1,4萘醌和1,2萘醌化合物对肌质网钙通道Ryanodine受体的调节作用

The Modulation of 1,4NQs and 1,2NQs on Ryanodine Receptor in Sarcoplasmic Reticulum.

目的研究萘醌钙通道蛋白（ＮＱＲｙＲ）的作用机制。方法对ＮＱ旋的１，４ＮＱ、１，４ＮＱ２ｓｕｌｆｏｎａｔｅ（１，４ＮＱ２Ｓ）、１，２ＮＱ、１，２ＮＱ４ｓｕｌｆｏｎａｔｅ（１，２ＮＱ４Ｓ）、２ＣＨ３１，４ＮＱ和２ＯＨ１，４ＮＱ等６种ＮＱ与骨骼肌肌质网（ＳＲ）ＲｙＲ的相互作用进行了观察和比较。结果所有ＮＱ都不同程度地激活钙通道引起钙流释放；１，４ＮＱ、１，２ＮＱ、１，２ＮＱ、１，４ＮＱ２Ｓ和１，２ＮＱ４Ｓ对ＲｙＲ的调节表现出强烈的浓度依赖性的双相作用性；ＮＱ通过氧化还原作用调控ＲｙＲ的门控机制；ＮＱ在氧化还原循环中产生的超氧等伴生物没有参与ＲｙＲ的相互作用。结论ＮＱ对ＲｙＲ的调控是通过氧化还原作用调节通道蛋白的门控状态。

Objective To study the modulation mechanism of naphthoquinones(NQ) on ryanodine receptor(RyR) in sarcoplasmic reticulum.Methods The interactions of six naphthoquinones (1,4NQ,1,4NQ 2 sulfonate,1,2NQ 4 sulfonate,2 CH 3 1,4 NQ and 2 OH 1,4 NQ) and rynodine reaptor in sarcoplasmic reticulum were observed and compared.Results All the NQs can activate the calcium release channel to some entent and induce Ca 2+ transportation.The modulations of 1,4 NQ,1,2 NQ,1,4 NQ2S and 1,2 N are biphasic and depend on their concentrations.The mechanism of gating modulation depends on oxidation and reduction of NQ.The by products of NQ during oxidation and reduction do not interact with RyR. Conclusion The modulation of NQ on RyR is realized by regulating the gating of RyR through oxidation and reduction.