title: Screening epidermal growth factor receptor antagonists from Radix et Rhizoma Asari by two-dimensional liquid chromatography.
abstract: 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.
authors.affiliation: School of Pharmacy, Xi'an Jiaotong University Health Science Center, Xi'an, China.
authors.forename: Shengli
authors.initials: S
authors.lastname: Han
authors.forename: Jing
authors.initials: J
authors.lastname: Huang
authors.forename: Jingjing
authors.initials: J
authors.lastname: Hou
authors.forename: Sicen
authors.initials: S
authors.lastname: Wang
mesh_terms: D030023:Asarum / Q000737:chemistry*; D002853:Chromatography, Liquid / Q000295:instrumentation / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000295:instrumentation; D004365:Drugs, Chinese Herbal / Q000032:analysis*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D006801:Humans; D010936:Plant Extracts / Q000032:analysis*; D027343:Rhizome / Q000737:chemistry*
chemical_list: D004365:Drugs, Chinese Herbal; D010936:Plant Extracts; D066246:ErbB Receptors
keywords: Asarinin; Cell membrane chromatography; Epidermal growth factor receptors; High-performance liquid chromatography with mass spectrometry; Radix et Rhizoma Asari