Synthesis, Characterization and Anti-hepatoma Activity of New Hederagenin Derivatives

Background: Based on the biological significance of hederagenin-type saponins found in our previous investigation, a series of new hederagenin derivatives were designed and synthesized. Methods : Their in vitro antiproliferative activities were evaluated against the HepG2 liver cancer cell line and normal cell line L929 by MTT assay. Results: The preliminary bioassay results demonstrated that all the tested compounds 1-7 showed potent anti-hepatoma activities, and some compounds exhibited better effects than 5-fluorouracil against human hepatocellular carcinoma HepG2 cell line. Furthermore, compound 5 showed a significant antihepatoma activity against HepG2 cells with an IC50 value of 1.88 µM. Besides, all of the tested compounds showed a low cytotoxic effect against the normal cell line L929. Conclusion: All the compounds 1-7 displayed superior selectivity against human hepatocellular carcinoma HepG2 cell line, and the results suggest that the structural modifications of C ring on the hederagenin backbone are vital for modulating anti-hepatoma activities.

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CHARACTERIZATION OF THE HUMAN HEPATOCELLULAR CARCINOMA (HEPG2) CELL LINE AS AN IN VITRO MODEL FOR CADMIUM TOXICITY STUDIES

In Vitro Cellular & Developmental Biology - Animal ◽

10.1290/1543-706x(2004)40<172:cothhc>2.0.co;2 ◽

2004 ◽

Vol 40 (5) ◽

pp. 172 ◽

Cited By ~ 39

Author(s):

P. F. DEHN ◽

C. M. WHITE ◽

D. E. CONNERS ◽

G. SHIPKEY ◽

T. A. CUMBO

Keyword(s):

Hepatocellular Carcinoma ◽

Cell Line ◽

Hepg2 Cell ◽

In Vitro Model ◽

Cadmium Toxicity ◽

Human Hepatocellular Carcinoma ◽

Hepg2 Cell Line ◽

Vitro Model

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Characterization of In Vitro 3D Cell Model Developed from Human Hepatocellular Carcinoma (HepG2) Cell Line

Cells ◽

10.3390/cells9122557 ◽

2020 ◽

Vol 9 (12) ◽

pp. 2557

Author(s):

Martina Štampar ◽

Barbara Breznik ◽

Metka Filipič ◽

Bojana Žegura

Keyword(s):

Hepatocellular Carcinoma ◽

Cell Line ◽

Hepg2 Cell ◽

Cell Model ◽

Human Hepatocellular Carcinoma ◽

Time Dependent ◽

Hepg2 Cell Line ◽

Cell Models

In genetic toxicology, there is a trend against the increased use of in vivo models as highlighted by the 3R strategy, thus encouraging the development and implementation of alternative models. Two-dimensional (2D) hepatic cell models, which are generally used for studying the adverse effects of chemicals and consumer products, are prone to giving misleading results. On the other hand, newly developed hepatic three-dimensional (3D) cell models provide an attractive alternative, which, due to improved cell interactions and a higher level of liver-specific functions, including metabolic enzymes, reflect in vivo conditions more accurately. We developed an in vitro 3D cell model from the human hepatocellular carcinoma (HepG2) cell line. The spheroids were cultured under static conditions and characterised by monitoring their growth, morphology, and cell viability during the time of cultivation. A time-dependent suppression of cell division was observed. Cell cycle analysis showed time-dependent accumulation of cells in the G0/G1 phase. Moreover, time-dependent downregulation of proliferation markers was shown at the mRNA level. Genes encoding hepatic markers, metabolic phase I/II enzymes, were time-dependently deregulated compared to monolayers. New knowledge on the characteristics of the 3D cell model is of great importance for its further development and application in the safety assessment of chemicals, food products, and complex mixtures.

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