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Design, Synthesis, and Biological Evaluation of Scutellarein Derivatives Based on Scutellarin Metabolic Mechanism In Vivo
Author(s) -
Dong ZeXi,
Shi ZhiHao,
Li NianGuang,
Zhang Wei,
Gu Ting,
Zhang PengXuan,
Wu WenYu,
Tang YuPing,
Fang Fang,
Xue Xin,
Li HeMin,
Cheng HaiBo,
Yang JianPing,
Duan JinAo
Publication year - 2016
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12727
Subject(s) - scutellarin , chemistry , in vivo , partial thromboplastin time , thrombin time , antioxidant , prothrombin time , dpph , pharmacology , fibrinogen , combinatorial chemistry , biochemistry , chromatography , medicine , coagulation , surgery , biology , microbiology and biotechnology
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 H 2 O 2 ‐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.