Abstract

An activity-directed fractionation and purification process was used to isolate antitumor compounds from the roots of Belamcanda chinensis (L.) DC. The ethyl acetate extract showed greater antitumor activities than the other extracts, consequently leading to the isolation of 18 compounds identified as β-sitosterol (1), dausterol (2), quercetin (3), kampferol (4), shikimic acid (5), gallic acid (6), ursolic acid (7), betulin (8), betulonic acid (9), betulone (10), tectoridin (11), irisflorentin (12), 4′,5,6-trihydroxy-7-methoxyisoflavone (13), tectorigenin (14), irilins A (15), iridin (16), irigenin (17), and iristectongenin A (18). Compounds 3–10, 13, and 15 were isolated from B. chinensis for the first time. Compounds 4 and 7–10 showed potent cytotoxic activities against PC3, MGC-803, Bcap-37, and MCF-7 cell lines. The mechanism of the antitumor action of compound 7 was preliminarily investigated through acridine orange/ethidium bromide (AO/EB) staining, Hoechst 33258 staining, and terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay, which indicated the growth inhibition of MGC-803 cells via the induction of tumor cell apoptosis.

Highlights

  • Belamcanda chinensis (L.) DC from the Iridaceaefamily consists of about 60 genera and 800 species worldwide and mainly two genera (Iridacea and Belamcanda) in China

  • During the screening for the antitumor agents from tropical medicinal plants, the ethyl acetate extract of B. chinensis exhibited great antitumor activity, and some of the compounds isolated from the ethyl acetate extract showed moderate antitumor activity against PC3, MGC-803, Bcap-37, MCF-7 cell lines and less cytotoxic activities toNIH3T3 cells which suggesting that these compounds can be used as lead compounds for further research

  • Each solvent extraction process was performed twice, and the extracts were combined and concentrated using a vacuum rotary evaporator at 50 °C to afford the petroleum ether extract (40 g), ethyl acetate extract (289 g), and methanol extract (321 g), respectively, which were evaluated for their antitumor activity using an MTT assay

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Summary

Introduction

Belamcanda chinensis (L.) DC from the Iridaceaefamily consists of about 60 genera and 800 species worldwide and mainly two genera (Iridacea and Belamcanda) in China. The Chinese Pharmacopoeia (2005 edition) listed B. chinensis as an official drug, which showed that the plant could be used as an anticancer herb. We have recently investigated the chemical constituents of B. chinensis systematically, and we tested the antitumor activity of the extracts and compounds. Ten of the compounds were isolated from B. chinensis for the first time. During the screening for the antitumor agents from tropical medicinal plants, the ethyl acetate extract of B. chinensis exhibited great antitumor activity, and some of the compounds isolated from the ethyl acetate extract showed moderate antitumor activity against PC3, MGC-803, Bcap-37, MCF-7 cell lines and less cytotoxic activities toNIH3T3 cells which suggesting that these compounds can be used as lead compounds for further research

Isolation and Identification
Antitumor Activities
Investigation of Cell Apoptosis
Hoechst 33258 Staining
General Procedures and Reagents
Plant Materials
Extraction and Isolation of Antitumor Compounds
Spectroscopic Data
Cell Lines and Culture
MTT Assays
TUNEL Assay
3.10. Statistical Analysis
Conclusions

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