Discovery of Novel Mono-Carbonyl Curcumin Derivatives as Potential Anti-Hepatoma Agents
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Published:2023-09-25
Issue:19
Volume:28
Page:6796
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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:
Cao Weiya12,
Yu Pan12ORCID,
Yang Shilong3,
Li Zheyu2,
Zhang Qixuan2,
Liu Zengge2,
Li Hongzhuo2
Affiliation:
1. College of Public Health, Anhui University of Science and Technology, Hefei 230000, China
2. College of Medicine, Anhui University of Science and Technology, Huainan 232001, China
3. College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China
Abstract
Curcumin possesses a wide spectrum of liver cancer inhibition effects, yet it has chemical instability and poor metabolic properties as a drug candidate. To alleviate these problems, a series of new mono-carbonyl curcumin derivatives G1–G7 were designed, synthesized, and evaluated by in vitro and in vivo studies. Compound G2 was found to be the most potent derivative (IC50 = 15.39 μM) compared to curcumin (IC50 = 40.56 μM) by anti-proliferation assay. Subsequently, molecular docking, wound healing, transwell, JC-1 staining, and Western blotting experiments were performed, and it was found that compound G2 could suppress cell migration and induce cell apoptosis by inhibiting the phosphorylation of AKT and affecting the expression of apoptosis-related proteins. Moreover, the HepG2 cell xenograft model and H&E staining results confirmed that compound G2 was more effective than curcumin in inhibiting tumor growth. Hence, G2 is a promising leading compound with the potential to be developed as a chemotherapy agent for hepatocellular carcinoma.
Funder
Natural Science Research Project of Anhui Educational Committee
Scientific Research Foundation for High-level Talents of Anhui University of Science and Technology
Anhui Provincial Natural Science Foundation
Practice Innovation Training Program for College Students in Anhui Province
Subject
Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science
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