栀子的化学成分及抗白血病活性研究

Active constituents from Gardenia jasminoides against acute lymphoblastic leukemia

目的阐明栀子Gardenia jasminoidesEllis中抗急性淋巴细胞白血病的活性成分。方法用色谱方法分离栀子中化学成分,用波谱技术(IR,ESI-MS,1H-NMR,13C-NMR)进行结构鉴定,用四唑盐(MTT)比色法测定化合物对白血病细胞(HL-60-人早幼粒细胞白血病、REH-人急性淋巴细胞白血病、Raji-淋巴瘤)增殖的影响。结果分离鉴定了8个化合物:β-谷甾醇(1),5-羟基-7,3′,4′,5′-四甲氧基黄酮(2),熊果酸(3),D-甘露醇(4),栀子苷(5),去乙酰车叶草甙酸甲酯(6),京尼平-1-β-龙胆苷(7),鸡矢藤次苷甲酯(8)。化合物3对3种白血病细胞增殖均表现出了一定的抑制作用,其中对REH细胞系抑制活性最强,IC50为7.5μg/mL。结论化合物3具有抗急性淋巴细胞白血病的作用。

Objective To determine lymphoblastic leukemia. Methods the active constituents from Compounds were isolated Gardenia jasminoides against acute and purified by various column chromatographic techniques and their structures were elucidated on the basis of spectral analysis （ IR, ESI- MS, ^1H-NMR, ^13C-NMR）. The inhibitory activity against the proliferation of HL-60, REH and Raji cell lines was determined by using MTT assay. Results Eight compounds were isolated and identified as β- sitosterol （ 1 ）, 5-hydroxy-7,3′, 4′, 5′-tetramethoxyflavone （ 2 ）, Ursolic acid （ 3 ）, D-mannitol （ 4 ）, geniposide （ 5 ）, deacetylasperulosidic acid methyl ester （ 6 ）, genipin-1-β-gentiobioside （7） and scandoside methyl ester （8）. Compound 3 exhibited inhibitory effects on leukemic cell proliferation in vitro with IC50 of 12.2, 7.5 and 15.4 μg/mL aginst HL-60, REH and Raji cell lines, respectively. Conclusion Ursolic acid might be one of the active ingredients against anti - acute lymphoblastic leukemia conferred by Gardenia jasminoides Ellis.