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Acetylcholinesterase Inhibitory Activity of Pigment Echinochrome A from Sea Urchin Scaphechinus mirabilis

机译:海胆Scaphechinus mirabilis色素Echinochrome A的乙酰胆碱酯酶抑制活性

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摘要

Echinochrome A (EchA) is a dark-red pigment of the polyhydroxynaphthoquinone class isolated from sea urchin Scaphechinus mirabilis. Acetylcholinesterase (AChE) inhibitors are used in the treatment of various neuromuscular disorders, and are considered as strong therapeutic agents for the treatment of Alzheimer’s disease (AD). Although EchA is clinically used to treat ophthalmic diseases and limit infarct formation during ischemia/reperfusion injury, anti-AChE effect of EchA is still unknown. In this study, we investigated the anti-AChE effect of EchA in vitro. EchA and its exhausted form which lost anti-oxidant capacity did not show any significant cytotoxicy on the H9c2 and A7r5 cells. EchA inhibited AChE with an irreversible and uncompetitive mode. In addition, EchA showed reactive oxygen species scavenging activity, particularly with nitric oxide. These findings indicate new therapeutic potential for EchA in treating reduced acetylcholine-related diseases including AD and provide an insight into developing new AChE inhibitors.
机译:Echinochrome A(EchA)是从海胆Scaphechinus mirabilis分离的聚羟基萘醌类的深红色颜料。乙酰胆碱酯酶(AChE)抑制剂可用于治疗各种神经肌肉疾病,并且被视为治疗阿尔茨海默氏病(AD)的强效治疗剂。尽管临床上已将EchA用于治疗眼科疾病并限制了缺血/再灌注损伤期间的梗塞形成,但EchA的抗AChE效果仍然未知。在这项研究中,我们调查了EchA在体外的抗AChE效应。 EchA及其丧失抗氧化能力的精疲力尽的形式对H9c2和A7r5细胞未显示任何明显的细胞毒性。 EchA以不可逆和非竞争性模式抑制AChE。此外,EchA表现出活性氧清除能力,尤其是一氧化氮。这些发现表明,EchA在治疗减少的乙酰胆碱相关疾病(包括AD)方面具有新的治疗潜力,并为开发新型AChE抑制剂提供了见识。

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