Department of Dermatology and Venereology, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, China.
Department of Urinary Surgery, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, China.
Phytother Res. 2019 Jan;33(1):205-213. doi: 10.1002/ptr.6218. Epub 2018 Nov 12.
Puerarin is the major bioactive ingredient derived from the root of the Pueraria lobata (Willd.), and its antioxidative stress effects have been demonstrated in several previous studies. Moreover, Puerarin can upregulate melanin synthesis and microphthalmia-associated transcription factor (MITF) transcription by increasing cAMP level of intracellular cyclic adenosine monophosphate. Vitiligo is an acquired cutaneous disorder of pigmentation, and the pathogenesis has remained elusive. Current treatment modalities are directed towards achieving repigmentation. In this study, we found that after treating with puerarin at various concentrations of 40 μmol/L, the melanin content of human melanocytes increased significantly and the apparent level of protein and the RNA levels of MITF, tyrosinase (TYR), and tyrosinase-related protein 1 (TRP-1) were also increased. Further, puerarin was shown to inhibit phosphorylation and activation of extracellular signal-regulated kinase 1 and 2 (ERK1/2) without significantly affecting p38 and c-Jun N-terminal kinase phosphorylation. These results demonstrated that puerarin stimulated melanogenesis in human melanocytes via inhibition of ERK1/2 signaling pathways, which leads to upregulation of MITF and TYR as well as TRP-1 subsequently. Additionally, mice vitiligo models with puerarin treatment showed lighter pathological changes. Therefore, we suggested that puerarin might be a potential medicine for vitiligo.
葛根素是从野葛(Willd.)的根部提取的主要生物活性成分,已有多项研究表明其具有抗氧化应激作用。此外,葛根素可以通过增加细胞内环磷酸腺苷(cAMP)水平来上调黑色素合成和小眼畸形相关转录因子(MITF)转录。白癜风是一种获得性色素沉着皮肤疾病,其发病机制仍不清楚。目前的治疗方法旨在实现复色。在这项研究中,我们发现,用不同浓度的葛根素(40 μmol/L)处理后,人黑素细胞中的黑色素含量显著增加,MITF、酪氨酸酶(TYR)和酪氨酸酶相关蛋白 1(TRP-1)的蛋白和 RNA 水平也明显增加。此外,葛根素抑制细胞外信号调节激酶 1 和 2(ERK1/2)的磷酸化和激活,而对 p38 和 c-Jun N-末端激酶(JNK)的磷酸化没有明显影响。这些结果表明,葛根素通过抑制 ERK1/2 信号通路刺激人黑素细胞中的黑色素生成,从而随后上调 MITF、TYR 和 TRP-1。此外,用葛根素治疗的小鼠白癜风模型显示出较轻的病理变化。因此,我们认为葛根素可能是一种治疗白癜风的潜在药物。