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Caged polycyclic polyprenylated acylphloroglucinols as Ca v 3.2 low voltage-gated Ca 2+ channel inhibitors from Hypericum curvisepalum .

Yan-Song YeRui LiuNa-Na JiangSong-Yu LiYin NianGang Xu
Published in: Chemical communications (Cambridge, England) (2022)
Five caged polycyclic polyprenylated acylphloroglucinols including an unprecedented octahydro-2,5-methanoindene skeleton (1) were discovered from Hypericum curvisepalum . Biologically, 1 and 2 are potent Ca v 3.2 T-type Ca 2+ channel inhibitors with negligible effect on the cardiovascular antitarget, the human ether-à-go-go-related gene potassium channel. Additionally, 2 indicates strong antinociception in the mouse acetic acid writhing test.
Keyphrases
  • protein kinase
  • endothelial cells
  • genome wide
  • copy number
  • gene expression
  • drug induced
  • genome wide identification