Department of Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka 422-8526, Japan.
Department of Organic Chemistry, School of Pharmaceutical Sciences, Hiroshima International University, Hiroshima 737-0112, Japan.
Int J Mol Sci. 2021 Mar 20;22(6):3187. doi: 10.3390/ijms22063187.
Sialidase cleaves sialic acid residues from glycans such as glycoproteins and glycolipids. In the brain, desorption of the sialic acid by sialidase is essential for synaptic plasticity, learning and memory and synaptic transmission. BTP3-Neu5Ac has been developed for sensitive imaging of sialidase enzyme activity in mammalian tissues. Sialidase activity in the rat hippocampus detected with BTP3-Neu5Ac increases rapidly by neuronal depolarization. It is presumed that an increased sialidase activity in conjunction with neural excitation is involved in the formation of the neural circuit for memory. Since sialidase inhibits the exocytosis of the excitatory neurotransmitter glutamate, the increased sialidase activity by neural excitation might play a role in the negative feedback mechanism against the glutamate release. Mammalian tissues other than the brain have also been stained with BTP3-Neu5Ac. On the basis of information on the sialidase activity imaging in the pancreas, it was found that sialidase inhibitor can be used as an anti-diabetic drug that can avoid hypoglycemia, a serious side effect of insulin secretagogues. In this review, we discuss the role of sialidase in the brain as well as in the pancreas and skin, as revealed by using a sialidase activity imaging probe. We also present the detection of influenza virus with BTP3-Neu5Ac and modification of BTP3-Neu5Ac.
唾液酸酶从糖蛋白和糖脂等聚糖中切割唾液酸残基。在大脑中，唾液酸酶的唾液酸解吸对于突触可塑性、学习和记忆以及突触传递是必不可少的。BTP3-Neu5Ac 已被开发用于敏感成像哺乳动物组织中的唾液酸酶活性。用 BTP3-Neu5Ac 检测大鼠海马中的唾液酸酶活性，神经元去极化后迅速增加。据推测，与神经兴奋相关的唾液酸酶活性增加参与了记忆的神经网络形成。由于唾液酸酶抑制兴奋性神经递质谷氨酸的胞吐作用，神经兴奋引起的唾液酸酶活性增加可能在对抗谷氨酸释放的负反馈机制中发挥作用。除大脑以外的哺乳动物组织也用 BTP3-Neu5Ac 进行了染色。基于胰腺中唾液酸酶活性成像的信息，发现唾液酸酶抑制剂可用作抗糖尿病药物，可避免胰岛素分泌剂的严重副作用——低血糖。在这篇综述中，我们讨论了使用唾液酸酶活性成像探针揭示的唾液酸酶在大脑以及胰腺和皮肤中的作用。我们还介绍了用 BTP3-Neu5Ac 检测流感病毒和 BTP3-Neu5Ac 的修饰。
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