title: Synthesis of scutellarein derivatives to increase biological activity and water solubility.
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.
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China; Department of Organic Chemistry, China Pharmaceutical University, Nanjing, Jiangsu 211198, China.
authors.forename: Zhi-Hao
authors.initials: ZH
authors.lastname: Shi
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China. Electronic address: linianguang@njutcm.edu.cn.
authors.forename: Nian-Guang
authors.initials: NG
authors.lastname: Li
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Qian-Ping
authors.initials: QP
authors.lastname: Shi
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Ze-Xi
authors.initials: ZX
authors.lastname: Dong
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China. Electronic address: yupingtang@njutcm.edu.cn.
authors.forename: Yu-Ping
authors.initials: YP
authors.lastname: Tang
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Peng-Xuan
authors.initials: PX
authors.lastname: Zhang
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Ting
authors.initials: T
authors.lastname: Gu
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Wen-Yu
authors.initials: WY
authors.lastname: Wu
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Fang
authors.initials: F
authors.lastname: Fang
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.lastname: Xin-Xue
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: He-Min
authors.initials: HM
authors.lastname: Li
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Jian-Ping
authors.initials: JP
authors.lastname: Yang
authors.affiliation: Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, and National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing 210023, China. Electronic address: dja@njutcm.edu.cn.
authors.forename: Jin-Ao
authors.initials: JA
authors.lastname: Duan
mesh_terms: D000818:Animals; D000925:Anticoagulants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000975:Antioxidants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D047310:Apigenin / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D005340:Fibrinogen / Q000378:metabolism; D006861:Hydrogen Peroxide / Q000633:toxicity; D018384:Oxidative Stress / Q000187:drug effects; D016716:PC12 Cells; D011517:Prothrombin Time; D051381:Rats; D012995:Solubility; D013917:Thrombin / Q000037:antagonists & inhibitors / Q000378:metabolism; D013918:Thrombin Time
chemical_list: D000925:Anticoagulants; D000975:Antioxidants; D047310:Apigenin; D005340:Fibrinogen; D006861:Hydrogen Peroxide; D013917:Thrombin; C458179:scutellarein
keywords: Antioxidant; Scutellarein; Scutellarin; Solubility; Thrombin