Abstract

To enrich the bioactive cycloartane triterpenoid glycoside named actein and find out more cytotoxic cycloartane triterpenes, a phytochemical study of Cimicifuga foetida was conducted. 113 g (0.17%) actein was purified by recrystallization while eight cycloartane-type triterpenes (1–8) were isolated from the mother liquid. The chemical structures of new compounds (1–4) were elucidated by 1D and 2D NMR and HRESIMS spectroscopic analyses. Moreover, new compounds showed moderate and broad-spectrum cytotoxicity against 5 human cancer cell lines with IC50 values ranging from 4.02 to 15.80 μM.Graphic

Highlights

  • 2 Results and DiscussionCimicifuga foetida, commonly known as “shengma”, is a famous traditional chinese medicine native to china

  • The cyclolanostane triterpenoid glycosides of Cimicifuga genus have been noticed for their strong cytotoxic activities on cancer, especially breast cancer

  • Actein is the representative cyclolanostane triterpene isolated from Cimicifuga, exhibited an anti-angiogenic and anti-cancer activities on human breast cancer models by suppressing the protein expressions JNK/ERK pathways

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Summary

Results and Discussion

Cimicifuga foetida, commonly known as “shengma”, is a famous traditional chinese medicine native to china. 49.1 q 170.5 s 22.0 q 107.2 d 75.6 d 74.8 d 73.0 d 63.01 t arabinopyranoside (5) [22], 3′-O-acetyl-actein (7) [23], 25-O-acetylcimigenol-3-O-β-d-xylopyranoside (8), were isolated and identified These isolated new compounds (1‒4) were evaluated for their cytotoxicities against HL-60, SMMC-7721, A-549, MCF-7, and SW-480 cell lines (Table 3). Based on the above results, we found that the cytotoxic activities of new compounds, which means these substituents (like acetyl, butenoyl or methoxyloxo-propionyl) attached to sugar unit may contribute to inhibition activity In this present study, a great amount of high-purity actein were obtained by recrystallization, which laid a material foundation for the pre-clinical research. Compounds 1‒4 isolated from the mother liquid showed inhibition activity to different cancer cell lines, which provide chemical model for discovering potential anticancer agents, and a proof for further development and utilization of Cimiciguga genus

General Experimental Procedures
Extraction and Isolation
Characteristic Data of Compounds
Cytotoxicity Assay
Findings
Hydrolysis and Identification of the Sugar Moieties in Compounds 1–4
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