title: Design, Synthesis, and Biological Evaluation of Scutellarein Derivatives Based on Scutellarin Metabolic Mechanism In Vivo.
abstract: 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 H2 O2 -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.
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, 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 Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, 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 Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
authors.forename: Nian-Guang
authors.initials: NG
authors.lastname: Li
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, 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 Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, 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 Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, 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 Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, 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 Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
authors.forename: Yu-Ping
authors.initials: YP
authors.lastname: Tang
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, 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 Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
authors.forename: Xin
authors.initials: X
authors.lastname: Xue
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, 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: Key Laboratory of SATCM for Empirical Formulae Evaluation and Achievements Transformation, Nanjing University of Chinese Medicine, Nanjing, Jiangsu, 210023, China.
authors.forename: Hai-Bo
authors.initials: HB
authors.lastname: Cheng
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, 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 Key Laboratory for High Technology Research of TCM Formulae, Jiangsu Collaborative Innovation Center of Chinese Medicine Resources Industrialization, National and Local Collaborative Engineering Center of Chinese Medicine Resources, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
authors.forename: Jin-Ao
authors.initials: JA
authors.lastname: Duan
mesh_terms: D000818:Animals; D000925:Anticoagulants / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D047310:Apigenin / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D002545:Brain Ischemia / Q000188:drug therapy / Q000378:metabolism; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D018696:Neuroprotective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D016716:PC12 Cells; D051381:Rats
chemical_list: D000925:Anticoagulants; D000975:Antioxidants; D018696:Neuroprotective Agents; D047310:Apigenin; C458179:scutellarein
keywords: antioxidant; scutellarein; scutellarin; solubility; thrombin