcome will be pain severity using indicators such the presence or absence of pain and self-report measures such as the numeric pain intensity rating scale. Secondary outcomes will include pain-related disability, mood, coping with pain, quality of life, health care utilization, and work capability. A systematic review of English and French articles in MEDLINE, Embase, PsycINFO, CINAHL, and the Cochrane Central Register of Controlled Trials will be conducted without date restriction. Extracted data will include demographics and clinical characteristics, sample size, intervention and control group types, assessment tools used, time interval of measurement, fidelity of the intervention, and attrition rate. Standardized mean differences (SMD) and risk ratios with 95% confidence intervals (CI) will be used to assess treatment effects. Discussion This systematic review is the first in examining the effects of psychological interventions implemented in the acute pain phase with the objective of preventing chronic pain. Results of this systematic review could provide information on psychological intervention characteristics that are most helpful for individuals with pain and guidance as to when such interventions should be applied in the continuum of care. Systematic review registration PROSPERO CRD4201604931

    Synthesis, antiproliferative activity and estrogen receptor α affinity of novel estradiol-linked platinum(II) complex analogs to carboplatin and oxaliplatin. Potential vector complexes to target estrogen-dependent tissues

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    In the course of efforts to develop 17ÎČ-estradiol-linked to anticancer agents targeting estrogen-dependent tissue, we identified three estradiol-linked platinum(II) complex analogs to cisplatin (E-CDDP) derivatives namely: VP-128 (1), CD-38 (2) and JMP-39 (3) that exhibit potent in vitro and in vivo (for derivative VP-128) activity along with interaction with the estrogen receptor α (ERα). In this study, we prepared and biologically evaluated two novel classes of estradiol-linked platinum(II) complex analogs to carboplatin (E-CarboP, 1a-3a) and oxaliplatin (E-OxaP, 1b-3b). E-CarboP and E-OxaP were designed and based on the estradiol-linker scaffold of E-CDDP derivatives previously identified. Consequently, we assessed the importance of the nature of platinum(II) salt on the antiproliferative activity on MCF-7 and MDA-MB-231 human mammary carcinoma cell lines together with affinity for the ERα by replacing the dichloroplatinum(II) moiety by a cyclobutane-1,1-dicarboxylateplatinum(II) or an oxalateplatinum(II) moiety. Except for compound 3b which is inactive at the concentration tested, the antiproliferative activity of all compounds on both human mammary carcinomas cell lines are in micromolar range and are more active than carboplatin and oxaliplatin alone but less active that their E-CDDP counterparts (1-3). In addition, E-CarboP derivatives 1a-3a show very low affinity for ERα whereas E-OxaPs 1b and 2b show higher affinity for ERα than their parents E-CDDPs (1-2), suggesting that the nature of the platinum(II) salt involved in the vector complexes is extremely important to both retain significant antiproliferative activity and selectivity for the ERα and possibility to target estrogen-dependent tissues. Finally, E-OxaPs 1b and 2b are potentially promising alternatives vector complexes to target estrogen-dependent tissues
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