Method and compositions for reducing cholesterol absorption

A - Human Necessities – 61 – K

Patent

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Details

A61K 38/46 (2006.01) A61K 51/04 (2006.01) C12N 9/20 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2206526

Compositions derived from all or a portion of the carboxy terminal region of human bile salt-activated lipase (BAL) are described, which, when orally ingested, compete with native BAL in binding to the intestinal surface, thus reducing the physiological role of BAL in mediating the transfer of cholesterol into the intestinal cells, and, as a result, reducing the amount of cholesterol absorbed from the intestine into the blood stream. Useful derivatives of the carboxy terminal region of BAL are derived from all or portion of the region containing amino acid residues 539 to 722, and have a mucin-like structure containing at least three of the repeating proline-rich units of eleven amino acid residues each.

Compositions dérivées de la région intégrale ou partielle de l'extrémité carboxylique de la lipase activée par les sels biliaires humains (BAL). Lorsqu'elles sont administrées par voie orale, ces compositions concurrencent la BAL à l'état natif en se liant à la paroi de l'intestin, ce qui réduit le rôle physiologique de la BAL dans la médiation du transport de cholestérol dans les cellules intestinales, d'où une réduction de la quantité de cholestérol absorbée par l'intestin et introduite dans le courant sanguin. Les dérivés utiles de la région de l'extrémité carboxylique de la BAL, sont dérivés de la région intégrale ou partielle contenant les restes d'acide aminé en position 539 à 722 et ont une structure semblable à celle de la mucine et contiennent au moins trois des unités récurrentes riches en proline comportant chacune onze restes d'acide aminé.

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