COMPARATIVE ANALYSIS OF GLYCYRRHETINIC ACID DERIVATIVES BASED ON THEIR ACTIVITY INDICATORS: A CROSS-STUDY EVALUATION OF CYTOTOXICITY IN STANDARD CANCER CELL LINES
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This work was designed as an analytical comparative review based exclusively on original experimental publications.Abstrak
Glycyrrhetinic acid (GA, 18 β-glycyrrhetinic acid) is a pentacyclic triterpenoid scaffold of considerable interest in anticancer drug discovery because chemical modification of its hydroxyl, carboxyl, and ring A functionalities can markedly alter cytotoxic potency, selectivity, and mechanism of action. The aim of the present article was to conduct a comparative analysis of glycyrrhetinic acid derivatives on the basis of activity indicators reported in original experimental studies and to identify the most promising structural series across different standard cancer cell lines. Five peer-reviewed papers with real and verifiable DOI numbers were selected: Molecules (2016), Bioorganic Chemistry (2019), Biological and Pharmaceutical Bulletin (2020), Bioorganic Chemistry (2020), and Molecules (2023). The comparison focused on derivative class, cancer cell-line spectrum, IC50 values, selectivity toward normal cells, apoptosis-related findings, oxidative stress markers, and preliminary structure–activity relationship (SAR) trends
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Li Y., Feng L., Song Z.-F., Li H.-B., Huai Q.-Y. Synthesis and Anticancer Activities of Glycyrrhetinic Acid Derivatives. Molecules. 2016;21(2):199. DOI: 10.3390/molecules21020199.
Wang R., Yang W., Fan Y., Dehaen W., Li Y., Li H., Wang W., Zheng Q., Huai Q. Design and synthesis of the novel oleanolic acid-cinnamic acid ester derivatives and glycyrrhetinic acid-cinnamic acid ester derivatives with cytotoxic properties. Bioorganic Chemistry. 2019;88:102951. DOI: 10.1016/j.bioorg.2019.102951.
Zheng Q.-X., Wang R., Xu Y., He C.-X., Zhao C.-Y., Wang Z.-F., Zhang R., Dehaen W., Li H.-J., Huai Q.-Y. Design, Preparation and Studies Regarding Cytotoxic Properties of Glycyrrhetinic Acid Derivatives. Biological and Pharmaceutical Bulletin. 2020;43(1):102–109. DOI: 10.1248/bpb.b19-00615.
Huang M., Gong P., Wang Y., Xie X., Ma Z., Xu Q., Liu D., Jing Y., Zhao L. Synthesis and antitumor effects of novel 18β-glycyrrhetinic acid derivatives featuring an exocyclic α,β-unsaturated carbonyl moiety in ring A. Bioorganic Chemistry. 2020;103:104187. DOI: 10.1016/j.bioorg.2020.104187.
Chen J., Xu Y., Yang Y., Yao X., Fu Y., Wang Y., Liu Y., Wang X. Evaluation of the Anticancer Activity and Mechanism Studies of Glycyhetic Acid Derivatives toward HeLa Cells. Molecules. 2023;28(7):3164. DOI: 10.3390/molecules28073164.
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