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Neuroprotective effect of catechins derivatives isolated from Anhua dark tea on NMDA-induced excitotoxicity in SH-SY5Y cells

机译:儿茶素衍生物从安库沙暗茶中分离的神经保护作用在南甘草诱导的SH-SY5Y细胞中吞噬毒性

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摘要

Anhua dark tea known as the earliest produced Chinese dark tea, has been commercially available and famous for its unique flavor and health care effect. NMDA receptors are glutamate-coupled ion channels that critically involved in survival of neuronal cells and neurodegenerative diseases. Thus, it is considered a promising target for the therapy of neurodegenerative disease. In this study, four catechins including two new catechins derivatives (1-2), together with thirteen known flavonoids were isolated from Anhua dark tea. The structures of compounds 1-2 [2.S,3R-6-methoxycarbonylgallocatechin (1) and 2R,3R-6-methoxycarbonylgallocatechin (2)] were determined on the basis of their spectroscopic data. The preliminary bioassay indicated that compound 1 showed the best neuroprotective effects via N-methyl-D-aspartate (NMDA) receptors inhibition. Compound 1 protected SH-SY5Y cells against NMDA-induced injury and cell apoptosis via the modulation of NR2B expression, the activation of PI3K/Akt signaling and caspase-dependent pathway. The results suggested compound 1 would be a potent dietary therapy reagent for prevention of excitable brain injury.
机译:安徽黑茶被称为最早的中国暗茶,已商购,以其独特的风味和保健效果而闻名。 NMDA受体是谷氨酸偶联的离子通道,批判性地参与神经元细胞的存活和神经变性疾病。因此,它被认为是神经变性疾病治疗的有希望的靶标。在这项研究中,包括两个新的儿茶素衍生物(1-2)的四种儿茶素,与Anhua暗茶中分离出三十名已知的黄酮类化合物。基于其光谱数据测定化合物1-2 [2.S,3R-6-甲氧基羰基甘油酰蛋白(1)和2R,3R-6-甲氧基羰基甘油蛋白(2)]的结构。初步生物测定表明,化合物1通过N-甲基-D-天冬氨酸(NMDA)受体抑制显示了最佳的神经保护作用。化合物1通过调节NR2B表达,对抗NMDA诱导的损伤和细胞凋亡的化合物1受保护的SH-SY5Y细胞,激活PI3K / AKT信号传导和胱天蛋白依赖性途径。结果表明化合物1是一种用于预防兴奋性脑损伤的有效膳食治疗试剂。

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  • 来源
    《Fitoterapia》 |2019年第2019期|共10页
  • 作者单位

    Shenyang Pharmaceut Univ Key Lab Struct Based Drug Design &

    Discovery Minist Educ Shenyang 110016 Liaoning Peoples R China;

    Guizhou Med Univ State Key Lab Funct &

    Applicat Med Plants Guiyang 550014 Guizhou Peoples R China;

    Seoul Natl Univ Coll Pharm Nat Prod Res Inst Seoul 08826 South Korea;

    Guizhou Med Univ State Key Lab Funct &

    Applicat Med Plants Guiyang 550014 Guizhou Peoples R China;

    Guizhou Med Univ State Key Lab Funct &

    Applicat Med Plants Guiyang 550014 Guizhou Peoples R China;

    Shenyang Pharmaceut Univ Key Lab Struct Based Drug Design &

    Discovery Minist Educ Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Key Lab Struct Based Drug Design &

    Discovery Minist Educ Shenyang 110016 Liaoning Peoples R China;

    Guizhou Med Univ State Key Lab Funct &

    Applicat Med Plants Guiyang 550014 Guizhou Peoples R China;

    Seoul Natl Univ Coll Pharm Nat Prod Res Inst Seoul 08826 South Korea;

    Shenyang Pharmaceut Univ Key Lab Struct Based Drug Design &

    Discovery Minist Educ Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Key Lab Struct Based Drug Design &

    Discovery Minist Educ Shenyang 110016 Liaoning Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 林区药材;
  • 关键词

    Anhua dark tea; Catechin derivatives; NMDA receptors; Neuroprotective effects;

    机译:安徽黑茶;儿茶素衍生物;NMDA受体;神经保护作用;

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