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目的:对山胡椒根的化学成分进行研究,并探讨其分离得到的生物碱成分对4种肿瘤细胞株增殖抑制活性。方法:采用硅胶柱层析、RP-18和Sephadex LH-20等多种色谱分离方法并结合MS、NMR等波谱解析技术及与文献数据对比,鉴定山胡椒根中生物碱及萜类成分,对分离得到的生物碱进行抗肿瘤活性测试。结果:从山胡椒根共分离得到10个化合物,分别鉴定为:木兰箭毒碱(1)、N-甲基樟苍碱(2)、樟苍碱(3)、波尔定碱(4)、去甲异波尔定碱(5)、去甲异紫堇定碱(6)、对$烷-反式-3,8-二醇(7)、对$烷-顺式-3,8-二醇(8)、eudesm-4(15)-ene-7,11-diol(9)、4β,6β-dihydroxy-1α,5β(H)-guai-9-ene(10)。化合物2~4对4种肿瘤细胞HT-29、SGC-7901、SMMC-7721和A549增殖均具有抑制活性。结论:其中,化合物1~6为生物碱类成分,化合物1、9和10为首次从该植物中分离得到。化合物2具有强烈的抑制肿瘤细胞增殖活性,特别是抑制结肠癌细胞HT-29、胃癌细胞SGC-7901细胞增殖活性,在中、高浓度给药情况下,甚至优于同浓度的阳性对照药物依托泊苷VP-16。
OBJECTIVE: To study the chemical constituents of pepper root and explore the inhibitory activities of alkaloids isolated from them on the proliferation of four tumor cell lines. Methods: The alkaloids and terpenoids in pepper root were identified by silica gel column chromatography, RP-18, Sephadex LH-20 and other chromatographic methods combined with MS and NMR spectral analysis techniques and compared with the literature data The alkaloids isolated were tested for anti-tumor activity. Results: A total of 10 compounds were isolated from Rhizoma Pepper and identified as Magnolins (1), N-Methylzanthogen (2), Camphogenine (3) (5), Norcordine (6), alkane-trans-3,8-diol (7) Diol (8), eudesm-4 (15) -ene-7,11-diol (9), 4β, 6β-dihydroxy-1α, 5β (H) -guai-9-ene (10). Compounds 2 ~ 4 inhibited the proliferation of four tumor cell lines HT-29, SGC-7901, SMMC-7721 and A549. Conclusion: Among them, compounds 1 to 6 are alkaloids, and compounds 1, 9 and 10 are isolated from this plant for the first time. Compound 2 has a strong inhibitory effect on the proliferation of tumor cells, in particular, inhibits the proliferation activity of colon cancer cells HT-29 and gastric cancer cells SGC-7901 cells, and even better than the same concentration of positive control drugs under medium and high concentration administration Parkin VP-16.