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Compositions comprising complexes of proanthocyanidins with vegetable proteins

a technology of proanthocyanidins and complexes, which is applied in the field of complexes comprising proanthocyanidins and vegetable proteins, can solve the problems of complexes with animal proteins that can also give rise to ethical or religious problems in some patient populations, and are incapacity and dangerous

Inactive Publication Date: 2016-02-25
NOVINTETHICAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes a complex of pea protein and proanthocyanidins that is effective in treating disorders of the intestinal epithelium, such as Crohn's disease and ulcerative colitis. The complex has been found to be safe and devoid of liver toxicity. The pea protein and proanthocyanidins interact with each other to form a stable complex that has improved properties compared to the individual components. The complex can be formulated into various administration forms and can protect the intestinal mucosa against damage and infection.

Problems solved by technology

Diarrhoea is a symptom of many gastrointestinal disorders and is often incapacitating and dangerous, especially in children and the elderly.
Acute diarrhoea with an infectious cause is a serious problem in developing countries; it is believed to cause the death of at least 4 million children under 5 years old every year.
Moreover, the complexes known and available to date are obtained from protein materials of animal origin, with the consequent safety problems associated with the possible transmission of diseases such as BSE, or allergies, which are particularly common in the case of proteins derived from milk and eggs.
Complexes with animal proteins can also give rise to ethical or religious problems in some patient populations.

Method used

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  • Compositions comprising complexes of proanthocyanidins with vegetable proteins
  • Compositions comprising complexes of proanthocyanidins with vegetable proteins
  • Compositions comprising complexes of proanthocyanidins with vegetable proteins

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Complex

[0029]A) 10 g of pea protein (Dal Cin Gildo S.p.A.) is suspended in 200 g purified water. The pH of the suspension is adjusted from pH 6.3 to pH 4 with anhydrous citric acid, 20% sol. w / v in water. The suspension is left under stirring for 3 hours, and the temperature is increased to 30° C.

[0030]B) 10 g of proanthocyanidins (Grape Seed Dry Extract®, Indena Spa) is dissolved in 100 ml of purified water; the solution is prepared shortly before use, adjusting the pH from 6.7 to 4 with anhydrous citric acid, 20% sol. w / v in water, and heated to 30° C.; the dark red solution is added in portions to suspension A), still under stirring.

[0031]The complex in homogenous suspension that immediately forms is dark red, while the aqueous solution is reddish.

[0032]The suspension is kept under stirring for 3 hours, leaving the temperature to fall to 20° C.

[0033]Stirring is stopped and the suspension is left to stand for a further 8 hours, during which time it rapidly decants. ...

example 2

Biological Tests in Vitro

[0047]The efficiency of the barrier and the chemical stability of the complex of the invention were evaluated by comparison with commercial gelatin tannate (Tasectan®) in the intestinal epithelium using the well-established predictive model of Caco-2 cells, a cell line of the intestinal epithelium deriving from a colorectal adenocarcinoma (ATCC HTB 37) (Cell. Biol. Toxicol. 2005, 21(1) 1-26).

[0048]The paracellular flow and the barrier permeability of the compounds tested were determined.

[0049]Paracellular flow was determined by measuring the transepithelial electrical resistance (TEER), which provides a direct measurement of the barrier function and is a further parameter of the integrity of the barrier at the tight junctions.

[0050]The permeability of the barrier was measured by determining the passage of the Lucifer Yellow dye (Le Ferrec et al., Altern Lab Anim. 2001 November-December; 29(6):649-68; Hidalgo et al., Gastroenterology. 1989 March; 96(3):736-49...

example 3

Biological Tests in Vivo

[0053]The activity of the complex of proanthocyanidin obtained from Vitis vinifera and pea protein on the altered intestinal permeability and intestinal inflammation induced by lipopolysaccharide (LPS) was evaluated.

[0054]Groups of 8 male Wistar rats (200-225 g) have been used. After on overnight fast, the animals were injected intraperitoneally (IP) with 250 μL of sterile saline (NaCl 0.9%) containing or not (control) 1 mg / kg of lipopolysaccharide (LPS) from E. Coli. This dose has been previously shown to alter intestinal permeability and to release pro-inflammatory cytokines in the mucosa (TNFα, IL-1β, IFNγ (Moriez R,. Am J Pathol. 2005; 167(4):1071-9). Six hours later, the animals have been sacrificed and strips of jejunum were used for evaluation of TEER and FITC-dextran paracellular permeability. Other segments were also collected for other parameters of mucosal inflammation (myeloperoxidase-MPO).

[0055]Six hours after LPS administration, the rats were sa...

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Abstract

Disclosed is a complex of pea protein and proanthocyanidins for use in the treatment of disorders caused by alterations of the intestinal epithelial tissue.

Description

[0001]The invention relates to complexes of proanthocyanidins with a vegetable protein and their use as active ingredients in compositions for the treatment of gastrointestinal disorders, in particular disorders caused by alterations of the intestinal epithelial tissue (simple non-ciliated cylindrical epithelium).PRIOR ART[0002]Diarrhoea is a symptom of many gastrointestinal disorders and is often incapacitating and dangerous, especially in children and the elderly. Acute diarrhoea is mainly caused by intestinal infections, but can also be due to the use of medicaments or radiotherapy and to other pathological conditions (diverticulitis, heavy-metal poisoning, intestinal ischaemia, allergies and intolerances).[0003]Acute diarrhoea with an infectious cause is a serious problem in developing countries; it is believed to cause the death of at least 4 million children under 5 years old every year.[0004]Chronic diarrhoea is generally due to irritable bowel syndrome, coeliac disease or in...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K38/16A61K31/353A61K36/87A61K45/06
CPCA61K38/168A61K45/06A61K36/87A61K31/353A61K9/0095A61K36/22A61K36/45A61K36/48A61K47/14A61K47/22A61K47/36A61P1/00A61P1/12A61K2300/00A61K9/0056
Inventor ALONSO, MIGUEL ANGELDI FULVIO, MARCODI SCHIENA, MICHELE
Owner NOVINTETHICAL PHARMA
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