16 July 2022, Published by Phytomeedicine (IF 6.656) © Elsevier. B.V.

In this study, researchers analyzed the main functional compounds in Zexie. 6 triterpenoids were newly found, named Alisolinal A/B/C/D/E/F; and 34 well-known triterpenoids were also found in Zexie. Subsequently, the researchers studied the absorptioned promotion of 40 kinds of triterpenoids on low-density lipoprotein (LDL) and the inhibitory effects on PCSK9.

Through cell based assay, researchers studied the inhibitory effects of 40 kinds of triterpenoids on PCSK9 protein expression. PCSK9 is a protease synthesized in the liver. This protease could break down (LDL) receptor, which leads to reduce LDL absorption. PCSK9 is an effective target in the treatment of atherosclerotic cardiovascular disease. Among the 40 triterpenoids, 6 triterpenoids were investigated the significant inhibition against PCSK9, the highest inhibitory rate reached to 58%. The same character of triterpenoids with high inhibitory rate showed the same positon of double bond, at C-25 and C-26. In addition, an exciting found was that 17 triterpenoids showed significant activities in increasing LDL absorption. Based on the results and found of this study, the researchers suggested the triterpenoids from Zexie could serve as a new source of PCSK9 inhibitors.

Zhang, Yan, X., Jin, Q., Chen, J., Yang, L., Wei, W., Qu, H., Yao, C., Hou, J., Gong, L., Wu, W., & Guo, D. (2022). Novel triterpenoids from Alisma plantago-aquatica with influence on LDL uptake in HepG2 cells by inhibiting PCSK9. Phytomedicine (Stuttgart), 105.