title: Synthesis and bio-activity evaluation of scutellarein as a potent agent for the therapy of ischemic cerebrovascular disease.
abstract: Scutellarein, the main metabolite of scutellarin in vivo, has relatively better solubility, bioavailability and bio-activity than scutellarin. However, it is very difficult to obtain scutellarein in nature compared with scutellarin. Therefore, the present study focused on establishing an efficient route for the synthesis of scutellarein by hydrolyzing scutellarin. The in vitro antioxidant activities of scutellarein were evaluated by measuring its scavenging capacities toward DPPH, ABTS(+•), (•)OH free radicals and its protective effect on H(2)O(2)-induced cytotoxicity in PC12 cells using MTT assay method. The results showed that essential point to the synthesis was the implementation of H(2)SO(4) in 90% ethanol in N(2) atmosphere; scutellarein had stronger antioxidant activity than scutellarin. The results have laid the foundation for further research and the development of scutellarein as a promising candidate for ischemic cerebrovascular disease.
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210046, China; E-Mails:  nanzhongyilihua@139.com  (L.-H.Q.);  linianguang@163.com  (N.-G.L.);  15850534175@163.com  (H.T.);  tianruoxi@126.com  (Z.-J.W.);  liuli-44@163.com  (L.L.);  sshl2009@126.com  (S.-L.S.);  njuguo@njutcm.edu.cn  (J.-M.G.);  ltcmf@njutcm.edu.cn  (A.-W.D.).
authors.forename: Li-Hua
authors.initials: LH
authors.lastname: Qian
authors.forename: Nian-Guang
authors.initials: NG
authors.lastname: Li
authors.forename: Yu-Ping
authors.initials: YP
authors.lastname: Tang
authors.forename: Li
authors.initials: L
authors.lastname: Zhang
authors.forename: Hao
authors.initials: H
authors.lastname: Tang
authors.forename: Zhen-Jiang
authors.initials: ZJ
authors.lastname: Wang
authors.forename: Li
authors.initials: L
authors.lastname: Liu
authors.forename: Shu-Lin
authors.initials: SL
authors.lastname: Song
authors.forename: Jian-Ming
authors.initials: JM
authors.lastname: Guo
authors.forename: An-Wei
authors.initials: AW
authors.lastname: Ding
mesh_terms: D000818:Animals; D047310:Apigenin / Q000494:pharmacology*; D052160:Benzothiazoles / Q000378:metabolism; D001713:Biphenyl Compounds / Q000378:metabolism; D002470:Cell Survival / Q000187:drug effects; D002561:Cerebrovascular Disorders / Q000188:drug therapy; D016166:Free Radical Scavengers / Q000494:pharmacology*; D005965:Glucuronates / Q000494:pharmacology*; D006861:Hydrogen Peroxide / Q000009:adverse effects; D007511:Ischemia / Q000188:drug therapy*; D016716:PC12 Cells; D010851:Picrates / Q000378:metabolism; D051381:Rats; D013451:Sulfonic Acids / Q000378:metabolism
chemical_list: D052160:Benzothiazoles; D001713:Biphenyl Compounds; D016166:Free Radical Scavengers; D005965:Glucuronates; D010851:Picrates; D013451:Sulfonic Acids; C484876:scutellarin; C002502:2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid; D047310:Apigenin; D006861:Hydrogen Peroxide; C004931:1,1-diphenyl-2-picrylhydrazyl; C458179:scutellarein