Design, Synthesis, and Biological Evaluation of Scutellarein Derivatives Based on Scutellarin Metabolic Mechanism In Vivo

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• 作者：Ze-Xi Dong ; Zhi-Hao Shi ; Nian-Guang Li ; Wei Zhang ; Ting Gu ; Peng-Xuan Zhang ; Wen-Yu Wu ; Yu-Ping Tang ; Fang Fang ; Xin Xue ; He-Min Li ; Hai-Bo Cheng ; Jian-Ping Yang and Jin-Ao Duan
• 刊名：Chemical Biology & Drug Design
• 出版年：2016
• 出版时间：June 2016
• 年：2016
• 卷：87
• 期：6
• 页码：946-957
• 全文大小：816K
• ISSN：1747-0285

文摘

Three series of scutellarein derivatives have been designed and synthesized based on metabolic mechanism of scutellarin (1) in vivo. Their thrombin inhibition activities were tested through the analyzation of prothrombin time (PT), activated partial thromboplastin time (APTT), thrombin time (TT), and fibrinogen (FIB). The antioxidant activities of these target products were assessed by 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) assay and the ability to protect PC12 cells against H₂O₂-induced cytotoxicity, and their solubilities were evaluated by ultraviolet (UV) spectrophotometer. The results showed that the two isopropyl groups substituted derivative (18c) demonstrated stronger anticoagulant activity, better water solubility, and good antioxidant activity compared with scutellarein (2), which warrants further development of 18c as a promising agent for ischemic cerebrovascular disease treatment.