Design and synthesis of aloe-emodin derivatives as potent anti-tyrosinase, antibacterial and anti-inflammatory agents
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- 作者：Jinbing Liu ; syuliujb@163.com" class="auth_mail" title="E-mail the corresponding author ; Fengyan Wu ; Changhong Chen
- 关键词：Aloe-emodin derivatives ; Tyrosinase inhibitory activities ; Antibacterial activity ; Anti-inflammatory activity
- 刊名：Bioorganic & Medicinal Chemistry Letters
- 出版年：2015
- 出版时间：15 November 2015
- 年：2015
- 卷：25
- 期：22
- 页码：5142-5146
- 全文大小：555 K
文摘
Twenty aloe-emodin derivatives were designed, synthesized, and their biological activities were evaluated. Some compounds displayed potent tyrosinase inhibitory activities, especially, compounds with thiosemicarbazide moiety showed more potent inhibitory effects than the other compounds. The structure–activity relationships (SARs) were preliminarily discussed. The inhibition mechanism of selected compounds 1 and 13 were investigated. The results showed compound 1 was reversible inhibitor, however, compound 13 was irreversible. Kinetic analysis indicated that compound 1 was competitive tyrosinase inhibitor. Furthermore, the antibacterial activities and anti-inflammatory activities of some selected compounds were also screened. The results showed that compound 3 exhibited more potent antibacterial activity than the aloe-emodin, compounds 5 and 6 possessed more potent anti-inflammatory activities than the diacerein.