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[摘要]
目的 对苏木Caesalpiniasappan水提物中化学成分进行分析及有效成分的结构表征。方法 采用高效液相色谱串联质谱法(HPLC-MS/MS)分析苏木水提物中的化学成分,考察苏木水提物对膀胱癌T24细胞的杀伤作用,使用柱色谱法对其中主要化学成分巴西苏木素进行分离纯化以及使用核磁共振(NMR)进行结构表征。结果 经HPLC-MS/MS对苏木水提物进行分析,共检出16种化合物,鉴定出14种,其主要成分分别为槲皮素、巴西苏木素、异甘草素、原苏木素B、brazil A、3′-去氧苏木醇、4-O-hydroxybrazilin、苏木查耳酮、(αS)-α, 2′, 4, 4′-tetrahydroxydihydrochalcone等。其中巴西苏木素针对膀胱癌T24细胞的杀伤试验结果表明癌细胞的杀伤率与主要成分巴西苏木素浓度呈正相关。通过分离纯化得到了苏木水提物中巴西苏木素的纯品。结论 为苏木水提物中化学成分的鉴定提供了新的方法,为今后研究苏木的药用功能提供了依据。
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[Abstract]
Objective To investigate, purify, and characterize the active ingredients in the aqueous extract from Sappan Lignum (the dry heartwood of Caesalpinia sappan). Methods HPLC-MS/MS was used in the analysis of the chemical constituents in the aqueous extract from Sappan Lignum. Then the inhibitory effect of the aqueous extract from Sappan Lignum on human bladder tumor cell line T24 in vitro was studied. The main chemical constituents were purified by column chromatography and their structures were characterized by NMR. Results In the aqueous extract from Sappan Lignum, 16 compounds were separated and detected well by HPLC-MS/MS and 14 were identified. The main compounds were quercetin, brazilin, isoliquiritigeni, protosappanin B, brazil A, 3’-deoxysappanol, 4-O-hydroxybrazilin, sappanchalcone, and (αS)-α, 2’, 4, 4’-tetrahydroxy dihydrochalcone. The killing rate of cancer cells was positively correlated to the concentration of the main component which was brazilin. At last, according to the purification by column chromatography and the structural characterization by NMR, we obtained the pure brazilin in the aqueous extract from Sappan Lignum. Conclusion The research offers a new method for the identification of the components in the aqueous extract from Sappan Lignum and provides a basis for the medicinal functions of Sappan Lignum for future study.
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[基金项目]
国家自然科学基金资助项目(31171748);山西省国际科技合作项目(2013081051);山西省普通高校特色重点学科建设项目