Title: Chemical Analysis and Anticancer Potential of Phenolic Compounds Derived from Ehretia asperula Zoll. & Mor.
Authors: Nguyen Thi Thu Thuy , Tran Vy Anh
Volume: 9
Issue: 9
Pages: 58-67
Publication Date: 2025/09/28
Abstract:
Ehretia asperula Zoll. & Mor, known medicinally in Vietnam, has been utilized in folk medicine, particularly in treating cancer. Our goal is to isolate, characterize, and assess the cytotoxicity of boned E. asperula leaves to a set of E. asperula cytotoxicity. E. asperula leaves were dried, then extracted using methanol, and the dried methanol extract was fractioned using a set of organic solvents based on their increasing polarity. The most active solid phase from the column was the ethyl acetate fraction where column chromatographies on silica gel and Sephadex LH-20 were performed. The elucidation of the molecules was performed using NMR, and mass spectrometry. The cells on which the cytotoxic activity was tested include Hep-G2 (liver), LU-1 (lung), MCF-7 (breast), and He La (cervical), using the sulforhodamine B (SRB) assay. The cytotoxicity tests on E. asperula leaves indicated that the leaves are no active cancer therapeutic options. Focusing on the phenolics, 4 were isolated and identified as: Caffeic acid (Ed 3.2), Methyl caffeate (Ed 5.5), Rosmarinic acid (Ed 17.3), Methyl rosmarinate (Ed 11.4). Out of all, Caffeic acid and Rosmarinic acid were the only ones that exhibited some activity. Methyl caffeate and Methyl rosmarinate showed stronger cytotoxic activities against Hep-G2, HeLa, and MCF-7 cell lines with respect to their IC50 values ranging from 2.83 to 9.32 µg/mL. Methyl caffeate demonstrated better results compared to Methyl rosmarinate among all of the three active cell lines. The results suggest there is some kind of structure-activity relationship since the methyl esterification of the free carboxylic acid group substantially increased the cytotoxicity of the compounds. This could be attributed to the increased lipophilicity associated with the methyl group which enhances cellular permeation. More mechanistic studies and in vivo experiments are needed for Methyl caffeate and Methyl rosmarinate as they appear to be valuable lead candidates.