201. Synthesis of scutellarein derivatives to increase biological activity and water solubility.
- Author
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Shi ZH, Li NG, Shi QP, Zhang W, Dong ZX, Tang YP, Zhang PX, Gu T, Wu WY, Fang F, Xin-Xue, Li HM, Yang JP, and Duan JA
- Subjects
- Animals, Anticoagulants chemical synthesis, Anticoagulants chemistry, Anticoagulants pharmacology, Antioxidants chemistry, Antioxidants pharmacology, Apigenin chemical synthesis, Apigenin pharmacology, Fibrinogen metabolism, Hydrogen Peroxide toxicity, Oxidative Stress drug effects, PC12 Cells, Prothrombin Time, Rats, Solubility, Thrombin antagonists & inhibitors, Thrombin metabolism, Thrombin Time, Antioxidants chemical synthesis, Apigenin chemistry
- Abstract
In order to improve the biological activity and water solubility of scutellarin (1), some derivatives of its main metabolite (scutellarein) were designed and synthesized. All the compounds were tested for their thrombin inhibition activity through the analyzation of thrombin time (TT), activated partial thromboplastin time (APTT), prothrombin time (PT) and fibrinogen (FIB). Their antioxidant activities were assessed by measuring their scavenging capacities toward 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and the ability to protect PC12 cells against H2O2-induced cytotoxicity, their water solubility were also assessed by ultraviolet (UV) spectrophotometer. The results showed that compound 8b demonstrated stronger anticoagulant and antioxidant activity, better water solubility compared with scutellarein (2), which warrants it as a promising agent for the treatment of ischemic cerebrovascular disease., (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Published
- 2015
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