透明质酸酶
齐墩果酸
药剂师
吲哚试验
化学
化妆品
药理学
生物化学
酶
IC50型
体外
医学
有机化学
化妆品
病理
替代医学
作者
Hao He,Huifang Li,Toyosi Akanji,Shengli Niu,Zhujun Luo,Dongli Li,Navindra P. Seeram,Panpan Wu,Hang Ma
标识
DOI:10.1080/14756366.2021.1956487
摘要
Oleanolic acid (OA) is a natural cosmeceutical compound with various skin beneficial activities including inhibitory effect on hyaluronidase but the anti-hyaluronidase activity and mechanisms of action of its synthetic analogues remain unclear. Herein, a series of OA derivatives were synthesised and evaluated for their inhibitory effects on hyaluronidase. Compared to OA, an induction of fluorinated (6c) and chlorinated (6g) indole moieties led to enhanced anti-hyaluronidase activity (IC50 = 80.3 vs. 9.97 and 9.57 µg/mL, respectively). Furthermore, spectroscopic and computational studies revealed that 6c and 6g can bind to hyaluronidase protein and alter its secondary structure leading to reduced enzyme activity. In addition, OA indole derivatives showed feasible skin permeability in a slightly acidic environment (pH = 6.5) and 6c exerted skin protective effect by reducing cellular reactive oxygen species in human skin keratinocytes. Findings from the current study support that OA indole derivatives are potential cosmeceuticals with anti-hyaluronidase activity.
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