2. Academic Validation
  3. Synthesis and bio-activity evaluation of scutellarein as a potent agent for the therapy of ischemic cerebrovascular disease

Synthesis and bio-activity evaluation of scutellarein as a potent agent for the therapy of ischemic cerebrovascular disease

  • Int J Mol Sci. 2011;12(11):8208-16. doi: 10.3390/ijms12118208.
Li-Hua Qian 1,  Nian-Guang Li,  Yu-Ping Tang,  Li Zhang,  Hao Tang,  Zhen-Jiang Wang,  Li Liu,  Shu-Lin Song,  Jian-Ming Guo,  An-Wei Ding
Affiliations

Affiliation

  • 1 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.).
PMID: 22174659 DOI: 10.3390/ijms12118208
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.

Keywords

antioxidant activity; ischemic cerebrovascular disease; scutellarein; scutellarin; synthesis.

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