Cytotoxicity Activity of Some meso‐Dihydroguaiaretic Acid Derivatives and Mode of Action of the Most Active Compound

The aim of this study was to screen sixteen meso‐1 semi‐synthetic derivatives bearing ether, esther, carbamate, phosphate or aminoether functional groups against five cancer cell lines: MCF‐7 (breast), A549 (lung), HepG2 (liver), HeLa (cervix), and DU145 (prostate) at 25 μM using the MTT assay. Resu...

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Bibliographic Details
Published in:Chemistry & biodiversity 2024-02, Vol.21 (2), p.e202301930-n/a
Main Authors: Domínguez‐Chavarría, José Antonio, García, Abraham, Romo‐Mancillas, Antonio, Reyes‐Melo, Karen Y., Chávez‐Villareal, Karen G., Vázquez‐Ramírez, Ana L., Ávalos‐Alanís, Francisco G., Cabral‐Romero, Claudio, Hernández‐Delgadillo, Rene, García‐Cuellar, Claudia María, Rayo Camacho‐Corona, María
Format: Article
Language:English
Subjects:
Breast
Cancer
Cell viability
cytotoxic cancer cells
Cytotoxicity
docking studies
Functional groups
lignans
Lungs
meso-Dihydroguaiaretic acid
Mode of action
semi-synthetic derivatives
Toxicity
Tumor cell lines
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Summary:The aim of this study was to screen sixteen meso‐1 semi‐synthetic derivatives bearing ether, esther, carbamate, phosphate or aminoether functional groups against five cancer cell lines: MCF‐7 (breast), A549 (lung), HepG2 (liver), HeLa (cervix), and DU145 (prostate) at 25 μM using the MTT assay. Results from the screening showed that two derivatives had the lowest percentage of cell viability at 25 μM, the aminoether derivative meso‐11 and the esther derivative meso‐20 against A549 (44.15±0.78 %) and MCF‐7 (41.60±0.92 %), respectively. Then, it was determined the IC50 value of each compound against their most sensitive cancer cell line. Results showed that aminoether derivative meso‐11 showed potent cytotoxicity against A549 (IC50=17.11±2.11 μM), whereas it resulted more cytotoxic against the LL‐47 lung normal cell line (IC50=9.49±1.19 μM) having a Selective Index (SI) of 0.55. On the other hand, the esther derivative meso‐20 exhibited potent activity against MCF‐7 (IC50=18.20±1.98 μM), whereas it displayed moderate cytotoxicity against the MCF‐10 breast normal cell line (IC50=41.22±2.17 μM) with a SI of 2.2. Finally, studies on the mechanism of action of meso‐20 indicated disruption of MCF‐7 plasma membrane in vitro and the AMPK activation in silico.
ISSN:1612-1872
1612-1880
DOI:10.1002/cbdv.202301930