Advanced Hair Research Laboratory, AMOREPACIFIC Corp. R&D Unit, Gyeonggi Province, South Korea.
Analysis Research Team, AMOREPACIFIC Corp. R&D Unit, Gyeonggi Province, South Korea.
Planta Med. 2014 Feb;80(2-3):153-8. doi: 10.1055/s-0033-1360300. Epub 2014 Feb 4.
Androgens affect several human skin and prostate functions, and the androgen receptor is crucial for regulating the androgen-related mechanisms. In this study, we assessed the antagonizing effects of a Scutellaria baicalensis extract and its main component baicalin on proliferation of human scalp dermal papilla cells. First, the extract and baicalin slightly dissociated the radioisotope-labeled androgen receptor-agonist complex in the androgen receptor binding assay, and the IC50 values were measured to assess the androgen receptor antagonistic effect of the extract (93 µg/mL) and baicalin (54.1 µM). Second, the extract and baicalin treatments dose-dependently inhibited the overgrowth of LNCaP prostate cancer cells, which were stimulated by dihydrotestosterone. Third, the extract and baicalin inhibited nuclear translocation of the androgen receptor stimulated by dihydrotestosterone in human dermal papilla cells. Additionally, the extract and baicalin enhanced proliferation of human dermal papilla cells in vitro. These results show that the extract and baicalin inhibited androgen activation signaling and promoted hDPC proliferation, suggesting that they could be used as active ingredients for treating androgen-associated disorders, such as androgenetic alopecia.
雄激素影响多种人类皮肤和前列腺功能,而雄激素受体对于调节雄激素相关机制至关重要。在这项研究中,我们评估了黄芩提取物及其主要成分黄芩苷对人头皮真皮乳头细胞增殖的拮抗作用。首先,提取物和黄芩苷在雄激素受体结合测定中轻微解离放射性同位素标记的雄激素受体激动剂复合物,并且测量 IC50 值以评估提取物(93µg/mL)和黄芩苷(54.1µM)的雄激素受体拮抗作用。其次,提取物和黄芩苷处理剂量依赖性地抑制了二氢睾酮刺激的 LNCaP 前列腺癌细胞的过度生长。第三,提取物和黄芩苷抑制了二氢睾酮刺激的人真皮乳头细胞中雄激素受体的核转位。此外,提取物和黄芩苷增强了人真皮乳头细胞在体外的增殖。这些结果表明,提取物和黄芩苷抑制了雄激素激活信号,并促进了 hDPC 的增殖,提示它们可被用作治疗雄激素相关疾病(如雄性激素性脱发)的活性成分。