Faberidilactone A, a Sesquiterpene Dimer, Inhibits Hepatocellular Carcinoma Progression Through Apoptosis, Ferroptosis, and Anti-Metastatic Mechanisms

Cancer remains a significant global public health challenge, with hepatocellular carcinoma (HCC) ranking among the top five malignancies in terms of mortality. Faberidilactone A, a sesquiterpenoid dimer isolated from <i>Inula japonica</i>, exhibits potent cytotoxicity against various hum...

Full description

Saved in:
Bibliographic Details
Main Authors: Ruyu Cao, Yuhui Liu, Jiahe Bao, Mingming Rong, Jing Xu, Haibing Liao, Yuanqiang Guo
Format: Article
Language:English
Published: MDPI AG 2025-02-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/30/5/1095
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1850031359664324608
author Ruyu Cao
Yuhui Liu
Jiahe Bao
Mingming Rong
Jing Xu
Haibing Liao
Yuanqiang Guo
author_facet Ruyu Cao
Yuhui Liu
Jiahe Bao
Mingming Rong
Jing Xu
Haibing Liao
Yuanqiang Guo
author_sort Ruyu Cao
collection DOAJ
description Cancer remains a significant global public health challenge, with hepatocellular carcinoma (HCC) ranking among the top five malignancies in terms of mortality. Faberidilactone A, a sesquiterpenoid dimer isolated from <i>Inula japonica</i>, exhibits potent cytotoxicity against various human tumor cell lines and demonstrates remarkable antitumor potential. In vitro studies using HepG2 cells revealed that faberidilactone A induces apoptosis and ferroptosis, causes cell cycle arrest, enhances the production of intracellular reactive oxygen species (ROS), and disrupts mitochondrial function. Mechanistic investigations via Western blot analysis indicated that faberidilactone A impedes HepG2 cell proliferation by modulating the signal transducer and activator of the transcription 3 (STAT3) signaling pathway and inhibits metastasis by affecting the focal adhesion kinase (FAK) pathway. In vivo experiments using a zebrafish model demonstrated that faberidilactone A effectively suppresses the dissemination and metastasis of HepG2 cells and exhibits anti-angiogenic properties. When the concentration of faberidilactone A reached 10 µM, the inhibition rates of tumor proliferation, migration, and intersegmental vessels (ISVs) length were 76.9%, 72.6%, and 46.2%, respectively. These findings underscore the therapeutic potential of faberidilactone A as a promising agent for HCC treatment.
format Article
id doaj-art-70f6882a63bd487d813adf558fa48fe7
institution DOAJ
issn 1420-3049
language English
publishDate 2025-02-01
publisher MDPI AG
record_format Article
series Molecules
spelling doaj-art-70f6882a63bd487d813adf558fa48fe72025-08-20T02:59:00ZengMDPI AGMolecules1420-30492025-02-01305109510.3390/molecules30051095Faberidilactone A, a Sesquiterpene Dimer, Inhibits Hepatocellular Carcinoma Progression Through Apoptosis, Ferroptosis, and Anti-Metastatic MechanismsRuyu Cao0Yuhui Liu1Jiahe Bao2Mingming Rong3Jing Xu4Haibing Liao5Yuanqiang Guo6State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, ChinaState Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, ChinaState Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, ChinaState Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, ChinaState Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, ChinaState Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, ChinaState Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, ChinaCancer remains a significant global public health challenge, with hepatocellular carcinoma (HCC) ranking among the top five malignancies in terms of mortality. Faberidilactone A, a sesquiterpenoid dimer isolated from <i>Inula japonica</i>, exhibits potent cytotoxicity against various human tumor cell lines and demonstrates remarkable antitumor potential. In vitro studies using HepG2 cells revealed that faberidilactone A induces apoptosis and ferroptosis, causes cell cycle arrest, enhances the production of intracellular reactive oxygen species (ROS), and disrupts mitochondrial function. Mechanistic investigations via Western blot analysis indicated that faberidilactone A impedes HepG2 cell proliferation by modulating the signal transducer and activator of the transcription 3 (STAT3) signaling pathway and inhibits metastasis by affecting the focal adhesion kinase (FAK) pathway. In vivo experiments using a zebrafish model demonstrated that faberidilactone A effectively suppresses the dissemination and metastasis of HepG2 cells and exhibits anti-angiogenic properties. When the concentration of faberidilactone A reached 10 µM, the inhibition rates of tumor proliferation, migration, and intersegmental vessels (ISVs) length were 76.9%, 72.6%, and 46.2%, respectively. These findings underscore the therapeutic potential of faberidilactone A as a promising agent for HCC treatment.https://www.mdpi.com/1420-3049/30/5/1095faberidilactone Asesquiterpenoid dimerSTAT3FAKzebrafishantitumor
spellingShingle Ruyu Cao
Yuhui Liu
Jiahe Bao
Mingming Rong
Jing Xu
Haibing Liao
Yuanqiang Guo
Faberidilactone A, a Sesquiterpene Dimer, Inhibits Hepatocellular Carcinoma Progression Through Apoptosis, Ferroptosis, and Anti-Metastatic Mechanisms
Molecules
faberidilactone A
sesquiterpenoid dimer
STAT3
FAK
zebrafish
antitumor
title Faberidilactone A, a Sesquiterpene Dimer, Inhibits Hepatocellular Carcinoma Progression Through Apoptosis, Ferroptosis, and Anti-Metastatic Mechanisms
title_full Faberidilactone A, a Sesquiterpene Dimer, Inhibits Hepatocellular Carcinoma Progression Through Apoptosis, Ferroptosis, and Anti-Metastatic Mechanisms
title_fullStr Faberidilactone A, a Sesquiterpene Dimer, Inhibits Hepatocellular Carcinoma Progression Through Apoptosis, Ferroptosis, and Anti-Metastatic Mechanisms
title_full_unstemmed Faberidilactone A, a Sesquiterpene Dimer, Inhibits Hepatocellular Carcinoma Progression Through Apoptosis, Ferroptosis, and Anti-Metastatic Mechanisms
title_short Faberidilactone A, a Sesquiterpene Dimer, Inhibits Hepatocellular Carcinoma Progression Through Apoptosis, Ferroptosis, and Anti-Metastatic Mechanisms
title_sort faberidilactone a a sesquiterpene dimer inhibits hepatocellular carcinoma progression through apoptosis ferroptosis and anti metastatic mechanisms
topic faberidilactone A
sesquiterpenoid dimer
STAT3
FAK
zebrafish
antitumor
url https://www.mdpi.com/1420-3049/30/5/1095
work_keys_str_mv AT ruyucao faberidilactoneaasesquiterpenedimerinhibitshepatocellularcarcinomaprogressionthroughapoptosisferroptosisandantimetastaticmechanisms
AT yuhuiliu faberidilactoneaasesquiterpenedimerinhibitshepatocellularcarcinomaprogressionthroughapoptosisferroptosisandantimetastaticmechanisms
AT jiahebao faberidilactoneaasesquiterpenedimerinhibitshepatocellularcarcinomaprogressionthroughapoptosisferroptosisandantimetastaticmechanisms
AT mingmingrong faberidilactoneaasesquiterpenedimerinhibitshepatocellularcarcinomaprogressionthroughapoptosisferroptosisandantimetastaticmechanisms
AT jingxu faberidilactoneaasesquiterpenedimerinhibitshepatocellularcarcinomaprogressionthroughapoptosisferroptosisandantimetastaticmechanisms
AT haibingliao faberidilactoneaasesquiterpenedimerinhibitshepatocellularcarcinomaprogressionthroughapoptosisferroptosisandantimetastaticmechanisms
AT yuanqiangguo faberidilactoneaasesquiterpenedimerinhibitshepatocellularcarcinomaprogressionthroughapoptosisferroptosisandantimetastaticmechanisms