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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。
OBJECTIVE: To study the antitumor activity components of Vernonia nakogenica.Methods: The compounds were separated by column chromatography and preparative high performance liquid chromatography. The structures of compounds were identified by 1H, 13CNMR and MS spectral analysis. Seven compounds were detected by MTT assay In vitro cytotoxicity test of myeloid leukemia cells (HL-60). Results: 6 sesquiterpene lactones [8α- (4-hydroxymethacryloyloxy) -10α-hydroxy-13-methoxyhirsutinolide (1) and 8α-methacry-loyloxy- piptocarphin A (3), 8α- [4-hydroxymethacryloyloxy] -10α-hydroxyhisutinolide-13-O-acetate (4), piptocarphin F (5) and 8α-acetoxy- 10α-hydroxy-13-O-methylhirsutinolide And one inosine saussureosides B (7). Six sesquiterpene lactones (1-6) inhibited the activity of human myeloid leukemia cells (HL-60) (IC503.87-12.5μmol·L-1) in inosine saussureosides B (7) has no inhibitory activity on HL-60. CONCLUSION: Compounds 1, 2, 6 and 7 were obtained from this plant for the first time. The sesquiterpene lactones in Vernonia lugens have anti-tumor activity.