Han Shengli, Huang Jing, Hou Jingjing, Wang Sicen
School of Pharmacy, Xi'an Jiaotong University Health Science Center, Xi'an, China.
J Sep Sci. 2014 Jul;37(13):1525-32. doi: 10.1002/jssc.201400236. Epub 2014 May 15.
Radix et Rhizoma Asari is a traditional Chinese medicine, and has many pharmacological effects, such as calming, analgesia, anti-inflammation, antiarrhythmic, antihypertensive, antivirus, etc. But few studies have screened the active compounds from extracts of Radix et Rhizoma Asari for tumor therapy. In this study, a two-dimensional liquid chromatography system was built to screen active compounds acting on epidermal growth factor receptor (EGFR) from Radix et Rhizoma Asari. The screening result showed that asarinin from Radix et Rhizoma Asari was the targeted component that could act on EGFR specificity. The competitive binding assay and molecular docking assay results showed asarinin binding with EGFR in similar manner as with gefitinib, which was used as a positive control drug. Then the antitumor effect of asarinin was studied through cell growth assay in vitro. The results showed that gefitinib and asarinin could inhibit highly expressed EGFR cell growth in a dose-dependent manner in the range of dose from 0.10 to 102.4 μM. This two-dimensional liquid chromatography system will be a useful method in drug discovery from natural medicinal herbs for searching potential antitumor candidates.
细辛是一种传统中药，具有多种药理作用，如镇静、镇痛、抗炎、抗心律失常、降压、抗病毒等。但很少有研究从细辛提取物中筛选用于肿瘤治疗的活性化合物。在本研究中，构建了二维液相色谱系统，以从细辛中筛选作用于表皮生长因子受体（EGFR）的活性化合物。筛选结果表明，细辛中的细辛脂素是能够特异性作用于EGFR的目标成分。竞争结合试验和分子对接试验结果表明，细辛脂素与EGFR的结合方式与作为阳性对照药物的吉非替尼相似。然后通过体外细胞生长试验研究了细辛脂素的抗肿瘤作用。结果表明，在0.10至102.4 μM的剂量范围内，吉非替尼和细辛脂素均可剂量依赖性地抑制高表达EGFR细胞的生长。这种二维液相色谱系统将成为从天然草药中发现药物以寻找潜在抗肿瘤候选物的一种有用方法。
