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 H2O2-induced cytotoxicity in PC12 cells using MTT assay method. The results showed that essential point to the synthesis was the implementation of H2SO4 in 90% ethanol in N2 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: scutellarein; scutellarin; synthesis; antioxidant activity; ischemic cerebrovascular disease
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Qian, L.-H.; Li, N.-G.; Tang, Y.-P.; Zhang, L.; Tang, H.; Wang, Z.-J.; Liu, L.; Song, S.-L.; Guo, J.-M.; Ding, A.-W. Synthesis and Bio-Activity Evaluation of Scutellarein as a Potent Agent for the Therapy of Ischemic Cerebrovascular Disease. Int. J. Mol. Sci. 2011, 12, 8208-8216.
Qian L-H, Li N-G, Tang Y-P, Zhang L, Tang H, Wang Z-J, Liu L, Song S-L, Guo J-M, Ding A-W. Synthesis and Bio-Activity Evaluation of Scutellarein as a Potent Agent for the Therapy of Ischemic Cerebrovascular Disease. International Journal of Molecular Sciences. 2011; 12(11):8208-8216.
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. 2011. "Synthesis and Bio-Activity Evaluation of Scutellarein as a Potent Agent for the Therapy of Ischemic Cerebrovascular Disease." Int. J. Mol. Sci. 12, no. 11: 8208-8216.