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

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 r...

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Published in:International journal of molecular sciences 2011-11, Vol.12 (11), p.8208-8216
Main Authors: Qian, Li-Hua, Li, Nian-Guang, Tang, Yu-Ping, Zhang, Li, Tang, Hao, Wang, Zhen-Jiang, Liu, Li, Song, Shu-Lin, Guo, Jian-Ming, Ding, An-Wei
Format: Article
Language:English
Subjects:
Animals
antioxidant activity
Antioxidants
Apigenin - pharmacology
Atmosphere
Benzothiazoles - metabolism
Bioavailability
Biphenyl Compounds - metabolism
Cell Survival - drug effects
Cerebrovascular disease
Cerebrovascular diseases
Cerebrovascular Disorders - drug therapy
Chromatography
Cytotoxicity
Ethanol
Free Radical Scavengers - pharmacology
Free radicals
Glucuronates - pharmacology
Hydrogen Peroxide - adverse effects
Ischemia
Ischemia - drug therapy
ischemic cerebrovascular disease
Metabolites
Oral administration
PC12 Cells
Pheochromocytoma cells
Picrates - metabolism
Rats
scutellarein
scutellarin
Solubility
Sulfonic Acids - metabolism
synthesis
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Summary: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.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms12118208