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Nonpeptidal compounds from the insect Polyphaga plancyi and their biological evaluation.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-09-02 , DOI: 10.1016/j.bioorg.2020.104258
Hong-Jie Zhu 1 , Te Xu 2 , Yong-Ming Yan 2 , Yong-Xian Cheng 2
Affiliation  

Five new nitrogen-containing compounds (13, 5, and 6), two compounds which was firstly isolated from natural origin (7 and 10), along with six known ones, were isolated from the ethanol extract of the whole bodies of Polyphaga plancyi. The structures of the new compounds including their absolute configurations at stereogenic centers were assigned on the basis of spectroscopic analyses and computational methods. Racemic 10 was separated by chiral HPLC. Biological activities of these isolates against extracellular matrix components in rat renal proximal tubular cells, EV71, COX-2, ROCK2, JAK3, and tuberculosis were evaluated. Importantly, 8 was found to be a selective Smad3 phosphorylation inhibitor.



中文翻译:

昆虫Poly虫的非肽类化合物及其生物学评价。

五个新的含氮化合物(1 - 35,和6),其首先从天然来源(隔绝两种化合物710),有六个已知的那些一起,被从整个机构的乙醇提取物中分离多食普兰西。根据光谱分析和计算方法确定了新化合物的结构,包括其立体构型中心的绝对构型。外消旋10通过手性HPLC分离。评估了这些分离物对大鼠肾近端肾小管细胞,EV71,COX-2,ROCK2,JAK3和肺结核中细胞外基质成分的生物活性。重要的是,发现8是选择性Smad3磷酸化抑制剂。

更新日期:2020-09-20
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