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Use of molecular biologically produced, non-viral agents for the treatment of acne

机译:分子生物学生产的非病毒药物在治疗痤疮中的用途

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.
机译:使用通过分子生物学方法制备的非病毒活性剂(I)来治疗痤疮和痤疮样皮肤疾病,包括酒渣鼻,是新的。通过分子生物学方法制备的非病毒活性剂(I)在治疗痤疮和痤疮样皮肤疾病(包括酒渣鼻)中的用途。 (I)是反义寡核苷酸(ASON); (稳定的)核酶; (镜子)适体;嵌合RNA / DNA寡核苷酸;裸质粒DNA或包裹在脂质体中的DNA,尤其是对编码类固醇激素受体或类固醇激素代谢酶(尤其是雄激素受体和/或5α-还原酶)的基因具有特异性的ASON。活动:皮肤科;抗脂溢性。作用机理:反义抑制雄激素受体和/或5α-还原酶基因,因此雄激素诱导皮脂腺活性的刺激。当用0.1 MicroM睾丸激素(T)处理永生化的S295人皮脂细胞时,它们的增殖受到了明显的刺激。在用T处理之前,将细胞与1 MicroM的针对雄激素受体基因转录起始位点的寡核苷酸(S2)孵育4小时,从而消除了刺激作用;然后,在免疫印迹测定中受体表达的吸光度约为0.6,而未经T处理的细胞的吸光度约为1.2。寡核苷酸对细胞有毒性。

著录项

  • 公开/公告号DE10141443B4

    专利类型

  • 公开/公告日2007-02-01

    原文格式PDF

  • 申请/专利号DE2001141443

  • 发明设计人

    申请日2001-08-23

  • 分类号A61K48;A61K31/713;A61P17/10;

  • 国家 DE

  • 入库时间 2022-08-21 20:30:12

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