天然抗肿瘤分子筛选方法研究新进展

天然产物是抗癌药物的重要来源，全球应用的175种抗癌药物中，有57％直接或间接来源于天然产物^1]。但是全球的高等植物中仅6％做过生物活性筛选，15％经过植物化学的评价^2]，不到10％的药用植物经过详细的药理研究^3]。所以，从天然产物研发创新药物的潜能十分巨大。但是如何有效地从数目庞大的天然产物中找到具有抗肿瘤活性的分子，是目前药物研发亟待解决的瓶颈问题之一。G-四链体结构的发现及现代分子生物学技术对其生理功能的揭示，为解决目前药物研究的瓶颈问题提供了一个新的契机。

Research Progress on Fast Screening Potential Antitumar Agents from Natural Plant

The development of a simple and efficient method, which allows to fast screen compounds with high biological activity from natural plant extracts, is an attractive field in drug discovery. Our group propounded a novel method for fast screening and structural identification of antitumor agents from natural plant extracts by coupling the DNA target molecule＇ s recognition with NMR techniques. By introduction of DNA target molecule into natural plant extracts, the ligand （s） in the extracts will be recognized by target molecule and therefore can be monitored by NMR techniques. Our tactics includes the following three steps： judging the existence of G-quadruplex ligand（s） in the test extracts by 1H NMR spectra; detecting the characteristic peak （s） of G-quadruplex ligand（s） using DOSY NMR methods; and subsequently identifying the structure of G-quadruplex ligand （s） by 2D NMR experiments such as HSQC and HMBC. By the combination of G-quadruplex recognition and NMR methods, we have successfully obtained several active molecules stabilizing G-quadruplex with high cytotoxicity from two kinds of natural product extracts.