目的 研究徐长卿Cynanchum paniculatum逆转肿瘤多药耐药活性部位的化学成分。方法 MTT法评价徐长卿提取物分离部位逆转3种人肿瘤耐药细胞株对临床常用化疗药物的耐药作用,采用ODS柱色谱和制备HPLC等技术方法对活性部位进行分离,运用理化性质和波谱数据鉴定化合物结构。结果 徐长卿提取物分离部位显著逆转人胃癌耐药细胞株SGC-7901/VCR和人结肠癌耐药细胞株HCT-8/VCR对5-氟尿嘧啶(5-FU)的耐药作用。从活性部位中分离得到9个化合物,分别鉴定为华北白前苷元B 3-O-β-D-吡喃夹竹桃糖苷(1)、3β,14-二羟基-14β-孕甾-5-烯-20-酮(2)、新白薇苷元F(3)、白前苷元A(4)、白前苷元C(5)、新白薇苷元F 3-O-β-D-吡喃夹竹桃糖苷(6)、白前苷元C 3-O-β-D-吡喃黄花夹竹桃糖苷(7)、白前苷元A 3-O-β-D-吡喃夹竹桃糖苷(8)、20-羟基-4,6-二烯-孕甾-3-酮(9)。结论 化合物1为新化合物,命名为徐长卿苷D;徐长卿C₂₁甾体化合物具有潜在的逆转肿瘤多药耐药作用。

Objective To investigate the chemical consituents from the active fraction in the roots and rhizomes of Cynanchum paniculatum with reversal activity of multidrug resistance. Methods The active fraction was evaluated for reversing activities toward three human drug-resistance cell lines to clininally common used anticancer chemotherapeutic drugs. The compounds were isolated and purified by chromatography on ODS and preparative HPLC. Their structures were elucidated on the basis of chemical and spectroscopic methods, including MS, 1D, and 2D NMR spectral techniques. Results The active fraction exhibited the significant effects in sensitization of human drug-resistance on gastric carcinoma cell line SGC-7901/VCR and human drug-resistance on colonic carcinoma cell line HCT-8/VCR to fluorouracil (5-FU). Nine compounds were isolated and identified as hancogenin B 3-O-β-Doleandropyranoside (1), 3β,14-dihydroxy-14β-pregn-5-en-20-one (2), neocynapanogenin F (3), glaucogenin A (4), glaucogenin C (5), neocynapanogenin F 3-O-β-D-oleandropyranoside (6), glaucogenin C 3-O-β-D-thevetoside (7), glaucogenin A 3-O-β-Doleandropyranoside (8), and 20-hydroxypregna-4,6-dien-3-one (9). Conclusion Compound 1 is a new steroidal saponin named paniculatumoside D. C₂₁ Steroids isolated from the active fraction in the roots and rhizomes of C. paniculatum have the potential value as multidrug resistance reversing agents.

国家自然科学基金资助项目(81273396);山东省高等学校科技计划项目(J15LM12)