Enhancement of the pro-fertility action of a molecule...

A - Human Necessities – 61 – K

Patent

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A61K 38/00 (2006.01) A61K 38/16 (2006.01) A61K 38/18 (2006.01) C07K 14/475 (2006.01)

Patent

CA 2322666

A synthetic peptide with enhanced pro-fertility action was produced by inclusion of additional amino acids at the carboxyl end of a previously disclosed synthetic peptide. Improvement in bioactivity over the previously disclosed peptide was demonstrated. A direct comparison of an earlier known synthetic peptide and said extended peptide involved brief exposure of sperm in vitro to one or the other peptide at several concentrations. When sperm then were evaluated in vitro using an egg-membrane substrat e, an increased percentage of sperm bound for cells exposed to the new extended peptide. Similarly, when fertility of sperm after artificial insemination was the criterion, a greater percentage of eggs was fertilized by sperm exposed to the new extended peptide. In one preferred embodiment, this enhanced pro-fertility action was achieved with a peptide having a 68 amino acid sequence (SEQ ID NO:1): Cys- Gln-Ser- Leu-Gln-Glu-Tyr- Leu-Ala-Glu-Gln- Asn-Gln-Arg-Gln- Leu- Glu-Ser- Asn-Lys-Ile-Pro- Glu-Val-Asp-Leu- Ala-Agr-Val-Val-Ala-Pro-Phe-Met-Ser- Asn-Ile-Pro-Leu-Leu-Leu-Tyr-Pro-Gln-Asp-Arg-Pro-Arg-Ser-Gln-Pro-Gln-Pro-Lys- Ala-Asn-Glu-Asp-Val-Cys-Val-Asn-His-His-His-His-His-His.

La présente invention concerne un peptide synthétique à action de pro-fertilité, produit par l'adjonction d'acides aminés supplémentaires au niveau de l'extrémité carboxyle d'un peptide synthétique déjà décrit et dont l'amélioration apportée à sa bioactivité a déjà été démontrée. Une comparaison directe entre un peptide synthétique déjà connu et ledit peptide étendu consiste à exposer brièvement in vitro du sperme à l'un ou l'autre peptide avec différentes concentrations. Lors de l'évaluation in vitro du sperme, en utilisant un substrat de membrane d'ovule, on remarque qu'un pourcentage élevé de sperme s'est fixé aux cellules exposées au nouveau peptide étendu. De même, lorsque la fécondité du sperme après insémination artificielle était le critère requis, un plus grand pourcentage d'ovules a été fertilisé par le sperme exposé au nouveau peptide étendu. Dans un mode préféré de réalisation, cette action perfectionnée de pro-fertilité a été effectuée avec un peptide composé de 68 séquences d'acides aminés (SEQ ID NO:1):Cys- GLn-Ser- Leu-GLn-GLu-Tyr- Leu-ALa-GLu-GLn- Asn-GLn-Arg-GLn- Leu-GLu-Ser- Asn-Lys-ILe-Pro- GLu-VaL-Asp-Leu- ALa-Agr-Val-Val-Ala-Pro-Phe-Met-Ser-Asn-ILe-Pro-Leu-Leu-Leu-Tyr-Pro-GLn-Asp-Arg-Pro-Arg-Ser-GLn-Pro-GLn-Pro-Lys-ALa-Asn-Glu-Asp-Val-Cys-Val-Asn-His-His-His-His-His-His.

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