Chemical constituents from Carpesium cernuum and their anti-leukemia activities in vitro

Abstract

In order to study the chemical constituents from Carpesium cernuum and their inhibitory effects on leukemia cells in vitro. The chemical constituents from ethyl acetate fraction of C. cernuum were isolated and purified by silica gel column chromatography, Sephadex LH-20 column chromatography and macroporous adsorption resin, and their structures were identified by means of various spectroscopic techniques such as 1H NMR, 13C NMR and MS. The inhibitory effects of compounds 1-10 on leukemia cells (K562, HEL) in vitro were determined by MTT assay. The results were as follows: (1) Eleven compounds were isolated and identified as 2, 9-epoxy-5, 9-dihydroxy-8-angeloyloxy-11-methoxymethyl-4(15)-germacraen-6, 12-olide (1), cardivin D (2), cernuumolide I (3), cernuumolide J (4), 8-hydroxy-9, 10-diisobutyryloxythymol (5), (2E, 6Z, 10E, 12R)-7-［(acetyloxy)methyl］-3, 11, 15-trimethylhexadeca-2, 6, 10, 14-tetraene-1, 12-diol (6), 9, 10-dihydroxyoctadecanoate (7), 1, 6-dihydroxy-8-hydroxymethyl-anthraquinone (8), emodin (9), 4-megastigmen-3, 9-dione (10), β-sitosterol (11). Among them, Compound 1 was identified as a new compound, compounds 5, 7-10 were isolated from Carpesium for the first time, compounds 2, 5-10 were isolated from C. cernuum for the first time. (2) The results of activity test showed that cardivin D (2), cernuumolide I (3) and cernuumolide J (4) had good inhibitory effects on leukemia cells in vitro. The IC50 of compounds 2-4 against K562 cells and HEL cells were (2.27 ± 0.46), (5.53 ± 0.41), (3.90 ± 0.80) μmol·L-1 and (1.84 ± 0.14), (2.36 ± 0.90), (2.31 ± 1.17) μmol·L-1, respectively. The study enriches the chemical constituents of C. cernuum, and provides a material basis for the development of anti-leukemia drugs.

Keywords

• carpesium cernuum
• chemical constituents
• isolation and purification
• structure identification
• leukemia cells
• inhibition effect