Etudes sur les boosters sexuels et la sexualité

Le jus de cassis comme inhibiteur MAO?

10/10/2018 | Etudes Compléments alimentaires et Etudes Perte de poids et Etudes Anti-âge et Etudes sur les boosters sexuels et la sexualité

 

The pharmacodynamic profile of “Blackadder” blackcurrant juice effects upon the monoamine axis in humans: A randomised controlled trial
Anthony W. Watson       Nutritional Neuroscience         05 Oct 2018

Emerging evidence from human intervention trials indicates health benefits of consuming blackcurrant fruit, including improvements to cognitive performance, modulation of blood flow, regulation of blood glucose and inhibition of enzymes underpinning normal cognitive function. Of particular relevance is our previous demonstration of monoamine oxidase (MAO)-A and B inhibition after the consumption of a New Zealand “Blackadder” blackcurrant juice in humans.

The current study uses a double-blind, placebo-controlled, randomised cross- over design to assess the pharmacodynamics of the effects on platelet MAO-B inhibition and associated substrates, plasma prolactin levels and blood glucose levels after consumption of a single serve of “Blackadder” blackcurrant juice standardised to 500 mg polyphenols. Eight healthy male (20-–35 years) participants completed the trial. Measurements were obtained at baseline 15, 30, 45, 60, 100, 120, 150, 180, 240 mins and 24 h post dose.

A fast, absolute and reversible inhibition of blood platelet MAO-B (P 

< 0.001) and a significant but delayed reduction in plasma prolactin (P 

< 0.001) were observed following the consumption of “Blackadder” blackcurrant juice when compared to a placebo control. No interpretable changes in substrates of MAO or associated metabolites were seen.

These data provide a clear time course of the reversible inhibition of MAO-B after the single consumption of a of New Zealand “Blackadder” blackcurrant juice standardised at

500 mg of polyphenols and, therefore, provide a therapeutic window on which to base future nutritional interventions.

Liens Cordyceps sinensis et cancer?

02/10/2018 | Etudes Compléments alimentaires et Etudes Anti-âge et Etudes sur les boosters sexuels et la sexualité

 

Cordyceps sinensis Promotes the Growth of Prostate Cancer Cells
Ming-wei Ma           Nutrition and Cancer   01 Oct 2018

Abstract
Background: This study aims to test whether Cordyceps sinensis (CS), the most expensive Asian nutrient supplement might stimulate growth of prostate cancer cells.

Methods: Impact of CS on growth of prostate cancer was determined in vivo and in vitro.

Results: Firstly, the serum testosterone level was significantly elevated in mice fed CS. Prostate glands were significantly enlarged (weight index 0.53 ± 0.04 mg/g vs. 0.31 ± 0.04 mg/g, P = 0.006). Furthermore, cell viability was increased twofold in the androgen-responsive prostate cancer cell line (VCaP) after CS treatment. This promoting effect disappeared after bicalutamide was added. In addition, serum prostate-specific antigen (PSA) in mice bearing VCaP xenografts was significantly elevated (0.66 ± 0.04 ng/ml vs. 0.26 ± 0.06 ng/ml, P 

< 0.001) after treatment with CS. Finally, VCaP tumors in mice treated with CS grew much faster (479.2 ± 78.74 mm3 vs. 283 ± 58.97 mm3, P = 0.074). However, the above promoting effects of CS were not observed in parallel studies using the PC-3 cell line which lacks AR expression.

Conclusions:

These results suggest that CS promotes growth of prostate cancer cells by increasing production of testosterone and stimulating the AR-dependent pathway. Additional studies are required to see whether CS is safely consumed by patients with prostate cancer.

Les boosters de NO pour maigrir sur le long terme?

14/12/2017 | Etudes Perte de poids et Etudes Anti-âge et Etudes sur les boosters sexuels et la sexualité

 

Ca fait quand même un peu beaucoup…

Sildenafil induces browning of subcutaneous white adipose tissue in overweight adults
Metabolism Volume 78, January 2018, Pages 106-117

To investigate that short-term treatment of sildenafil can induce browning of subcutaneous white adipose tissue (sWAT) in human adults.

Design
A randomized, double-blinded, placebo-controlled, parallel group trial.

Methods
Sixteen eligibility overweight male subjects were recruited, comparing 100 mg/day sildenafil versus an identical placebo therapy for 7 days. sWAT samples were collected from subjects before and after 7-day sildenafil or placebo interventions.

Results
The results showed that multilocular UCP1-positive adipocytes existed in sWAT samples from subjects after sildenafil treatment. Compared to before treatment in both group as well as after treatment in placebo, sildenafil significantly decreased adipocyte size, increased the expressions of UCP1 protein and mRNA, mitochondrial density, and leak respiratory capacity in sWAT (p < 0.05). Sildenafil also increased plasma cyclic guanosine-3′,5′-monophosphate (cGMP) and catecholamine concentrations (p < 0.05), and consequently activated the expressions of vasodilator-stimulated phosphoprotein (VASP) and p70 ribosomal S6 kinase 1 (S6 K1) (p < 0.05). Sildenafil did not activate typical brown fat.

Conclusions
The current findings demonstrate that sildenafil can induce browning of sWAT in human, and this action may be through cGMP-dependent protein kinase I and mechanistic/mammalian target of rapamycin (mTOR) signaling pathways. Sldenafil may be a promising treatment for metabolic disease.

Le Viagra est-il aussi un anti-aromatase?

01/12/2016 | Etudes Perte de poids et Etudes Anti-âge et Etudes sur les boosters sexuels et la sexualité

 

Effect of sildenafil on human aromatase activity: From in vitro structural analysis to catalysis and inhibition in cells
The Journal of Steroid Biochemistry and Molecular Biology Volume 165, Part B, January 2017, Pages 438–447       Roberta Baravalle

Highlights
• Human aromatase binds the drug sildenafil showing a Type II spectrum.
• EPR spectroscopy shows that sildenafil does not directly bind heme iron.
• Sildenafil acts as a mixed and partial inhibitor on human aromatase.
• Aromatase inhibition by sildenafil is confirmed in ST14A and MCF-7 cells.

Aromatase catalyses the conversion of androgens into estrogens and is a well-known target for breast cancer therapy. As it has been suggested that its activity is affected by inhibitors of phosphodiesterase-5, this work investigates the potential interaction of sildenafil with aromatase. This is carried out both at molecular level through structural and kinetics assays applied to the purified enzyme, and at cellular level using neuronal and breast cancer cell lines.

Sildenafil is found to bind to aromatase with a KD of 0.58 ± 0.05 μM acting as a partial and mixed inhibitor with a maximal inhibition of 35 ± 2%. Hyperfine sublevel correlation spectroscopy and docking studies show that sildenafil binds to the heme iron via its 6th axial water ligand.

These results also provide information on the starting molecular scaffold for the development of new generations of drugs designed to inhibit aromatase as well as phosphodiesterase-5, a new emerging target for breast cancer therapy.

Le curcuma est-il un inhibiteur de la 5 alpha réductase?

27/11/2016 | Etudes Compléments alimentaires et Etudes Anti-âge et Etudes sur les boosters sexuels et la sexualité

 

A new label-free screen for steroid 5α-reductase inhibitors using LC-MS
Steroids Volume 116, December 2016, Pages 67–75       Jukkarin Srivilai

Highlights
• A novel assay for 5 alpha reductase (S5αR) activity determination based on LC-MS quantitation of DHT.
• The assay showed high reproducibility and selectivity with Z′ factor of 0.77.
• The method was successfully used to quantify S5αR inhibitory activity of some herbal extracts.

Steroid 5α-reductase (S5αR) plays an important role in metabolizing testosterone into active androgen dihydrotestosterone (DHT) which is involved in many androgen dependent disorders, such as androgenic alopecia, benign prostatic hyperplasia and acne. The method for screening for S5αR inhibition is key in finding new antagonists. In this study, the label-free S5αR inhibitory assay using LC-MS was developed. S5αR type 1 enzyme was obtained from LNCaP prostate cancer cells. The enzymatic assay was optimised for enzyme-substrate (testosterone) concentration, NADPH-cofactor concentration, solvent tolerance, enzyme activity stability and incubation time. The developed assay was validated by measuring the signal to background ratio (S/B), the signal to noise ratio (S/N), the signal window (SW) and the zeta factor Z′ in accordance with published bioassay guidelines. The enzymatic reaction was performed in 96-well plates and DHT formation was determined by LC-MS. S/B, S/N, SW and Z′ factor were well above acceptable criteria and the reproducibility was good using Z′ factor other 3 days and further validated by dutasteride and finasteride inhibition. The method was successfully applied to quantify S5αR inhibitory activity of some Thai herbal extracts.

Two plant extracts, Impatiens balsamina L. and Curcuma longa L. showed IC50 at 5.4 ± 0.2 and 9.0 ± 1.2 μg mL−1 and are therefore promising sources of new S5αR inhibitors. The assay has high selectability and reproducibility and suited to medium throughput screening required by phytochemistry.

80% des suppléments européens de rhodiole sont de mauvaise qualité

27/05/2016 | Etudes Compléments alimentaires et Etudes Perte de poids et Etudes Anti-âge et Etudes sur les boosters sexuels et la sexualité

 

The authenticity and quality of Rhodiola rosea products
Phytomedicine Volume 23, Issue 7, 15 June 2016, Pages 754–762       Anthony Booker

Les suppléments européens de rhodiole sont de mauvaise qualité

Rhodiola rosea L. Crassulaceae, root (Golden Root, Arctic Root) is a high-value herbal medicinal product, registered in the UK for the treatment of stress-induced fatigue, exhaustion and anxiety based on traditional use and used throughout Europe as a herbal medicinal product for similar indications. Numerous unregistered supplements are also available. There are several Chinese species used in traditional Chinese medicine (TCM), including Rhodiola crenulata (Hook.f. & Thomoson) that is believed to be a common adulterant in the R. rosea value chain.

Aims

The project is embedded in a larger study aiming to investigate the diverse value chains that lead to the production of R. rosea as an herbal medicinal product or supplement. Here we focus on a comparison of the quality of the finished products and assess any phytochemical variation between products registered under the Traditional Herbal Medicine Products Directive (THMPD) and products obtained from the market without any registration (i.e. generally unlicensed supplements). Our key aim is to establish the extent of the problem in terms of adulteration of consumer products claiming to contain R. rosea (or R. crenulata).

Methods

Approximately 40 commercial products (granulated powders and extracts) were sourced from different suppliers. We analysed these samples using high performance thin layer chromatography (HPTLC), mass spectrometry (MS) and 1H NMR spectroscopy coupled with multi-variate analysis software following a method previously developed by our group for the analysis of turmeric products.

Results

We investigate the phytochemistry of the different species and assess the potential of R. crenulata as an adulterant at the end of the R. rosea value chains. The consistency of the products varies significantly. Approximately one fifth of commercial products that claimed to be R. rosea did not contain rosavin (the key reference markers used to distinguish R. rosea from related species). Moreover some products appeared not to contain salidroside, another marker compound found in other Rhodiola species. Approximately 80% of the remaining commercial products were lower in rosavin content than the registered products and appeared to be adulterated with other Rhodiola species.

Conclusions

The variation in phytochemical constituents present in Rhodiola products available to European buyers via the internet and other sources is a major cause for concern. Adulteration with different species, and other sometimes unknown adulterants, appears to be commonplace. Good quality systems and manufacturing practices, including those required under the THMPD, enable consumers to have confidence that products are authentic and meet a high specification for quality and safety.

Du Tadalafil pour maigrir?

03/03/2016 | Etudes Compléments alimentaires et Etudes Perte de poids et Etudes Anti-âge et Etudes sur les boosters sexuels et la sexualité

 

Tadalafil reduces visceral adipose tissue accumulation by promoting preadipocytes differentiation towards a metabolically healthy phenotype: Studies in rabbits
Elena Maneschi               Molecular and Cellular Endocrinology Volume 424, 15 March 2016, Pages 50–70

Highlights
• Tadalafil reduced visceral fat accumulation (VAT) in an animal model of MetS.
• Tadalafil dosing induced the expression of UCP1 (brown-fat marker) in visceral fat.
• Tadalafil improved insulin sensitivity in preadipocytes (PAD) isolated from VAT.
• Tadalafil promoted PAD differentiation towards a metabolically healthy phenotype.


Development of metabolically healthy adipocytes within dysfunctional adipose tissue may represent an attractive way to counteract metabolic syndrome (MetS). In an experimental animal model of high fat diet (HFD)-induced MetS, in vivo, long- and short-term tadalafil treatments were able to reduce visceral adipose tissue (VAT) accumulation and hypertriglyceridemia, and to induce the expression in VAT of the brown fat-specific marker, uncoupling protein 1 (UCP1). VAT preadipocytes (PAD), isolated from the tadalafil-treated HFD rabbits, showed: i) a multilocular morphology; ii) an increased expression of brown fat-specific genes (such as UCP1 and CIDEA); iii) improved mitochondrial structure and dynamic and reduced superoxide production; iv) improved insulin sensitivity. Similar effects were obtained after in vitro tadalafil treatment in HFD rPAD. In conclusion, tadalafil counteracted HFD-associated VAT alterations, by restoring insulin-sensitivity and prompting preadipocytes differentiation towards a metabolically healthy phenotype.

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