loading page

A non-retinol RAR-γ selective agonist-tectorigenin can effectively inhibit the UV-induced skin damage
  • +8
  • Hui-Juan Liu,
  • Xintong Dai,
  • Jing Jin,
  • Yan Jia,
  • Kai Yang,
  • Jingxia Han,
  • Zhiyuan Zhang,
  • Xiujuan Ding,
  • Cheng Yao,
  • Tao Sun,
  • Caibin Zhu
Hui-Juan Liu
Nankai University

Corresponding Author:[email protected]

Author Profile
Xintong Dai
Nankai University
Author Profile
Jing Jin
Cheermore Cosmetic Dermatology Laboratory
Author Profile
Yan Jia
Nankai University
Author Profile
Kai Yang
Cheermore Cosmetic Dermatology Laboratory
Author Profile
Jingxia Han
Nankai University
Author Profile
Zhiyuan Zhang
Nankai University
Author Profile
Xiujuan Ding
Nankai University
Author Profile
Cheng Yao
Cheermore Cosmetic Dermatology Laboratory
Author Profile
Tao Sun
Nankai University
Author Profile
Caibin Zhu
Cheermore Cosmetic Dermatology Laboratory
Author Profile

Abstract

Background and Purpose: Long-term Ultraviolet (UV) exposure can cause inflammation, pigmentation, and photoaging damage.Retinoic acid drugs are commonly used RAR agonists in the clinical treatment of UV-induced skin problems, but the use of such drugs is often accompanied by some systemic adverse reactions caused by nonspecific activation of RARs. Therefore, this study is expected to screen a novel RAR-γ selective agonist with high safety Experimental Approach: Molecular docking, dynamic simulation and Biacore were used to screen and obtain a novel RAR- γ selective agonists. RT‐PCR , ELISA, western blot, immunofluorescence staining, flow cytometry and proteome analysis were used to detect the effects of novel RAR-γ selective agonists on UV-induced inflammation and photoaging cell model. UV-induced mouse models and volunteer skin tests were used to evaluate the effects of TEC on skin repair, aging and inflammation. Key Results: TEC is a novel RAR-γ selective agonist. TEC can inhibit UV-induced oxidative damage, inflammatory factor release, and MMPs production. TEC can also reverse the loss of collagen induced by UV. The results of signaling pathway research showed that TEC mainly affect the MAPK/JNK/AP-1 pathway. Nanoparticle-loaded TEC, which significantly improved the effect of TEC, was also presented. TEC can reduce inflammation areas and facial wrinkles and caused less skin irritation than tretinoid (TRE). Conclusions and Implications: TEC is a non-retinol RAR-γ selective agonist, which can inhibit UV-induced skin damage and may be developed as a safe pharmaceutical component for the prevention of photoaging and skin inflammation.