Bioactive flavonoids from plant extract of Pyrethrum pulchrum and its acute toxicity

Pyrethrum pulchrum Ledeb. has been a phytochemically unexplored Mongolian medicinal folklore plant. In this study, its total flavonoid content was determined and fourteen flavonoids (1-14) were isolated from the aerial parts of P. pulchrum. Their structures were elucidated on the basis of spectroscopic data. The compounds 12-14, methoxyflavones, were tested for antiproliferative and cytotoxic activity against A549, HeLa, K-562, THP-1 and HUVEC cell lines. This is the first report on the effects of 5,7,4'-trihydroxy-3,6,3'-trimethoxyflavone (13) against all tested cell lines and it exhibited potent activity against chronic myeloid leukemia K-562 and acute monocytic leukemia THP-1 cells, each with GI₅₀ value at 2.0 μg/mL. The 5,4'-dihydroxy-3,6,7,3'-tetramethoxyflavone (14) showed the most potent activity against THP-1 (GI₅₀ = 1.1 μg/mL) and the highest cytotoxicity (5.6 μg/mL). In addition, acute toxicity of plant ethanol extract was evaluated and the lethal dose (LD₅₀) was estimated at 1048 mg/kg.

Keywords: Pyrethrum pulchrum; Asteraceae (Compositae); antiproliferative activity; cytotoxicity; flavonoid.