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This patented ingredient is a purified fraction obtained from the bark, leaves and flowers of Myrica cerifera (Bayberry) by means of a purification process with a chromatographic column to remove non-active components of the plant.
It is used to prevent and remove cellulite, and forms part of the formula of our Herbal Cellulite Gel, which you can look at by clicking here.
This page contains information, and technical specifications of the extract of bayberry, which is patented as Myriceline™.
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The information below may be a bit technical for easy reading, but if you have the time and the interest, you will see how the bayberry extract, patented as Myriceline, was tested and clinically evaluated, to be an extremely effective remedy for cellulite, preventing and removing this problem.
Myriceline, the patented name of the bayberry extract, is a novel molecule acting on the lipid (fat) metabolism and the differentiation processes of adipocytes (fat cells).
 Fat cells
The product is standardized in Dihydromyricetin, which is obtained from the herb Myrica cerifera L. by extraction and subsequent purification.
It significantly reduces Lipogenesis (- 64%), Adipogenesis (-27%) and promotes Lipolysis (x 11,7 times) by selective inhibition of tyrosine kinase activity of the a receptor subunit and other enzymes involved in lipid metabolism pathways of adipocytes.
Dihydromyricetin (also called ampelopsin, 3,3’,4’,5,5’,7-hexahydroxy-2,3- dihydroflavanonol) is a flavonol involved in the synthesis pathway of delfinidin (anthocyanin).
MYRICELINE is a novel molecule acting on the three above cited pathways (lipogenesis, lipolysis and adipogenesis). But, the basis of its activity is the inhibition of the anabolic and adipogenic pathways in the adipose cells. This action is vastly different from the action of traditional cosmetic ingredients. Moreover, its chronic and acute effects on adipocytes have been clinically evaluated.
The word 'adipose' comes from the Latin prefix “adeps” meaning “fat”. The adipose tissue is a specialized conjunctive tissue with a predominance of the cell type called adipocyte. Their main function is to store energy as triglycerides. The energy storing function of adipose tissue is highly efficient due to the low density and high caloric value of triglycerides.
Adipose tissue is also important for temperature isolation, for structural support of organs and for a recently discovered endocrine function [1].
Adipose tissue can be classified into unilocular (white) and multilocular (brown) adipose tissue, according to the characteristic of the constituent cells.
Brown adipose tissue is composed of polygonal cells, smaller than those in the unilocular adipose tissue. Their cytoplasm contains several differently sized lipid droplets, and numerous mitochondria. This tissue has a thermogenic function. Its distribution in the adult body is rather restricted. It concentrates in the inter-scapular region of human embryos and newborns, and reduces considerably in the adult.
Adipocytes come from mesodermal stem cells, which are also able to produce other cell types such as muscle-cells or osteoblasts. When differentiated to pre-adipocytes, they can stay in that state or they can differentiate to mature adipocytes.
Differentiated adipocytes lose their ability to divide. However, they have a very long half-life and the ability to store increasing amounts of lipids.
Picture is of white adipocyte tissue
- Adipogenesis is the differentiation process by which pre-adipocyte cells end up as mature adipocytes.
- During this process, changes of aspect from fusiform cells like fibroblasts to more spherical and poliedric cells are observed.
- Adipocytes are specialized cells regulating the amount of stored fat in the adipose tissue through the basic mechanisms of lipolysis and lipogenesis.
- Lipolysis is a catabolic pathway, whereby stored triacylglycerides (TG) yield free fatty acids (FFA) and glycerol.
- This pathway activates as the organism demands energy, which is produced by the subsequent oxidation of FFA's.
- The activating stimulus is mediated by hormones involving the cyclic AMP pathway such as glucagon and adrenaline.
- The lipolysis process starts when these hormones increase cyclic adenosin 3´- 5´monophosphate (cAMP) levels, which induces PKA (Protein kinase A) to phosphorilate a serine on the hormone sensitive lipase (HSL), thus activating it.
- Once active, HSL migrates to the lipid droplet surface where it exerts lipase actions, by metabolising triglyceridels (TG) into diacylglycerides (DG) and these into monoacylglycerides (MG).
- Perilipin A is a characteristic protein in mature adipocytes, which covers lipid droplets into the adipocyte cell and prevents the HSL lipolytic action, inhibiting it up to 87%, under normal conditions. However, PKA also phosphorilates perilipin A that migrates away and leaves the way clear for HSL; thus promoting lipolysis
- Lipogenesis is a process that is aimed at storing energy, in the form of TG, into the adipocyte. In this case, the FFA's re-esterify to yield TG.
- Notice that synthesis of TG requires glycerol phosphate, while lipolysis yields glycerol. Since no glycerol kinase is present in the adipocytes, the occurrence of lipogenesis requires glucose intake, since glucose can be transformed into glycerol phosphate.
- The necessary FFA's for lipogenesis usually enter the bloodstream from the diet. However, they can also be synthesized from glucose entering the adipocyte, with the participation of the enzyme FAS (Fatty Acid Synthase) in a process called lipogenesis de novo. Although not a major process, it also takes place in the adipocyte.
- Adipose tissue metabolism is very active, involving the above mentioned processes of lipogenesis, lipolysis and adipogenesis which are under dynamic equilibrium.
- Depending on the stimulus, equilibrium will result in a greater or minor quantity of adipocytes and quantity of triacylglycerides inside.
- Lipid metabolism of adipose cells is modulated by the intracellular protein kinases pathway: initiated by activation of membrane receptors, inducing internal signaling cascades that ultimately result in the activation or inhibition of catabolic and anabolic pathways.
MYRICELINE action initiates on binding the tyrosine kinase activity - ß subunit of the specific receptor on the adipocyte membrane, which induces a cascade of fast biochemical reactions involved in the trans-membrane transport of glucose, activation or inactivation of several enzymes and changes in the level of expression of numerous genes.
- Activity on Adipogenesis
- Tyrosine kinase activity of ß subunit activates protein SHC, which initiates the RASMAPK pathway. This pathway is most important in cell differentiation and stimulates proliferation and differentiation into adipocytes, thus promoting adipogenesis.
- The RAS-MAPKinases pathway increases the expression and synthesis of several proteins that will initiate proliferation and differentiation processes. Among them, the following can be remarked:
- PERILIPIN
- Regulator barrier protein of adipogenesis and lipolysis. It has been found that, if perilipin is not present, cells cannot produce the lipid droplets and then HSL can better access them, all of which results in a higher lipolysis basal level.
- Therefore, preadipocytes cannot differentiate to adipocytes when perilipin is not present.
- CAVEOLIN-1
- This protein plays an important role in the differentiation processes and in the GLUT-4 membrane fusion.
- The cellular membrane surface is highly invaginated and these projections, between 50-100 nm, are called caveole. Caveole exist in most cells but are especially abundant in adipocytes. [4].
- Caveole formation requires structural proteins called caveolins. It has been found that, in adipocytes, the expression of caveolin-1 is enough for caveole to form [5].
- It seems that caveole are a cell membrane subcompartment specialized in signal transduction, where numerous receptors and cytoplasmic effectors concentrate. The lack of caveolin-1 prevents the formation of caveole, reduces the level of cell differentiation and decreases lipid accumulation in the adipose tissue.
- GLUT-4
- An isoform of the glucose transporter present in adipocytes and muscle cells.
- Its genic expression is induced by anabolic stimulation through the RAS-MAPK pathway and it is stored into vesicles in the cytoplasm.
- The vesicle translocation to the plasmatic membrane is also induced by intracellular signaling initiated by the tyrosine kinase activity of ß subunit, being PI3K and PKC - the involved enzymes.
- A reduction in the synthesis of these proteins will result in adipogenesis inhibition. This demonstrates, in in-vitro the mechanism and efficacy tests carried out with MYRICELINE.
- In-vitro efficacy tests described in the next chapter showed that MYRICELINE acts on decreasing the differentiation of pre-adipocyte cells into mature adipocytes resulting in a rate of 63% ADIPOGENESIS INHIBITION.
- Results of in-vitro mechanism tests also suggest that MYRICELINE inhibits induction of GLUT-4 (-40%), perilipin (-56%) and caveolin-1(-46%) and therefore, the adipose cell ability to promote adipogenesis.
- Conclusions
- MYRICELINE inhibits induction of GLUT-4, perilipin and caveolin-1, therefore inhibiting the adipose cell ability to promote adipogenesis and organize the cell surface in caveole. Consequently, it promotes a general decrease of the adipogenesis process.
- Activity on Lipolysis
- The tyrosine kinase activity of the receptor’s subunit ß is the key to block lipolysis in the adipocyte. Subunit ß phosphorilates different plasma proteins (IRS-1, IRS-2) and the signal transduction is thus initiated. IRS (insulin receptor substrate) – there exist different types (1,2,3,4), - binds subunit p85a of the enzyme phosphatidylinositol-3 kinase (PI3K) and activates its subunit p110.
- PI3K activates different proteins at the same time, until activation of phosphoinositoldependent kinase PDK-1. The latter enzyme activates protein PKB that activates by phosphorilation of the phosphodiesterase 3B, which metabolizes cAMP into 5’AMP. This degradation reduces PKA and HSL activity.
- The above described cascade of reactions means that tyrosine kinase activity of subunit ß also results finally in lipolysis inhibition. Then, a decrease in the tyrosine kinase activity of subunit ß will promote lipolysis activation and this is shown in in-vitro mechanism and efficacy tests performed on MYRICELINE.
- In-vitro efficacy tests described in the next chapter demonstrated that MYRICELINE is a selective blocking molecule of the tyrosine kinase activity - subunit ß and therefore causes a LIPOLYSIS ACTIVATION with an 11, 7 fold increase of triglycerides metabolism.
- Results of in-vitro mechanism tests confirmed that MYRICELINE acts by inhibiting four of the mentioned proteins: protein tyrosine kinase (-67%), IRS (86%), PI3K (-68%) and PKB (-72%).
- Conclusions
- MYRICELINE produces an inhibitor effect on four of the main proteins involved in the initial steps of the intracellular signaling for the lipolysis pathway in the adipose cell.
- Activity on Lipogenesis
- In the above paragraph, it was explained how PI3K activates, which in turn activates the transformation of phosphatidylinositol-2-phosphate (PIP2) into PIP3 [7]. The later stimulates the translocation of transporter GLUT-4 from intracellular vesicles, where it is stored, to the cell membrane surface, thus increasing glucose intake (due to the lack of glycerol kinase into the adipocytes, glucose intake is essential for the synthesis of triglycerides).
- Hence, the tyrosine kinase activity of subunit ß also results in inducing translocation of the transporter GLUT-4 and a consequent increase of lipogenesis.
- The phosphatidylinositol-3-phosphate (PIP3) enzyme is moreover involved in the activation of other proteins:
- Phosphatidylinositol-dependent kinase (PDK-1);
- Direct activation of different protein kinases C (PKC) and also indirect activation of them by PDK-1. These PKC are essential for the translocation of GLUT-4 to the membrane (an important process for lipogenesis to occur).
- PDK-1 activates different proteins (PRK-1, PKC p70S6K, PKB) in turn. Protein p70S6K, once active and phosphorilated, activates several transcription factors, which promote the synthesis of certain proteins and enzymes. One of them is FAS, catalyser of the steps from acetyl-CoA and malonyl-CoA to palmitate in the de novo lipid synthesis.
- Thus, a decreased tyrosine kinase activity of subunit ß will finally also promote lipogenesis inhibition as in-vitro mechanism and efficacy tests with MYRICELINE demonstrated.
- In-vitro efficacy tests described in the next chapter show that MYRICELINE has a selective inhibitor effect on tyrosine kinase activity of subunit ß of the receptor (by interaction with the active centre of this subunit) causing ultimately a 64% LIPOGENESIS DECREASE in cultures of adipocytes.
- In-vitro mechanism of the tests showed MYRICELINE activity is the consequence of its inhibitory effect on the activation of the following proteins, involved in lipogenesis process: protein tyrosine kinase (-67%), IRS (-86%) and PI3K (-68%).
- Conclusion
- MYRICELINE produces an inhibitor effect on three of the main proteins involved in the initial steps of the intracellular signaling for the lipogenesis pathway in the adipose cell.
Several in vitro assays using adipocyte culture, aimed at evaluating the effects of MYRICELINE on these cells have been carried out and on this basis adipocyte metabolism can be modulated in different ways:
- Inhibiting adipogenesis (preventing the formation of new adipose cells).
- Stimulating lipolysis (increasing the rate of triglyceride metabolism into the adipose cells, consequently reducing the fat amount).
- Inhibiting lipogenesis (decreasing the rate of fatty acid and triglyceride synthesis, consequently reducing the formation of new fat).
Evaluation of effect on dermis density
The in-vivo study was carried out on 10 volunteers and involved two daily applications of the product on a definite area of the thighs for 28 consecutive days. MYRICELINE was tested using a 0.5% formulation. Parallel applications of the placebo, namely identical formulation without the active compound, were carried out under the same conditions.
The efficacy of MYRICELINE was evaluated by measuring the dermal density.
Method
Adipose tissue infiltrates were measured by using the 2D DermaScan C® technique. This method is based on the use of ultrasound and allows for the bi-dimensional visualization of the skin, as well as for thickness and density measurements of the different skin layers. The less adipose tissue infiltrates present in the skin, the higher its density and the larger the recorded values.
References
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