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Isocoumarins and Benzoquinones with Their Proprotein Convertase Subtilisin/Kexin Type 9 Expression Inhibitory Activities from Dried Roots of Lysimachia vulgaris.


ABSTRACT: A phytochemical investigation of the n-hexane-soluble chemical constituents of Lysimachia vulgaris roots allowed for selection using a proprotein convertase subtilisin-kexin type 9 (PCSK9) mRNA expression monitoring assay in HepG2 cells. This led to the isolation of two previously undescribed isocoumarins of natural origin, 8'Z,11'Z-octadecadienyl-6,8-dihydroxyisocoumarin (1) and 3-pentadecyl-6,8-dihydroxyisocoumarin (2), along with 20 previously reported compounds (3-22). All of the structures were established using NMR spectroscopic data and MS analysis. Of the isolates, 1 and 3 were found to inhibit PCSK9, inducible degrader of the low-density lipoprotein receptor (IDOL), and SREBP2 mRNA expression. Further computational dockings of both 1 and 3 to C-ring of IDOL E3 ubiquitin ligase predicted the mechanism behind the inhibitory effect of these compounds on the enzyme.

SUBMITTER: Pel P 

PROVIDER: S-EPMC9774376 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature

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Isocoumarins and Benzoquinones with Their Proprotein Convertase Subtilisin/Kexin Type 9 Expression Inhibitory Activities from Dried Roots of <i>Lysimachia vulgaris</i>.

Pel Pisey P   Kim Young-Mi YM   Kim Hyun Ji HJ   Nhoek Piseth P   An Chae-Yeong CY   Son Min-Gyung MG   Won Hongic H   Lee Seung Eun SE   Lee Jeonghoon J   Kim Hyun Woo HW   Choi Young Hee YH   Lee Chang Hoon CH   Chin Young-Won YW  

ACS omega 20221208 50


A phytochemical investigation of the <i>n</i>-hexane-soluble chemical constituents <i>of</i> <i>Lysimachia vulgaris</i> roots allowed for selection using a proprotein convertase subtilisin-kexin type 9 (PCSK9) mRNA expression monitoring assay in HepG2 cells. This led to the isolation of two previously undescribed isocoumarins of natural origin, 8'Z,11'Z-octadecadienyl-6,8-dihydroxyisocoumarin (<b>1</b>) and 3-pentadecyl-6,8-dihydroxyisocoumarin (<b>2</b>), along with 20 previously reported compo  ...[more]

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