Novel oligonucleotide that interacts with a gene encoding tyrosinase-related protein-1 (TRP-1) to regulate its expression, and use of the oligonucleotide as a depigmenting agent

摘要

Anti-gene oligonucleotide comprising nucleotide sequence, where the oligonucleotide specifically hybridizes with the gene coding for human tyrosinase related protein-1 by Hoogsteen base pairing, and forms a triple helix structure with the human tyrosinase gene related protein-1, is new. Anti-gene oligonucleotide comprising a nucleotide sequence n, where the oligonucleotide specifically hybridizes with the gene coding for human tyrosinase related protein-1 by Hoogsteen base pairing, and forms a triple helix structure with the human tyrosinase gene related protein-1, is new. n : 10-25, preferably 16 (where n is 10-16, then the oligonucleotide sequence is n nucleotide comprising 5'-CTTC*CTTTTTTTTC*TT-3' (SEQ ID NO: 1 and C* is 5-methyl-cytosine), and n is 17-25, then the oligonucleotide sequence comprising 5'-CTTC*CTTTTTTTTC*TT-3' (SEQ ID NO:1, and C* is 5-methyl-cytosine)). Independent claims are included for: (1) a cosmetic or dermatological composition, comprising the oligonucleotide; and (2) a cosmetic treatment process for depigmenting or lightening the skin or body hair, comprises applying the composition on the pigmented areas of the skin or hairy zone of the skin for a determined duration, optionally repeating until the appearance of depigmenting effect. ACTIVITY : Dermatological; Cytostatic; Nootropic; Vulnerary. MECHANISM OF ACTION : Tyrosinase related protein-1 gene expression inhibitor. The ability of the oligonucleotide to inhibit the tyrosinase related protein-1 gene expression was tested in human melanocytes. The result showed that the oligonucleotide (SEQ ID NO: 2 (14416 5'-C+TT+C*C+TT+TT+TT+TT+C*T+T+-3' 14431)) (where C* is 5-methyl cytosine, C+ is LNA-dC, and the T+ is LNA-T) exhibited decreased the dopa-oxidase activity to 40% at 500 nm.