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Effect of modification of betulinic acid at the C3-carbon atom of homolupane triterpenoids on the antiproliferative activity in vitro

  1. 1.
    0562286 - ÚEB 2023 RIV GB eng J - Článek v odborném periodiku
    Rárová, L. - Pakulski, Z. - Strnad, Miroslav - Kvasnicová, M. - Štenclová, T. - Cmoch, P.
    Effect of modification of betulinic acid at the C3-carbon atom of homolupane triterpenoids on the antiproliferative activity in vitro.
    Journal of Steroid Biochemistry and Molecular Biology. Roč. 224, NOV (2022), č. článku 106161. ISSN 0960-0760
    Grant CEP: GA ČR(CZ) GA20-25308S
    Institucionální podpora: RVO:61389030
    Klíčová slova: Antiproliferative activity * Apoptosis * Cancer cells * Fibroblasts * Lupanes * Reformatsky reaction
    Obor OECD: Medicinal chemistry
    Impakt faktor: 4.1, rok: 2022
    Způsob publikování: Open access
    https://doi.org/10.1016/j.jsbmb.2022.106161

    In search of new cytotoxic derivatives based on the lupane scaffold, methyl betulonate and methyl 20,29-dihydrobetulonate were conjugated with Reformatsky reagents to provide homolupanes extended at the C3-carbon atom. Further transformations of the functional groups afforded a series of derivatives with 2-hydroxyethyl and allyl alcohol moieties. Their varying antiproliferative activity in vitro was then investigated in four cancer cell lines and in normal human BJ fibroblasts. In cervical carcinoma HeLa cells, derivatives 5, 6 and 17 were the most promising with lower micromolar IC50s and no toxicity to fibroblasts, thus showing a high therapeutic index. In addition, induction of apoptosis was found in HeLa cells after 24 h treatment with compounds 5, 6, 13 and 29. This newly synthesized series is more interesting than the published lupane and homolupane triterpenes and saponins, due to their nontoxicity towards healthy human cells and stronger cytotoxicity to various cancer cell lines. This approach increases their potential as anticancer agents.
    Trvalý link: https://hdl.handle.net/11104/0334634

     
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