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Updated: Sep 19, 2025

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
Published on: August 28, 2018
Kadcoccinoids A-K, triterpenoids from Kadsura coccinea with PCSK9 expression inhibitory activities
Yelin Duan1, Tong Chen2, Pengju Guo3
1School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing, 210023, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Road, Shanghai, 201203, China.
Abstract:
Two undescribed protostane-type triterpenoids (1-2), and nine undescribed lanostane-type triterpenoids (3-11), along with nine known compounds (12-20) were isolated from the stems of Kadsura coccinea. Their chemical structures were elucidated by extensive spectroscopic analyses, Mosher's method, X-ray crystallography, and electronic circular dichroism calculations. Kadcoccinoid A (1) possesses an undescribed 6/6/8-fused carbocyclic core containing a rare bicyclo [4.2.1] nonan-9-one system and proposed plausible biosynthetic pathway. Additionally, kadcoccinoid B (2) significantly decreased PCSK9 protein levels in the medium of HepG2 cells at 10 μM with an inhibition rate of 78.4 % and increased LDL uptake at 5 and 10 μM, while compounds 12-14 showed moderate PCSK9 inhibitory activities.
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