Liu Xuehui, Zhou Rongrong, Shen Bingbing, Chen Lin, Zhou Qingyijun, Wan Dan, Huang Luqi, Zhang Shuihan
Hunan Academy of Chinese Medicine, Research Institute of Chinese Medicine, Changsha, China.
Changchun University of Chinese Medcine, College of Pharmacy, Changchun, China.
Curr Pharm Biotechnol. 2017;18(13):1106-1114. doi: 10.2174/1389201019666180226145427.
Lonicera macranthoides is a Chinese herb that contains a large number of bioactive spanions possessing important pharmacological activities, such as anti-tumour activity. However, detailed information about their anti-tumor activity and bioactive compounds is limited.
In order to evaluate the scientific basis, the method of high-speed counter-current chromatography (HSCCC) combined with high performance liquid chromatography mass spectrometry (HPLC-ESI-QTOF/MS) has been developed to separate, purify and analyze saponins from Lonicera macranthoides. Four main saponins, Macranthoidin B (I), Macranthoidin A (II), Macranthoides B (III) and Akebia saponin D (IV) were separated by HSCCC with the solvent systems of ethyl acetate-nbutanol- water (3:2:5) and n-butanol-water-methanol-ethyl acetate (1:6:0.5:4). The purities of these four bioactive ingredients (I-IV) identified and detected by HPLC-ESI-QTOF/MS were 95.1%, 92.7%, 91.8% and 96.3%, respectively. The separated saponins were evaluated for their cytotoxic activities against six tumor cell lines (MCF-7, Hela, A549, HepG2, HT29 and Eca109).
Results show that compounds I-IV exhibited particular significant anti-tumor activities against human mammary adenocarcinoma MCF-7 cell with IC50 values ranging from 12.7 to 30.8 µM.
It was demonstrated that the combinative method using HPLC-ESI-QTOF/MS and HSCCC was suitable for rapid screening and isolating saponins of Lonicera macranthoides and the isolated compounds have great potential for the development of new antitumor drugs.
灰毡毛忍冬是一种中国草药，含有大量具有重要药理活性的生物活性成分，如抗肿瘤活性。然而，关于其抗肿瘤活性和生物活性化合物的详细信息有限。
为了评估其科学依据，已开发出高速逆流色谱（HSCCC）结合高效液相色谱质谱联用（HPLC-ESI-QTOF/MS）的方法，用于分离、纯化和分析灰毡毛忍冬中的皂苷。通过HSCCC，采用乙酸乙酯-正丁醇-水（3:2:5）和正丁醇-水-甲醇-乙酸乙酯（1:6:0.5:4）的溶剂系统，分离出四种主要皂苷，即灰毡毛忍冬皂苷B（I）、灰毡毛忍冬皂苷A（II）、灰毡毛忍冬皂苷B（III）和木通皂苷D（IV）。通过HPLC-ESI-QTOF/MS鉴定和检测的这四种生物活性成分（I-IV）的纯度分别为95.1%、92.7%、91.8%和96.3%。对分离得到的皂苷进行了针对六种肿瘤细胞系（MCF-7、Hela、A549、HepG2、HT29和Eca109）的细胞毒性活性评估。
结果表明，化合物I-IV对人乳腺腺癌MCF-7细胞表现出特别显著的抗肿瘤活性，IC50值范围为12.7至30.8μM。
证明了使用HPLC-ESI-QTOF/MS和HSCCC的联合方法适用于快速筛选和分离灰毡毛忍冬中的皂苷，且分离得到的化合物在开发新型抗肿瘤药物方面具有巨大潜力。
