瓜子金有效部位SubFra B3抗肿瘤活性及初步成分分析  

Antitumor activity and composition analysis of SubFra B3 from the effective fraction of Polygala Japonica Houtt.

作　　者：黄思而 谭钰霖 颜梦彤 王赢 李勇[1] 邓红[1] 张蜀[1] HUANG Sier;TAN Yulin;YAN Mengtong;WANG Ying;LI Yong;DENG Hong;ZHANG Shu(Center for Drug Research and Development,Guangdong Pharmaceutical University/Key Laboratory of Drug Formulation Research and Evaluation,Guangzhou 510006,China)

机构地区：[1]广东药科大学新药研发中心/广东省药物制剂研究与评价重点实验室,广东广州510006

出　　处：《广东药科大学学报》2025年第2期85-92,共8页Journal of Guangdong Pharmaceutical University

基　　金：广东省普通高校重点领域专项(乡村振兴)(2020ZDZX1030);广州市科技局重点研发计划项目(2024B03J1322)。

摘　　要：目的探索瓜子金抗肿瘤有效部位并进行初步成分分析,为其抗肿瘤有效成分及开发利用提供依据。方法利用大孔吸附树脂及反向硅胶柱层析从瓜子金醇提取物中分离富集SubFra B3部位,并基于CCK8法以6种肿瘤细胞株筛选SubFra B3的体外抗肿瘤活性,根据体外活性结果进一步构建斑马鱼肺癌模型,对SubFra B3进行体内抗肿瘤活性考察及验证,同时采用UPLC-Q-Exactive Orbitrap MS分析技术对该部位的有效成分进行分析鉴定。结果体内外抗肿瘤活性试验证明,SubFra B3对人急性T淋巴细胞白血病细胞(Jurkat T-cell lymphoma cells,Jurkat)、人慢性髓系白血病细胞(chronic myeloid leukemia cells,K562)、人宫颈癌细胞(henrietta lacks strain of cancer cells,Hela)、人非小细胞肺癌细胞(human non-small cell lung cancer cells,A549)、人类急性单核细胞白血病细胞(tohoku hospital pediatrics-1 cells,THP-1)、小鼠乳腺癌细胞(mouse breast cancer cells,4T1)6种肿瘤细胞均有不同程度的抑制作用,其中对A549细胞的抑制作用最强;当质量浓度为3.12μg/mL时,SubFra B3能显著抑制斑马鱼体内A549细胞的增殖;该有效部位由23个皂苷、8个黄酮(其中3个酮)、2个糖酯、1个酚类成分组成。结论SubFra B3为瓜子金抗肿瘤有效部位,其作用的有效成分主要为皂苷类,其次为黄酮类、酮类等成分。Objective To explore the antitumor effective fraction of Polygala Japonica Houtt.and preliminary component analysis,so as to provide a basis for its antitumor effective components and development and utilization.Methods The fraction of SubFra B3 was isolated and enriched from macroporous adsorptive resins and octadecylsilyl column chromatography,the in vitro antitumor activity of SubFra B3 was screened based on the CCK8 assay with six tumor cell strains,and a zebrafish lung cancer model was constructed based on the results of the in vitro activity to examine and validate the in vivo antitumor effective fraction of SubFra B3.The UPLC-Q-Exactive Orbitrap MS analysis was used to analyze and identify the active ingredients of its antitumor effective fraction.Results The in vitro and in vivo antitumor activity experiment proved that SubFra B3 inhibited six kinds of tumor cells about Jurkat,K562,A549,THP-1,4T1,and Hela with different degrees,among which the inhibitory effect was the strongest on the A549 human non-small cell lung cancer cells.SubFra B3 significantly inhibited the proliferation of A549 human non-small cell lung cancer cells in zebrafish at the concentration of 3.12μg/mL,the effective fraction consisted of 23 saponins,8 flavonoids(including 3 xanthones),2 glycol esters,1 phenolic and other components.Conclusion SubFra B3 is an active part of P.Japonica Houtt.,which has positive anti-tumor activity,and the active ingredient of its action is mainly saponins,followed by flavonoids and other components.

关 键 词：瓜子金 有效部位 抗肿瘤活性 UPLC-Q-Exactive Orbitrap MS 有效成分 

分 类 号：R917[医药卫生—药物分析学]