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Discovery of dimeric costunolide-triazole conjugates as antihepatoma agents via integrating dimerization and molecular hybridization
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Tianze Li1, Chenxi Jiang1, 2, Qihao Li1, 3, Min-min Hu1, 3, Yabo Li1, Yao Yang1, 3, Yunbao Ma1, Yongcui Wang1, Jijun Chen1, 3, *
Chinese Journal of Natural Medicines | 2026, 24(8) : 1006 - 1014
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Chinese Journal of Natural Medicines | 2026, 24(8): 1006-1014
• Original Article •
Discovery of dimeric costunolide-triazole conjugates as antihepatoma agents via integrating dimerization and molecular hybridization
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Tianze Li1, Chenxi Jiang1, 2, Qihao Li1, 3, Min-min Hu1, 3, Yabo Li1, Yao Yang1, 3, Yunbao Ma1, Yongcui Wang1, Jijun Chen1, 3, *
Affiliations
  • 1Kunming Institute of Botany, Chinese Academy of Sciences, State Key Laboratory of Phytochemistry and Natural Medicines, Kunming 650201, China
  • 2Key Laboratory of Applied Surface and Colloid Chemistry, Ministry of Education and School of Chemistry and Chemical Engineering, Shaanxi Normal University, Xi'an 710062, China
  • 3Medical School, University of Chinese Academy of Sciences, Beijing 100049, China
About Author:

∆

These authors contributed equally to this work.

Published: 2026-08-20 doi: 10.1016/S1875-5364(26)61098-9
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Costunolide, a natural germacranolide sesquiterpenoid, exhibits only moderate anti-HCC activity. To enhance its efficacy and tumor selectivity, a series of 37 dimeric costunolide-1,2,3-triazole conjugates was designed and synthesized by integrating dimerization and molecular hybridization strategies. Evaluation of their antiproliferative effects on HepG2, Huh-7, and SK-Hep-1 cells suggested that 25 compounds were more potent than either costunolide or sorafenib. The most active dimer 19 exhibited significant activity with IC50 values of 1.6, 1.3, and 0.7 μmol·L−1, which were 13.1, 14.2, and 34.9-fold greater than those of costunolide. Compound 19 showed favorable selectivity against human normal liver cells (THLE-2) and markedly inhibited colony formation. Through a combination of bioinformatics, docking, and molecular dynamics (MD) simulations, glucose-6-phosphate dehydrogenase (G6PD) was identified as a target of compound 19, which was subsequently validated by DARTS and SPR assays. Functional studies revealed that compound 19 arrested the HCC cell cycle at the G2/M phase, suppressed migration and invasion by inhibiting epithelial-mesenchymal transition, and triggered both apoptosis and ferroptosis. These findings establish triazole-linked costunolide dimer 19 as a promising lead candidate for the development of novel anti-HCC therapies.

Antihepatoma activity  /  Costunolide  /  Triazole  /  Dimers  /  Glucose-6-phosphate dehydrogenase (G6PD)  /  Mechanism
Tianze Li, Chenxi Jiang, Qihao Li, Min-min Hu, Yabo Li, Yao Yang, Yunbao Ma, Yongcui Wang, Jijun Chen. Discovery of dimeric costunolide-triazole conjugates as antihepatoma agents via integrating dimerization and molecular hybridization[J]. Chinese Journal of Natural Medicines, 2026 , 24 (8) : 1006 -1014 . DOI: 10.1016/S1875-5364(26)61098-9
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Funding
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  • National Natural Science Foundation of China(22137008; 82473809)
  • Xingdian Yingcai Project(YNWR-KJLJ-2019-002)
  • Reserve Talents of Young and Middle-aged Academic and Technical Leaders in Yunnan Province(202105AC160021)
  • Yunnan Fundamental Research Projects(202401AS070077)
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Year 2026 volume 24 Issue 8
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72
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Article Info
doi: 10.1016/S1875-5364(26)61098-9
  • Receive Date：2025-11-10
  • Online Date：2026-08-20
  • Published：2026-08-20
Article Data
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History
  • Received：2025-11-10
  • Revised：2025-12-14
  • Accepted：2026-01-28
Funding
National Natural Science Foundation of China(22137008; 82473809)
Xingdian Yingcai Project(YNWR-KJLJ-2019-002)
Reserve Talents of Young and Middle-aged Academic and Technical Leaders in Yunnan Province(202105AC160021)
Yunnan Fundamental Research Projects(202401AS070077)
Affiliations
    1Kunming Institute of Botany, Chinese Academy of Sciences, State Key Laboratory of Phytochemistry and Natural Medicines, Kunming 650201, China
    2Key Laboratory of Applied Surface and Colloid Chemistry, Ministry of Education and School of Chemistry and Chemical Engineering, Shaanxi Normal University, Xi'an 710062, China
    3Medical School, University of Chinese Academy of Sciences, Beijing 100049, China

Corresponding:

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E-mail address: (J. Chen)
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
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Genus		 种数
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Percentage of total
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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