Isocoumarins and Benzoquinones with Their Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Expression Inhibitory Activities from Dried Roots of Lysimachia vulgaris

Pel, P. and Kim, Y. and Kim, H.J. and Nhoek, P. and An, C. and Son, M. and Won, H. and Lee, S.E. and Lee, J. and Kim, H.W. and Choi, Y.H. and Lee, C.H. and Chin, Y. · ACS Omega · 2022

Preclinical

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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.

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How to cite

Pel, P. and Kim, Y. and Kim, H.J. and Nhoek, P. and An, C. and Son, M. and Won, H. and Lee, S.E. and Lee, J. and Kim, H.W. and Choi, Y.H. and Lee, C.H. and Chin, Y (2022) 'Isocoumarins and Benzoquinones with Their Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Expression Inhibitory Activities from Dried Roots of Lysimachia vulgaris', ACS Omega, 7(50), pp. 47296-47305. doi:10.1021/acsomega.2c06660

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