Antimicrobial amino acid sequences derived from...

A - Human Necessities – 61 – K

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A61K 38/04 (2006.01) A61K 9/00 (2006.01) A61K 38/07 (2006.01) A61K 38/34 (2006.01)

Patent

CA 2368387

The peptide a-melanocyte stimulating hormone (a-MSH) is found in barrier organs such as the gut and skin. The anti-inflammatory properties of the peptide make it useful for treating inflammation in human and veterinary disorders. It has been found that this peptide, and other peptides derived from a-MSH, possess antimicrobial activity against Staphylococcus aureus and Candida albicans. These a-MSH peptides exhibited antimicrobial effects over a broad concentration range, including the physiological (picomolar)range. Of particular interest are those peptides that include the amino acid sequence KPV, or those including the sequence MEHFRWG. Peptides having the most potent antimicrobial activity were those bearing the C-terminal amino acid sequence of a-MSH. Anti-inflammatory agents based on a-MSH peptides, with enhanced antimicrobial activity, would minimize the risk of further infection that is generally associated with treatments using coticosteroids or other nonsteroidal anti-inflammatory drugs.

L'hormone de stimulation des a-melsanocytes (a-MSH) se rencontre dans des organes d'arrêt tels que les intestins et la peau. Grâce à ses propriétés anti-inflammatoires, ce peptide convient pour le traitement anti-inflammatoire de troubles chez l'homme et l'animal. On a constaté que ce peptide, comme d'autres peptides tirés de a-MSH, possède une activité anti-microbienne contre Staphylococcus aureus et le Candida albicans. Ces peptides a-MSH ont des effets anti-microbiens sur une vaste plage de concentrations, dont la plage physiologique (picomolaire). Les peptides qui renferment la séquence d'acides aminés KPV ou bien la séquence MEHFRWG offrent un intérêt particulier. Les peptides présentant l'activité anti-microbienne la plus puissante sont ceux qui portent la séquence d'acides aminés à terminal C de a-MSH. L'emploi d'agents anti-inflammatoires à base de peptides a-MSH peptides, avec activité anti-microbienne accrue, devrait réduire les risques de surinfection généralement associés à des traitements aux corticostéroïdes et autres médicaments anti-inflammatoires non stéroïdiens.

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