Cytotoxic sesquiterpene lactones from Vernonia bockiana
2012
LIAO, Shang-Gao | Wang, Zhen | Li, Jing | Liu, Ying | LI, Yue-Ting | ZHANG, Li-Juan | LONG, Qing-De | WANG, Yong-Lin
AIM: To investigate antitumor compounds from Vernonia bockiana. METHODS: The compounds were isolated by column chromatography and preparative HPLC. Their structures were elucidated by ¹H and ¹³C NMR spectroscopic methods and MS experiments. The antitumor activity was evaluated by testing their cytotoxicity against the human promyelomonocyte leukemic cell line HL-60 by the MTT method. RESULTS: Six sesquiterpene lactones, 8α-(4-hydroxymethacryloyloxy)-10α-hydroxy-13-methoxyhirsutinolide (1), 8α-methacryloyloxy-10α-hydroxy-13-O-methylhirsutinolide (2), piptocarphin A (3), 8α-[4-hydroxymethacryloyloxy]-10α-hydroxyhisutinolide-13-O-acetate (4), piptocarphin F (5), and 8α-acetoxy-10α-hydroxy-13-O-methylhirsutinolide (6), and one known inone glycoside, saussureosides B (7), were isolated from the whole plant of V. bockiana. The six sesquiterpene lactones showed cytotoxic activity (IC₅₀ 3.87–12.5 μmol·L⁻¹) against the human leukemic cell line HL-60 while the inone glycoside 7 was inactive in the test. CONCLUSION: Compounds 1, 2, 6, and 7 were obtained for the first time from this plant; The sesquiterpene lactones present in V. bockiana were active as antitumor agents against the human leukemic cell line HL-60.
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