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首页> 外文期刊>RSC Advances >Evaluation of structure–activity relationships of ginsenosides against amyloid β induced pathological behaviours in transgenic Caenorhabditis elegans
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Evaluation of structure–activity relationships of ginsenosides against amyloid β induced pathological behaviours in transgenic Caenorhabditis elegans

机译：人参皂苷与β淀粉样蛋白诱导的秀丽隐杆线虫致病行为的结构活性关系评价

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Amyloid β (Aβ) induced toxicity has been postulated to initiate synaptic loss and subsequent neuronal degeneration in Alzheimer's disease (AD). The activities of ginsenosides against AD are widely reported, however, a systematic in vivo study comparing the effects of different ginsenosides on Aβ induced toxicity and cognitive impairment has not been described. In addition, the correlation between molecular structures and their anti-Aβ activities remains uncovered. In the present study, the in vivo anti-Aβ effects of 17 ginsenosides were explored using three transgenic Caenorhabditis elegans (C. elegans) models that exhibits pathological behaviors associated with Aβ. We found that (1) ginsenoside Rc, Rd, 20(S)-Rg3, Compound K (CK) and Rg1 could significantly reduce Aβ deposits, (2) ginsenoside Rc, Rd, CK, Rk3 and Rg1 inhibit Aβ induced paralysis, and (3) ginsenosides 20(S)-Rg3, CK and Rk3 prevented Aβ induced defects in associative learning capacity and showed antioxidative activity both in vitro and in vivo. The structure–activity relationships of 17 ginsenosides were investigated by comparing their anti-Aβ effects in C. elegans models. Results showed that the protopanaxadiol-type has higher activities than the protopanaxatriol-type or oleanane-type; the anti-Aβ effects of ginsenosides are inversely related to the sugar numbers. The results of the present study gain insight into the in vivo protective effects of ginsenosides against Aβ induced toxicity, and provide useful information for the clinical use of ginsenosides.
机译：据推测，淀粉样蛋白β（Aβ）诱导的毒性可引发突触丧失和随后的阿尔茨海默病（AD）神经元变性。人参皂苷对AD的活性已被广泛报道，但是，尚未有系统的体内系统研究比较人参皂苷对Aβ诱导的毒性和认知障碍的作用。另外，仍未发现分子结构与其抗Aβ活性之间的相关性。在本研究中，使用三种转基因线虫秀丽隐杆线虫模型研究了17种人参皂苷的体内抗Aβ作用。表现出与Aβ相关的病理行为。我们发现（1）人参皂苷Rc，Rd，20（ S ）-Rg3，化合物K（CK）和Rg1可以显着减少Aβ沉积物，（2）人参皂苷Rc，Rd，CK，Rk3和Rg1抑制Aβ诱导的麻痹，（3）人参皂甙20（ S ）-Rg3，CK和Rk3阻止Aβ诱导的联想学习能力缺陷，并在体外均显示抗氧化活性。和体内。通过比较17种人参皂甙在 C中的抗Aβ效应，研究了它们之间的构效关系。线虫模型。结果表明，普萘普生二醇型比普萘普生三醇型或齐墩果烷型具有更高的活性。人参皂苷的抗Aβ作用与糖值成反比。本研究结果深入了解人参皂甙对Aβ诱导的毒性的体内保护作用，为人参皂甙的临床应用提供了有用的信息。

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