PREPARATION OF SELECTED SEMISYNTHETIC GLYCYRRHETINIC ACID DERIVATIVES FOR IN VITRO AND IN VIVO STUDIES AND SELECTION OF APPROPRIATE EXPERIMENTAL MODELS
Ключевые слова:
The preparation of semisynthetic derivatives is only one side of the research problem. The second, equally important side is experimental model selection.Аннотация
Glycyrrhetinic acid is one of the most widely investigated pentacyclic triterpenoid scaffolds in contemporary natural-product-based medicinal chemistry. Its parent molecule already exhibits anti-inflammatory, antiviral, hepatoprotective, antimicrobial, and antitumor effects, but its intrinsic potency and pharmacokinetic behavior are often insufficient for direct translational development. For this reason, a large body of work has focused on semisynthetic modification of GA in order to generate derivatives with improved biological performance. However, the value of these derivatives depends not only on successful chemical preparation but also on the rational selection of in vitro and in vivo experimental models that can reveal cytotoxic, anti-inflammatory, anti-metastatic, and tumor-microenvironment-modulating activity. The aim of the present article was to analyze the preparation of selected semisynthetic GA derivatives and the principles of choosing appropriate in vitro and in vivo pharmacological models using six original experimental papers published in reputable journals with real and verifiable DOI numbers.
Библиографические ссылки
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.
Yang Y., Zhu Q., Zhong Y., Cui X., Jiang Z., Wu P., Zheng X., Zhang K., Zhao S. Synthesis, anti-microbial and anti-inflammatory activities of 18β-glycyrrhetinic acid derivatives. Bioorganic Chemistry. 2020;101:103985. DOI: 10.1016/j.bioorg.2020.103985.
Markov A.V., Sen’kova A.V., Zenkova M.A., Logashenko E.B. Novel Glycyrrhetinic Acid Derivative Soloxolone Methyl Inhibits the Inflammatory Response and Tumor Growth in vivo. Molecular Biology. 2018;52(2):306–313. DOI: 10.7868/S0026898418020143.
Tu B., Liang J., Ou Y., Zhang X., Zheng W., Wu R., Gan L., Li D., Lu Y., Wu J., Hong W.-D., Zhang K., Wu P., Jin J., Wong W.-L. Novel 18β-glycyrrhetinic acid derivatives as a Two-in-One agent with potent antimicrobial and anti-inflammatory activity. Bioorganic Chemistry. 2022;122:105714. DOI: 10.1016/j.bioorg.2022.105714.
Salomatina O.V., Sen’kova A.V., Moralev A.D., Savin I.A., Komarova N.I., Salakhutdinov N.F., Zenkova M.A., Markov A.V. Novel Epoxides of Soloxolone Methyl: An Effect of the Formation of Oxirane Ring and Stereoisomerism on Cytotoxic Profile, Anti-Metastatic and Anti-Inflammatory Activities In Vitro and In Vivo. International Journal of Molecular Sciences. 2022;23(11):6214. DOI: 10.3390/ijms23116214.
Markov A.V., Ilyina A.A., Salomatina O.V., Sen’kova A.V., Okhina A.A., Rogachev A.D., Salakhutdinov N.F., Zenkova M.A. Novel Soloxolone Amides as Potent Anti-Glioblastoma Candidates: Design, Synthesis, In Silico Analysis and Biological Activities In Vitro and In Vivo. Pharmaceuticals. 2022;15(5):603. DOI: 10.3390/ph15050603.
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