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
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黄芩素治疗缺血性脑血管病的合成及生物活性评价
DOI：
10.3390/ijms12118208
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发表时间：
2011-11-01
影响因子：
5.6
通讯作者：
Ding, An-Wei
中科院分区：
文献类型：
--
作者：
Qian, Li-Hua;Li, Nian-Guang;Ding, An-Wei
灯盏乙素是灯盏乙素在体内的主要代谢产物，具有较灯盏乙素更好的溶解度、生物利用度和生物活性。然而，与野黄芩苷相比，野黄芩苷元在自然界中的获得非常困难。因此，本研究旨在建立一条高效的水解野黄芩苷合成野黄芩苷元的路线。采用MTT法测定灯盏乙素对DPPH、ABTS+·、·OH自由基的清除能力及对H2 O2诱导的PC 12细胞毒性的保护作用，评价灯盏乙素的体外抗氧化活性。结果表明：在N2气氛下，以90%乙醇为溶剂，H2SO 4为催化剂，是合成野黄芩苷的关键;野黄芩苷元的抗氧化活性比野黄芩苷元强。本研究结果为进一步研究和开发灯盏乙素作为治疗缺血性脑血管病的候选药物奠定了基础。
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.