| 摘要 |
Using a non-viral active agent (I), prepared by molecular biological methods, for treatment of acne and acneform skin disorders, including rosacea, is new. Use of a non-viral active agent (I), prepared by molecular biological methods, for treatment of acne and acneform skin disorders, including rosacea. (I) is an antisense oligonucleotide (ASON); (stabilized) ribozyme; (mirror) aptamer; chimeric RNA/DNA oligonucleotide; naked plasmid DNA or DNA encapsulated in a liposome, especially an ASON specific for a gene that encodes a steroid hormone receptor or steroid hormone metabolizing enzyme, particularly the androgen receptor and/or 5alpha -reductase. ACTIVITY : Dermatological; Antiseborrheic. MECHANISM OF ACTION : Antisense inhibition of the androgen receptor and/or 5alpha -reductase gene, and therefore androgen-induced stimulation of sebaceous gland activity. When S295 immortalized human sebocytes were treated with 0.1 MicroM testosterone (T) their proliferation was significanly stimulated. When the cells were incubated for 4 hours with 1 MicroM of the oligonucleotide (S2) directed against the transcription start site of the androgen receptor gene before treatment with T, the stimulatory effect was abolished; the absorbance in an immunoblotting assay for receptor expression was then about 0.6 compared with about 1.2 for cells not treated with T. The oligonucleotide was toxic for the cells. |
