2. Academic Validation
  3. Nonpeptidal compounds from the insect Polyphaga plancyi and their biological evaluation

Nonpeptidal compounds from the insect Polyphaga plancyi and their biological evaluation

  • Bioorg Chem. 2020 Nov;104:104258. doi: 10.1016/j.bioorg.2020.104258.
Hong-Jie Zhu 1,  Te Xu 2,  Yong-Ming Yan 2,  Yong-Xian Cheng 3
Affiliations

Affiliations

  • 1 State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, People's Republic of China.
  • 2 School of Pharmaceutical Sciences, Shenzhen University Health Science Center, Shenzhen 518060, People's Republic of China.
  • 3 School of Pharmaceutical Sciences, Shenzhen University Health Science Center, Shenzhen 518060, People's Republic of China. Electronic address: yxcheng@szu.edu.cn.
PMID: 32956876 DOI: 10.1016/j.bioorg.2020.104258
Abstract

Five new nitrogen-containing compounds (1-3, 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.

Keywords

Insect; Nitrogen-containing compounds; Polyphaga plancyi; Renal protection; Smad3 phosphorylation inhibitor.

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