Convulsion-related activities of Scutellaria flavones are related to the 5,7-dihydroxyl structures.
Convulsion-related activities of Scutellaria flavones are related to the 5,7-dihydroxyl structures.
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DOI：
10.1016/j.ejphar.2011.03.012
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发表时间：
2011-06
影响因子：
5
通讯作者：
S. Yoon;Ike C Dela Peña;C. Shin;K. Son;Yong Soo Lee;J. Ryu;J. Cheong;K. Ko
中科院分区：
文献类型：
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作者：
S. Yoon;Ike C Dela Peña;C. Shin;K. Son;Yong Soo Lee;J. Ryu;J. Cheong;K. Ko
我们筛选了从黄芩中分离的主要生物活性黄酮（黄芩苷、黄芩素和木木精A）的惊厥相关活性。在生电反应评分系统和戊四唑癫痫模型中，黄芩素表现出抗惊厥作用，而木木精A和黄芩苷则没有。体外研究还表明，黄芩素诱导细胞内 Cl-内流，而 oroxylin A 则阻断蝇蕈醇和黄芩素诱导的细胞内 Cl-内流。黄芩素的抗惊厥作用可被苯二氮卓类（BZD）受体拮抗剂氟马西尼抑制。因此，黄芩素的抗惊厥作用是由GABAA受体的BZD结合位点介导的。 5, 7-二羟基存在于三种黄酮的结构中。据推测，该组在诱发惊厥相关活动中发挥了关键作用。
We screened the major bioactive flavones isolated fromScutellaria baicalensis(baicalin, baicalein and oroxylin A) for their convulsion related activities. In electrogenic response score system and the pentylenetetrazole seizure model, baicalein but not oroxylin A and baicalin exhibited anticonvulsant effects. In vitro studies also revealed that baicalein induced intracellular Cl−influx, whereas oroxylin A blocked muscimol- and baicalein-induced intracellular Cl−influx. The anticonvulsant effect of baicalein was inhibited by flumazenil, a benzodiazepine(BZD) receptor antagonist. Therefore, anticonvulsive effect of baicalein was mediated by the BZD binding site of GABAAreceptor. The 5, 7-dihydroxyl group is present in the structure of the three flavones. It is postulated that this group played a key role in inducing convulsion-related activities.