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Indole Alkaloids Inhibiting Neural Stem Cell from Uncaria rhynchophylla

机译:吲哚生物碱抑制钩藤的神经干细胞

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摘要

Uncaria rhynchophylla is commonly recognized as a traditional treatment for dizziness, cerebrovascular diseases, and nervous disorders in China. Previously, the neuro-protective activities of the alkaloids from U. rhynchophylla were intensively reported. In current work, three new indole alkaloids (>1–3), identified as geissoschizic acid (>1), geissoschizic acid N 4-oxide (>2), and 3β-sitsirikine N 4-oxide (>3), as well as 26 known analogues were isolated from U. rhynchophylla. However, in the neural stem cells (NSCs) proliferation assay for all isolated compounds, geissoschizic acid (>1), geissoschizic acid N 4-oxide (>2), isocorynoxeine (>6), isorhynchophylline (>7), (4S)-akuammigine N-oxide (>8), and (4S)-rhynchophylline N-oxide (>10) showed unexpected inhibitory activities at 10 μM. Unlike previous neuro-protective reports, as a warning or caution, our finding showcased a clue for possible NSCs toxicity and the neural lesions risk of U. rhynchophylla, while the structure–activity relationships of the isolated compounds were discussed also.Electronic supplementary materialThe online version of this article (doi:10.1007/s13659-017-0141-y) contains supplementary material, which is available to authorized users.
机译:在中国,钩藤钩藤通常被认为是头晕,脑血管疾病和神经疾病的传统疗法。以前,强烈报道了来自U. rhynchophylla的生物碱的神经保护活性。在当前的工作中,鉴定出三种新的吲哚生物碱(> 1-3-3 ),分别为Geissoschizic acid(> 1 ),Geissoschizic acid N 4-oxide(> 2 ) >)和3β-sitsirikineN 4-oxide(> 3 ),以及26种已知的类似物从支原丝藻中分离出来。但是,在所有分离的化合物的神经干细胞(NSCs)增殖测定中,geososchizic acid(> 1 ),geissoschizic acid N 4-oxide(> 2 ),isocorynoxeine(< strong> 6 ),异去乙酰胆碱(> 7 ),(4S)-akuammigine N-氧化物(> 8 )和(4S)-rhynchophylline N-氧化物( > 10 )在10μM时显示出意外的抑制活性。与先前的神经保护性报道不同,作为警告或警告,我们的发现显示了可能存在的NSC毒性和支原叶雷曼氏菌的神经损伤风险,同时还讨论了分离出的化合物的结构-活性关系。本文的版本(doi:10.1007 / s13659-017-0141-y)包含补充材料,授权用户可以使用。

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