Yunnan Botanee Bio-technology Group Co., Ltd., Yunnan, 650000, China; Shanghai Jiyan Bio-pharmaceutical Co., Ltd., Shanghai, 200000, China.
School of Pharmacy, Changzhou University, Changzhou, 213000, China.
Eur J Pharmacol. 2022 Oct 15;932:175231. doi: 10.1016/j.ejphar.2022.175231. Epub 2022 Aug 28.
Pterostilbene is a trans stilbene compound, which is an effective component of herbaceous plants such as Dalbergia woods and Vaccinium. Although pterostilbene has many uses in anti-inflammatory, anti-oxidant and anti-tumor, its whitening effect is drawing more and more attention, the mechanism of melanogenesis and melanosome transport still needs further study. In this research, we tried to further investigate how melanocyte melanogenesis is affected by pterostilbene and whether pterostilbene play a part in melanin transport. Our results showed that pterostilbene has a potent inhibitory effect on melanogenesis in B16F10 cells (3 μM, p < 0.001), in-vitro human skin (10 μM, p < 0.05) and zebrafish embryos (3 μM, p < 0.01). Besides, pterostilbene not only inhibited melanogenesis, but also inhibited melanocyte dendritic development and melanosome transport. Pterostilbene mainly plays a role by inhibiting cAMP/PKA/CREB signal pathway. After the cAMP/PKA/CREB signaling pathway was inhibited, tyrosinase activity and the expression of MITF, TYR, Rab27A, Rab17 and gp100 were decreased, which in turn suppressed melanogenesis, melanocyte dendritic development and melanosome transport. Our findings showed that pterostilbene can potently inhibit melanogenesis and melanosome transport, suggesting the applicability of pterostilbene in skin lightning. Therefore, a novel pharmacologic way to treat hyperpigmentation has been proposed.
紫檀芪是一种反式芪类化合物,是豆科和越橘属植物中的一种有效成分。虽然紫檀芪在抗炎、抗氧化和抗肿瘤方面有许多用途,但它的美白效果越来越受到关注,黑素生成和黑素小体运输的机制仍需要进一步研究。在这项研究中,我们试图进一步研究紫檀芪如何影响黑素细胞的黑素生成,以及紫檀芪是否在黑素体运输中发挥作用。我们的结果表明,紫檀芪对 B16F10 细胞(3 μM,p < 0.001)、体外人皮肤(10 μM,p < 0.05)和斑马鱼胚胎(3 μM,p < 0.01)的黑素生成有很强的抑制作用。此外,紫檀芪不仅抑制黑素生成,还抑制黑素细胞树突状发育和黑素小体运输。紫檀芪主要通过抑制 cAMP/PKA/CREB 信号通路发挥作用。cAMP/PKA/CREB 信号通路被抑制后,酪氨酸酶活性和 MITF、TYR、Rab27A、Rab17 和 gp100 的表达降低,从而抑制黑素生成、黑素细胞树突状发育和黑素小体运输。我们的研究结果表明,紫檀芪能有效抑制黑素生成和黑素小体运输,提示紫檀芪在皮肤美白方面的应用。因此,提出了一种治疗色素沉着过度的新的药理学方法。