Two novel thiophenes, grijisyne A (1), and grijisone A (2), were isolated from the crude ethanolic extract of the roots of Echinops grijissi Hance. Their structures were determined by spectral methods, especially 2D NMR spectra. All the isolated compounds were tested for their anti-tumor activities against three human tumor cell lines, HL-60, K562, and MCF-7.
A new thiophene, echinothiophenegenol (1), together with seven known thiophenes was isolated from the crude ethanol extract of roots of Echinops grijisii Hance. The structure of 1 was elucidated on the basis of spectroscopic data. Compounds 2 and 5, isolated from the plant for the fi rst time, and compounds 1 -7 were tested for their cytotoxicity against two human cancer cell lines, HL60 and K562. The thiophenes showed better activity than the bithiophenes.
The crude ethanol extract of Pulsatilla chinensis (Bunge) Regel roots was extracted successively with light petroleum, dichloromethane and n-butanol. The light petroleum fraction (PEF) exhibited potent anti-proliferation activity on HL60 cells with an IC 50 value of 14 μg/mL. As a result, ICR mice transplanted with tumor strain S180 were employed for testing the effectiveness of drug administration of PEF. The tumor inhibitory rate was 36.7% at a dose of 20 mg/kg/d, which was higher than the positive control, which produced 31.5% inhibition. However, an unusual phenomenon was observed in that the tumor inhibitory response was reverse dose-dependent since tumor inhibition was only 19.5% at a dose of 180 mg/kg/d. GC-MS revealed that the main components of the PEF were C-19 and C-22 polyunsaturated fatty acids. Previous studies had revealed that polyunsaturated fatty acids exhibit either anti-tumor or tumor promoting activities, and so it is proposed that the effects of PEF on tumor growth is dependent on dosage.
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