TY  - EJOU
AU  - Milan, M. Andreea
AU  - Mioc, M. Marius
AU  - Prodea, P. Alexandra
AU  - Șoica, Ș. Codruța
TI  - Betulinic Acid Fatty Esters and Their Liposomal Formulations: Targeting Cytotoxicity Against Ovarian, Colorectal, and Lung Cancer Cells
T2  - Journal of Experimental Pharmacology and Toxicology

PY  - 2025
VL  - 2
IS  - 2
SN  - 3091-0595

AB  - Despite its notable anticancer potential, betulinic acid (BA) exhibits limited bioavailability that hampers its therapeutic efficacy. To address this issue, betulinic acid fatty esters were previously synthesized by employing stearic (St-BA), palmitic (Pal-BA), and butyric acids (But-BA), and further incorporated into surface-modified liposomal formulations (St-BA-Lip, Pal-BA-Lip, But-BA-Lip). The BA derivatives, as well as their liposomal formulations, were assessed against three human cancer cell lines: colorectal adenocarcinoma Caco-2 cells, ovarian teratocarcinoma PA-1, and alveolar epithelial adenocarcinoma A549 cells. All compounds exhibited cytotoxic effects in a time- and dose-dependent manner, more potently than the positive control, 5-fluorouracil (5-FU). But-BA-Lip exhibited the best anticancer effects against all tested cancer cell lines, recording lower IC50 values than the parent compound (BA) and 5-FU (15.55 μM against Caco-2 cells, 48.16 μM against PA-1 cells, and 25.3 μM against A549 cells). In silico molecular docking studies revealed that Pal-BA showed superior binding affinity to AKT/PKB than the parent compound, BA, while But-BA showed enhanced interaction with EGFR1. Both derivatives achieved 93% of the native ligand’s docking score, highlighting their therapeutic potential through structural modifications.
KW  - anticancer
KW  - liposomes
KW  - betulinic acid
KW  - triterpenes
KW  - fatty esters
KW  - cytotoxicity assay
KW  - molecular docking
DO  - 10.6425/022025jept003