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Witten, Germany

Held C.,TU Dortmund | Neuhaus T.,Bitop AG | Sadowski G.,TU Dortmund
Biophysical Chemistry | Year: 2010

Compatible solutes like ectoine and its derivatives are deployed by halophile organisms as osmolytes to sustain the high salt concentration in the environment. This work investigates the relation of the thermodynamic properties of compatible solutes and their impact as osmolytes. The ectoines considered in this work are ectoine, hydroxyectoine, and homoectoine. Besides solution densities (15-45. °C) and solubilities in water (3-80. °C), component activity coefficients in the aqueous solutions were determined in the temperature range between 0 and 50. °C. The latter is important for adjusting a certain water activity and therewith a respective osmotic pressure within a cell. The characteristic effect of ectoines is compared to that of prolines, as well as to that of incompatible solutes as salts and urea. The experimental results show that the influence on the activity (coefficient) of water is quite different for compatible and incompatible solutes: whereas compatible solutes cause decreasing water activity coefficients, incompatible solutes lead to an increase in water activity coefficients. Based on this quantity, the paper discusses the impact of various osmolytes on biological systems and contributes to the explanation why some osmolytes are more often and at other temperatures used than others. Moreover, it was found that the anti-stress effect of an osmolyte is weakened in the presence of a salt.Finally, it is shown that the thermodynamic properties of compatible solutes can be modeled and even predicted using the thermodynamic model PC-SAFT (Perturbed-Chain Statistical Associating Fluid Theory). © 2010 Elsevier B.V. Source


Abdel-Aziz H.,Cairo University | Wadie W.,Cairo University | Abdallah D.M.,Cairo University | Lentzen G.,Bitop AG | Khayyal M.T.,Cairo University
Phytomedicine | Year: 2013

Evidence suggests an important role of intestinal barrier dysfunction in the etiology of inflammatory bowel disease (IBD). Therefore stabilizing mucosal barrier function constitutes a new therapeutic approach in its management. Ectoine is a compatible solute produced by aerobic chemoheterotrophic and halophilic/halotolerant bacteria, where it acts as osmoprotectant and effective biomembrane stabilizer, protecting the producing cells from extreme environmental stress. Since this natural compound was also shown to prevent inflammatory responses associated with IBD, its potential usefulness was studied in a model of colitis. Groups of rats were treated orally with different doses of ectoine (30-300 mg/kg) or sulfasalazine (reference drug) daily for 11 days. On day 8 colitis was induced by intracolonic instillation of 2,4,6-trinitrobenzenesulfonic acid, when overt signs of lesions develop within the next 3 days. On day 12, blood was withdrawn from the retro-orbital plexus of the rats and the animals were sacrificed. The colon was excised and examined macroscopically and microscopically. Relevant parameters of oxidative stress and inflammation were measured in serum and colon homogenates. Induction of colitis led to marked weight loss, significant histopathological changes of the colon, and variable changes in levels of myeloperoxidase, reduced glutathione, malondialdehyde, and all inflammatory markers tested. Treatment with ectoine ameliorated the inflammatory changes in TNBS-induced colitis. This effect was associated with reduction in the levels of TNF-α, IL-1β, ICAM-1, PGE2 and LTB4. The findings suggest that intestinal barrier stabilizers from natural sources could offer new therapeutic measures for the management of IBD. © 2013 Elsevier GmbH. Source


The present invention relates to osmolyte-containing preparations for the local treatment of dry mucous membranes. It describes the use of osmolytes for the production of a medicament, medical product or cosmetic product for the prevention, therapy and/or care of dry mucous membranes. The present invention relates to topical compositions based on osmolytes to which sodium chloride and/or moisturizers can optionally be added. The group of osmolytes proposed by the invention embraces various low-molecular substances, in particular ectoine, homoectoine, hydroxyectoine, di-myo-inositol phosphate (DIP), cyclic 2,3-diphosphoglycerate (cDPG), 1,1-di-glycerol phosphate (DGP), -mannosylglycerate (Firoin), -mannosylglyceramide (Firoin-A), di-mannosyl di-inositol phosphate (DMIP), glucosylglycerol and/or a derivative, e.g. an acid, salt or ester, of these compounds.


Patent
Bitop Ag | Date: 2012-09-07

The invention relates to a composition containing ectoine, hydroxyectoine and/or a salt, ester or amide of these compounds for the suppression of anti-apoptotic signals to neutrophil granulocytes and other cells taking part in inflammations. The delayed apoptosis of the neutrophils is a main component for various types of inflammation. Through the administration of ectoine restoring the normal rate of apoptosis is accomplished at least partially which is associated with a corresponding improvement of the inflammatory phenomena.


Patent
bitop AG | Date: 2013-03-15

The invention relates to a storage solution for the preservation of organs, tissue or organ systems to be transplanted, said solution being based on the known HTK, UW or Celsior solutions. In accordance with the invention it has been determined that ischemia and reperfusion injury could be reduced through the addition of ectoine or hydroxyectoine.

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