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. 2021 Apr;35(8):1372-1378.
doi: 10.1080/14786419.2019.1650355. Epub 2019 Aug 12.

Synthesis and cytotoxicity of the conjugates of diterpenoid isosteviol and N-acetyl-D-glucosamine

Bulat F Garifullin  1 , Irina Yu Strobykina  1 , Leysan R Khabibulina  1 , Anastasiya S Sapunova  1 , Aleksandra D Voloshina  1 , Radmila R Sharipova  1 , Bulat I Khairutdinov  2 , Yuriy F Zuev  2   3 , Vladimir E Kataev  1
Affiliations

Synthesis and cytotoxicity of the conjugates of diterpenoid isosteviol and N-acetyl-D-glucosamine

Bulat F Garifullin et al. Nat Prod Res. 2021 Apr.

Abstract

A series of conjugates of diterpenoid isosteviol (16-oxo-ent-beyeran-19-oic acid) and N-acetyl-D-glucosamine was synthesised and their cytotoxicity against several human cancer cell lines (M-Hela, MCF-7, Hep G2, Panc-1, PC-3), as well as normal human cell lines (WI-38, Chang liver) was assayed. Most of the conjugates were found to be cytotoxic against the mentioned cancer cell lines in the range of IC50 values 13-89 µM. Two lead compounds 14a and 14b showed selective cytotoxicity against M-Hela (IC50 13 and 14 µM) that was two times as high as the cytotoxicity of the anti-cancer drug Tamoxifen in control (IC50 28 µM). It was found that cytotoxic activity of the lead compounds against M-Hela cells is due to induction of apoptosis.

Keywords: N-Acetyl-D-glucosamine; conjugates; cytotoxicity; diterpenoids; isosteviol.

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