南川斑鸠菊中的抗肿瘤倍半萜内酯(英文)

Cytotoxic sesquiterpene lactones from Vernonia bockiana

目的:研究南川斑鸠菊中的抗肿瘤活性成分方法:采用层析柱和制备高效液相进行化合物分离,运用1H和13CNMR及MS等波谱分析技术鉴定化合物结构;采用MTT法进行7个化合物对人骨髓白血病细胞(HL-60)的体外细胞毒实验。结果:分离得到6个倍半萜内酯[8α-(4-hydroxymethacryloyloxy)-10α-hydroxy-13-methoxyhirsutinolide(1),8α-methacry-loyloxy-10α-hydroxy-13-O-methylhirsutinolide(2),piptocarphin A(3),8α-[4-hydroxymethacryloyloxy]-10α-hydroxyhisutinolide-13-O-acetate(4),piptocarphin F(5)以及8α-acetoxy-10α-hydroxy-13-O-methylhirsutinolide(6)]和1个inone苷saussureosides B(7);6个倍半萜内酯(1-6)具有抑制人骨髓白血病细胞(HL-60)的活性(IC503.87-12.5μmol·L-1),但inone苷saussureosides B(7)对HL-60没有抑制活性。结论:化合物1,2,6和7首次从该植物中得到;南川斑鸠菊中的倍半萜内酯类化合物具有抗肿瘤活性。

AIM：To investigate antitumor compounds from Vernonia bockiana.METHODS：The compounds were isolated bycolumn chromatography and preparative HPLC.Their structures were elucidated by 1H and 13C NMR spectroscopic methods and MSexperiments.The antitumor activity was evaluated by testing their cytotoxicity against the human promyelomonocyte leukemic cell lineHL-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）,andone known inone glycoside,saussureosides B（7）,were isolated from the whole plant of V.bockiana.The six sesquiterpene lactonesshowed cytotoxic activity（IC50 3.87-12.5 μmol·L-1） against the human leukemic cell line HL-60 while the inone glycoside 7 wasinactive in the test.CONCLUSION：Compounds 1,2,6,and 7 were obtained for the first time from this plant;The sesquiterpenelactones present in V.bockiana were active as antitumor agents against the human leukemic cell line HL-60.