期刊
EXPERIMENTAL DERMATOLOGY
卷 31, 期 8, 页码 1177-1187出版社
WILEY
DOI: 10.1111/exd.14569
关键词
epidermis; hyperpigmentation; melanocytes; skin whitening agents; tyrosinase
类别
资金
- National Nanotechnology Center [P1752418]
- National Science and Technology Development Agency (NSTDA)
- Thailand Graduate Institute of Science and Technology (TGIST) Scholarship from NSTDA [SCA-CO-2562-9832-TH]
Through a series of experiments, we identified two compounds with anti-pigmentation activity and an interaction with tyrosinase. These findings provide an alternative approach for the development of skin-whitening products that do not require animal testing.
Skin hyperpigmentation is commonly treated by topical drug application. Several naturally occurring compounds exhibit attractive biological effects including anti-melanogenic activity. Chemically modified derivatives of those compounds are expected to be more efficient. However, efficacy and safety testing processes are of significant consideration to identify the most effective compound among them. Herein, we demonstrated a tiered approach to investigate the antipigmentation activity of 17 trans-N-coumaroyltyramine derivatives. First, we evaluated the in chemico antityrosinase activity, then the cytotoxicity of the most potent derivatives using a mitochondrial activity-based assay, followed with the in vitro anti-melanogenic activity in two dimensional (2D) monolayer human melanocytes. The selected derivatives were topically applied on a three dimensional (3D) pigmented-reconstructed human epidermis (pRhE) containing melanocytes and keratinocytes to evaluate their depigmenting activity. Two of the 17 derivatives displayed a significant reduction in pigmentation in the 3D pRhE, comparable to kojic acid, a known tyrosinase inhibitor. In addition, a molecular docking experiment indicated an interaction of the three derivatives and tyrosinase, suggesting that these derivatives have potent anti-melanogenic activity through tyrosinase inhibition. Our findings provide an alternative approach for investigating skin-whitening agents, thereby facilitating the research and development of skin-whitening products that need not be tested on animals.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据