Cytotoxic potential of dihydrochalcones from Eriosema glomeratum and their semi-synthetic derivatives

• Published in: Natural product research 2024, Vol.38 (2), p.186-197
• Main Authors: Tabakam, Gaétan Tchangou, Kodama, Takeshi, Tchuenmogne, Marthe Aimée Tchuente, Hoang, Nhat Nam, Nomin-Erdene, Battsengel, Ngouela, Silvère Augustin, Tene, Mathieu, Morita, Hiroyuki, Awouafack, Maurice Ducret
• Format: Article
• Language: English
• Subjects: Antineoplastic Agents - pharmacology; Cytotoxic agents; Cytotoxicity; Dichloromethane; erioschalcones A and B; Eriosema; Eriosema glomeratum; HeLa Cells; Hexanes; Humans; MCF-7 Cells; n-Hexane; Plant Extracts - pharmacology; Precursors; semi-synthesis; Toxicity
• ISSN: 1478-6419; 1478-6427
• DOI: 10.1080/14786419.2022.2111563

In the search of cytotoxic dihydrochalcones, this investigation led to the isolation of seven compounds (1-7) from Eriosema glomeratum and the preparation of eight derivatives (8-15). The cytotoxicity of samples was evaluated against lung (A549), breast (MCF-7), and cervical (HeLa) human cancer cells. The CH 2 Cl 2 /MeOH extract of the aerial part had strong cytotoxicity against all cells [IC 50 11.2 (MCF-7), 8.4 (HeLa) and 13.1 (A549) μg/mL]. A strong activity was also displayed by the n-hexane fraction on MCF-7 (IC 50 11.2 μg/mL). The precursor 3 and the derivative 8 were specifically found as strong cytotoxic agents toward MCF-7 (7.6 μM) and HeLa (3.1 μM), respectively and were more effective than the positive control. Derivatives 8 (3.1 μM) and 9 (21.3 μM) against HeLa were most potent than their precursor 3 (23.7 μM). This is the first preparation of 8-14 as well as the cytotoxicity of 3, 4, 8-15, fractions, and extract.