Novel terpestacin derivatives with l-amino acid residue as anticancer agents against U87MG-derived glioblastoma stem cells

Arthproliferins A–D, Four New Sesterterpenes from the Mangrove-Sediment-Derived Fungus Arthrinium sp. SCSIO41221

“…Based on our isolated terpestacin, seventeen derivatives with various L-amino acid side chains were designed and synthesized. Their anticancer activities against U87MG-derived glioblastoma stem cells (GSCs) were evaluated, and two derivatives showed stronger activities related to their further development as anticancer agents for the treatment of GBM by targeting the GSCs [17].…”

“…All of the compounds were evaluated for their cytotoxic activities against the human cancer cells MDAMB-231, C4-2B, MGC803, MDA-MB-468, and A549 using the CCK-8 method, but they exhibited no inhibitory activities at 5 µM. The primary screening of compounds 2, 5, and 6 regarding the proliferation of U87MG-derived GSCs was carried out using an ATP-monitoring luminescence assay [17]. The results revealed that terpestacin (6) exhibited significant activity, with an IC 50 value of 20.3 µM, compared to the positive control A1938, with an IC 50 value of 10.9 µM.…”

“…Although very few have been found, they have shown significant biological activities [16]. Great interest in these sesterterpenes has come from the finding that terpestacin was shown to effectively inhibit the formation of syncytia, the angiogenesis, without affecting the endothelial cell viability and the extracellular signal-regulated kinase activity [17,18]. Several total syntheses of terpestacin have been reported to date, and a series of active derivatives have also been designed and synthesized [17,19,20].…”

“…Great interest in these sesterterpenes has come from the finding that terpestacin was shown to effectively inhibit the formation of syncytia, the angiogenesis, without affecting the endothelial cell viability and the extracellular signal-regulated kinase activity [17,18]. Several total syntheses of terpestacin have been reported to date, and a series of active derivatives have also been designed and synthesized [17,19,20]. These results demonstrate that terpestacin analogues for treatment as anticancer and anti-HIV agents might offer promising research outcomes, and they encourage us that more effort is worth spending in this prospective field.…”

Prospects of marine-derived compounds as potential therapeutic agents for glioma

“…Compounds 13 and 15 effectively induced apoptosis and significantly inhibited GSC invasion (95% and 97% inhibition, respectively, at 2.5 μM) (Liao et al. 2023 ).…”