TY - GEN
T1 - In Vitro Cytotoxicity of Gallic Acid Derivatives (Alkyl gallates) Against Breast MCF-7 Cancer Cells
AU - Arsianti, Ade
AU - Bahtiar, Anton
PY - 2022/12/23
Y1 - 2022/12/23
N2 - Breast cancer is the most common cancer in women. Based on WHO data in 2011, it is estimated that more than 508,000 women worldwide died of breast cancer. In Indonesia, the prevalence of breast cancer is 26.5% of all cancer cases, in which become the second frequent cancer. To date, the treatments for breast cancer are surgery, radiation therapy, chemoradiation, or combination therapy. However, the high rate of complications and side effects caused led to the need for the development of other therapies. Gallic acid is known to have potential anticancer effects. Structure modification on gallic acid by esterification of carboxyl group into alkyl gallate derivatives would change the hydrophobicity, as well as change its solubility and cytotoxicity against cancer cells. In this research, ten gallic acid derivatives (alkyl gallates) have been synthesized from the esterification of gallic acid and corresponding alkyl alcohol. Purification of the derivatives were conducted by flash column chromatography on silica gel by using the mixture of chloroform and methanol as mobile phase. Cytotoxic activities of gallic acid and its synthesized alkyl gallates against breast MCF-7 cancer cells were evaluated by MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. The data were analyzed by linear regression method to generate IC50 value. Among alkyl gallate derivatives, isoamyl gallate, heptyl gallate and octyl gallate showed a moderate cytotoxicity on breast MCF-7 cancer cells with IC50 values of 58.11; 25.94 and 42.34 μg/mL, respectively. Thus, isoamyl gallate, heptyl gallate and octyl gallate should be further developed as potent and promising agents for the treatment and therapy of breast cancer.
AB - Breast cancer is the most common cancer in women. Based on WHO data in 2011, it is estimated that more than 508,000 women worldwide died of breast cancer. In Indonesia, the prevalence of breast cancer is 26.5% of all cancer cases, in which become the second frequent cancer. To date, the treatments for breast cancer are surgery, radiation therapy, chemoradiation, or combination therapy. However, the high rate of complications and side effects caused led to the need for the development of other therapies. Gallic acid is known to have potential anticancer effects. Structure modification on gallic acid by esterification of carboxyl group into alkyl gallate derivatives would change the hydrophobicity, as well as change its solubility and cytotoxicity against cancer cells. In this research, ten gallic acid derivatives (alkyl gallates) have been synthesized from the esterification of gallic acid and corresponding alkyl alcohol. Purification of the derivatives were conducted by flash column chromatography on silica gel by using the mixture of chloroform and methanol as mobile phase. Cytotoxic activities of gallic acid and its synthesized alkyl gallates against breast MCF-7 cancer cells were evaluated by MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. The data were analyzed by linear regression method to generate IC50 value. Among alkyl gallate derivatives, isoamyl gallate, heptyl gallate and octyl gallate showed a moderate cytotoxicity on breast MCF-7 cancer cells with IC50 values of 58.11; 25.94 and 42.34 μg/mL, respectively. Thus, isoamyl gallate, heptyl gallate and octyl gallate should be further developed as potent and promising agents for the treatment and therapy of breast cancer.
UR - https://www.atlantis-press.com/proceedings/icolib-21/125979312
U2 - 10.2991/978-94-6463-062-6_26
DO - 10.2991/978-94-6463-062-6_26
M3 - Conference contribution
SN - 978-94-6463-062-6
BT - Proceedings of the 4th International Conference on Life Sciences and Biotechnology (ICOLIB 2021)
ER -