首页> 外文期刊>The Journal of Antibiotics: An International Journal >3-Normeridamycin:A Potent Non-lmmunosuppressive Immunophilin Ligand is Neuroprotective in Dopaminergic Neurons
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3-Normeridamycin:A Potent Non-lmmunosuppressive Immunophilin Ligand is Neuroprotective in Dopaminergic Neurons

机译:3-Normeridamycin:一种有效的非免疫抑制性免疫亲和素配体对多巴胺能神经元具有神经保护作用。

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摘要

3-Normeridamycin (1), isolated from fermen-tation extracts of the soil actinomycete Streptomyces sp.LL-C31037, demonstrated potent neuroprotective activity.When challenged with the neurotoxin 1-methyl-4-phenylpyridinium (MPP~+), known to induce parkinsonism, 1 restored functional dopamine uptake in a concentration-dependent manner, with an EC_(50) of 110nM in dopaminergic neurons.The structure of 1 was determined via spectroscopic methods, and the immunosuppressive and immunophilin binding properties of the compound were also measured.
机译:从土壤放线菌Streptomyces sp.LL-C31037的发酵提取物中分离得到的3-Normeridamycin(1)具有很强的神经保护活性。当受到神经毒素1-甲基-4-苯基吡啶鎓(MPP〜+)的攻击时帕金森病,1多巴胺能神经元的EC_(50)浓度依赖性地恢复了功能性多巴胺的摄取,通过光谱法确定了1的结构,并测定了该化合物的免疫抑制和亲和素结合特性。

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