The Guanidine Pseudoalkaloids 10-Methoxy-Leonurine and Leonurine Act as Competitive Inhibitors of Tyrosinase

Biomolecules

GaYoung Lee¹  HyunHee Leem²  JangHoon Kim³ 

[1] Hephzibah Korea Lnc, Techno 10-ro, Yuseong-gu, Daejeon 34036, Korea;National Development Institute of Korean Medicine, Gyeongsan 38573, Korea;Research Institute for Basic Sciences, JeJu National University, Jeju 63243, Korea;

关键词: leonurus japonicas;    guanidine pseudoalkaloid;    tyrosinase;    competitive inhibitor;    lead compound;   

DOI  :  10.3390/biom10020174

来源: DOAJ

【 摘 要 】

Tyrosinase plays a key role in the production of melanin. A variety of industrial fields have shown interest in the development of tyrosinase inhibitors from plants. In this study, compounds 1−5 derived from Leonurus japonicas were evaluated to determine their ability to inhibit tyrosinase. Of these, 10-methoxy-leonurine (1) and leonurine (2) exhibited IC₅₀ values of 7.4 ± 0.4 and 12.4 ± 0.8 μM, respectively, and acted as competitive inhibitors of tyrosinase, with Ki values in the micromolar range. In silico modeling revealed a guanidine group located in the inner cavity and a benzene ring docked within the active site of these compounds. These guanidine pseudoalkaloids show potential not only as tyrosinase inhibitors but also as lead compounds in new scaffolds for the development of novel inhibitors.

【 授权许可】

Unknown