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Updated: May 6, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Ferula ferulaeoides(Steud.)Korov.の根から単離された、選択的な細胞毒性活性を持つテルペノイドアセトフェノン
Yewen Jia1, Wen Dang1, Xueni Zhang1
1School of Traditional Chinese Materia Medica, Key Laboratory of Innovative Traditional Chinese Medicine for Major Chronic Diseases of Liaoning Province, Key Laboratory for TCM Material Basis Study and Innovative Drug Development of Shenyang City, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Abstract:
Eleven undescribed terpenylated acetophenones (1, 2a/2b, 3a/3b, 4-6, 7a/7b, 8) and twelve known analogues (9a/9b, 10-12, 13a/13b, 14a/14b, 15, 16a/16b) were isolated from the roots of Ferula ferulaeoides (Steud.) Korov. (Apiaceae) by the guidance of bioactivity-guided approach. The structures and relative configurations of the new compounds were established by extensive analysis of UV, HR-ESI-MS, and NMR data, supported by 13C NMR calculations with custom DP4+ probability analysis. Through electronic circular dichroism, the absolute configurations of all compounds were determined for the first time. Cytotoxic activities of all compounds were evaluated against HCT-116, HT-29, and HCoEpiC cell lines, and most of them (1, 4, 7-15) showed significant or moderate selective cytotoxic activity toward colon cancer cells. Among them, compound 10 showed the most potent cytotoxic effects against HCT-116 cells (IC50, 8.23 ± 2.3 μM) and HT-29 cells (IC50, 12.43 ± 2.2 μM), while showing significantly lower cytotoxicity toward normal colonic epithelial cells (IC50, 52.26 ± 2.9 μM for HCoEpiC).
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