Diterpenoids with Schistosomula-Killing and Anti-Fibrosis Activities In Vitro from the Leaves of Croton tiglium
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Published:2024-01-13
Issue:2
Volume:29
Page:401
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ISSN:1420-3049
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Container-title:Molecules
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language:en
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Short-container-title:Molecules
Author:
Li Li1, Zhao Biqing1, Zheng Xiaoxiao1, Liu Zhaohui2, Zou Huan2, Qin Li1, Zhou Xiaojiang1
Affiliation:
1. College of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, China 2. Hengxiu Tang Pharmaceutical Co., Ltd., Changsha 410219, China
Abstract
The leaves of C. tiglium have been comprehensively researched for their structurally novel bioactive natural compounds, especially those with anti-schistosomiasis liver fibrosis activity, because ethyl acetate extract, which can be extracted from the leaves of C. tiglium, has good anti-schistosomiasis liver fibrosis effects. One new tigliane-type diterpene, 20-acetyl-13-O-(2-metyl)butyryl-phorbol (1), and nine known (2–10) analogues were isolated from the leaves of C. tiglium. Their structures were elucidated on the basis of spectroscopic analysis and ECD analysis. All diterpenoids had a stronger insecticidal effect on schistosomula, and compounds 2, 4, and 10 had good anti-liver-fibrosis effects. Furthermore, compared with the model group, compound 2 significantly downregulated the protein and mRNA expression of COL-I, COL-III, α-SMA, and TGF-β1 on TGF-β1-induced liver fibrosis in LX-2 cells. Meanwhile, compound 2 also regulated the expression of TGF-β/Smad-pathway-related proteins. The results suggest that diterpenoids from C. tiglium may serve as potential schistosomula-killing and anti-liver-fibrosis agents in the future.
Funder
Science Program of Hunan Administration of Traditional Chinese Medicine, China Key Discipline Project on Chinese Pharmacology of Hunan University of Chinese Medicine, China
Subject
Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science
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