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The "cellular-level" patented repair particle Ectoine®, developed in Germany, redefines the concept of skin repair for you.

2023.06.16

News

by Reichpharm

The patented repair particle Ectoine®, which is the core ingredient of Wasser Dermatitis Cream, differs from conventional skin protection components. Its reparative ability directly safeguards the cells.

Ectoine®, an extremolyte molecule, is a small molecule that protects extremophilic microorganisms. Discovered by the German pharmaceutical company bitop AG from the salt flats of Bonaire in the Caribbean, the original strain has been developed and produced using the patented biNEXT technology to obtain the highest quality natural Ectoine® molecule. It is used for the treatment of respiratory diseases, allergies, and skin disorders. Ectoin represents a widely applicable and well-tolerated natural protective molecule that can withstand various harmful environmental influences such as heat, drought, or UV radiation.

From protecting extremophilic microorganisms in extreme climates and environments, Ectoine® now serves the purpose of safeguarding skin cells from external aggressors.

Extremophiles are a group of microorganisms that thrive in extreme environments such as extreme cold, extreme heat, extreme acidity, extreme alkalinity, extreme salinity, and extreme pressure. These bacteria have developed unique physiological characteristics to adapt and survive in such challenging conditions. The survival of extremophiles in extreme environments can be attributed to their distinct cell structures, which play a crucial role.

Thermophiles, which are commonly found among extremophiles, are organisms that thrive in high-temperature environments. The cell membrane, an essential organelle for maintaining cell integrity and growth, has been found to have different lipid compositions in thermophilic bacteria compared to normal bacteria. The Asian-Pacific volcanic belt, for example, is home to many geothermal hot spring areas where extreme environments such as submarine hydrothermal vents, alkaline or acidic geothermal springs exist. Previous studies have revealed the presence of various thermophilic microorganisms in these natural high-temperature environments.

Ectoine® is a low-molecular-weight cyclic amino acid derivative produced by various extremophilic microorganisms. It belongs to the class of compatible solutes, also known as extremolytes, which are osmoprotectants derived from extremophilic microorganisms. Ectoine® was first isolated from the “red halophilic bacteria” discovered in Egypt. In extremophilic microorganisms, these low-molecular-weight compounds accumulate with increasing extracellular salt concentration and serve as a response to other environmental changes, such as temperature elevation. This is one of the ingenious strategies developed by extremophilic microorganisms to cope with harsh environmental conditions.

Ectoine® minimizes denaturation typically observed under water stress conditions and remains compatible with intracellular environments even at high concentrations (>1M). It can protect biomacromolecules and cells from external stress damage, making it widely applicable in various fields.

 

Ectoine® is known for its skin barrier and moisturizing properties

Ectoine® stabilises biomolecules via a physical mechanism, called “preferential exclusion” According to this theory, the protein stabilisation effects of osmo- lytes like ectoine are due to their effect on the solvent water leading to a prefer- ential exclusion of the osmolyte from the protein surface and thereby to a prefer- ential hydration of the protein.
Because the surface area of globular proteins in the native state is smaller than in the denatured state, the equilibrium is shifted to the native state resulting in stabilisation of the native structure.

The effect is based on several mechanisms:
1. Steric exclusion from the protein surface: this plays a role only in cases where the protective molecule is substantially larger than water.
2. Increase of the surface tension of water by the protective molecule: According to the Gibbs adsorption isotherm this must result in the exclusion of ectoine from the water-macromolecule interface.
3. Preferential hydration due to the solvophobic effect: Solvophobicity is a con- sequence of increased hydrophobic interactions caused by a solute molecule that enforces the water structure. According to this concept of the osmophobic effect, the repulsion between the amide backbone of the protein and the os- molyte is due to the influence of the osmolyte on the water structure.

The formation of ectoine water complexes and thus the kosmotropic effect of ectoine on the water structure shown above can stabilise lipid mono- and bilayers as well, which can be considered as a model for cell membranes.

As shown in Figure 3, a lipid bilayer in water is stabilised by hydrophobic inter- actions of the apolar lipid tail and hydrophilic interactions of the polar lipid head groups to water. In an ectoine solution, the hydrophilic interactions are increased by the ectoine water complexes resulting in increased mobility of lipids and thus fluidity of lipid bilayers.

The effect of ectoine on fluidity of lipid membranes was shown recently by film balance measurements of lipid monolayers (Figure 4).
By increasing the surface pressure on a DPPC lipid monolayer in water the forma- tion of rigid well-shaped domains can be observed at higher pressure. These rigid domains are much smaller in ectoine solutions. The higher the concentration of ectoine the smaller the rigid domains. The effect is already observed at the lowest concentration tested (1 mM).

The physical state of the membrane influences the cell biology and its behaviour in response to external inputs. An increased fluidity of the membrane may for example induce the expression of stress-responsive, cell-protecting genes, such as heat-shock proteins, and reduce on-going inflammatory processes. The modification of the distribution of membrane proteins in a more fluid membrane also alters their activity.

An increase in the membrane fluidity could reduce disease symptoms and accel- erate healing. It is crucial for the efficient closure of wounds, and it has been suggested as mechanism for the very early effects of corticosteroids in asthma therapy  and the beneficial effect of dietary moderate ethanol and polyun- saturated fatty acids intake in inflammatory diseases such as psoriasis, allergy, asthma and inflammatory bowel disease .

Extracellular membrane components (transmembrane proteins, lipids, extracellular matrix) are stabilised by ectoine in their native form. Without protective mechan- isms, external and internal noxa can cause increased stress for cell membranes. Cells which are in direct contact with the environment like squamous epithelial cells, i.e. skin, upper airway, lung, and intestinal tract, are particularly endangered. The external stress leads to membrane damage, which causes water loss and in- flammatory reactions in the tissue.

The Ectoine®Hydro Complex protects the cells against dehydration by accumulating water. Water molecules are bound more effectively near the membranes and form a stabilising and protecting complex. The impact of external pollutants on the cells is decreased by the stabilising effect of the Ectoine®Hydro Complex. It protects the cells from inflammation caused by environmental stress factors like dehydration, UV radiation, tensides or airborne particles.
The Ectoine®Hydro Complex protects the membrane and prevents the release of stress mediators (e.g. ceramides), which mediate inflammatory processes. Therefore inflammation can be limited (Figure 5).

Ectoine® natural is an extremely hydrophilic hygroscopic (KOSMOTROPIC) substance that increases the number of adjacent water molecules and strengthens the cross-linking structure of water. It can stabilize and protect biological molecules such as proteins, peptides, and enzymes, as well as stabilize and protect cell membranes. It has a wide range of effective applications and commercial uses in the pharmaceutical and cosmetics markets. This product has the highest purity specifications in the market and has undergone multiple clinical trials. It has obtained ECOCERT COSMOS and NATRUE international certifications for natural standards, providing customers with the highest quality products and comprehensive technical services.