Wei Fen, Hu Qi, Huang Jing, Han Shengli, Wang Sicen
School of Pharmacy, Xi'an Jiaotong University, 76# Yanta West Road, Xi'an, 710061, China; National-Provincial Joint Engineering Research Center for Natural Vascular Medicine Screening & Analysis, Xi'an 710061, China.
School of Pharmacy, Xi'an Jiaotong University, 76# Yanta West Road, Xi'an, 710061, China; National-Provincial Joint Engineering Research Center for Natural Vascular Medicine Screening & Analysis, Xi'an 710061, China.
J Pharm Biomed Anal. 2017 Mar 20;136:134-139. doi: 10.1016/j.jpba.2017.01.005. Epub 2017 Jan 4.
Corydalis Thizoma,or Yuanhu in China, is a common herbal drug used for thousands of years as analgesic in Chinese medicine that has been reported to have potential anti-angiogenic effects. In this study, a VEGFR/cell membrane chromatography (VEGFR/CMC) coupled with HPLC- ESI-IT-TOF-MSn system was developed and successfully applied for identifying active components from YuanHu extract acting on VEGFR. We identified tetrahydropalmatine and corydaline as bioactive components with VEGFR activity, thus confirming their inhibitory activity on VEGFR engineered HEK293 cell growth by MTT assay. The activity of tetrahydropalmatine and corydaline was compared with the positive control sorafenib in a range of concentration from 6.25 to 50.0μM, showing a dose-dependent inhibitory trend. These results indicate that the VEGFR/CMC coupled with HPLC- ESI-IT-TOF-MSn system can purify and identify specific bioactive components from complex systems, thus representing a promising tool for screening molecules active towards VEGFR from natural herbs.
延胡索,在中国又称元胡,是一种常用草药,在中医中用作镇痛药已有数千年历史,据报道具有潜在的抗血管生成作用。在本研究中,开发了一种VEGFR/细胞膜色谱法(VEGFR/CMC)与HPLC-ESI-IT-TOF-MSn系统联用的方法,并成功应用于鉴定元胡提取物中作用于VEGFR的活性成分。我们鉴定出四氢巴马汀和紫堇碱为具有VEGFR活性的生物活性成分,从而通过MTT法证实了它们对VEGFR工程化HEK293细胞生长的抑制活性。在6.25至50.0μM的浓度范围内,将四氢巴马汀和紫堇碱的活性与阳性对照索拉非尼进行了比较,呈现出剂量依赖性抑制趋势。这些结果表明,VEGFR/CMC与HPLC-ESI-IT-TOF-MSn系统联用能够从复杂体系中纯化和鉴定特定的生物活性成分,因此是一种从天然草药中筛选对VEGFR有活性的分子的有前景的工具。