提出了基于亲和阵列及色谱联用系统的中药及天然产物活性成分高通量筛选方法。相对于先纯化后筛选的方法,利用先亲和再分离鉴定的方法更像从大量的鱼群中钓鱼,钓钩上的鱼饵不同,上钩的鱼会有差异。鱼饵类似于各种不同的生物作用靶点,将各类靶点固定后进行亲和吸附,吸附后的成分再进行色谱分离及色谱联用技术进行结构鉴定,将大大提高生物活性成分筛选的命中率。通过各类靶点亲和柱进行阵列后,可同步提高不同靶点筛选的通量。因此我们称这种筛选方式为:钓鱼法。以此方法为基础,介绍了从中药中筛选血管紧张素转换酶抑制剂的过程。
A novel "angling" method for the rapidly screening of bio-active component in Traditional Chinese Medicines (TCM) and natural products basing on the hyphenation of affinity column array with HPLC was proposed. The biotargets such as enzyme, receptor etc were used as fish baits on the fishhooks to "fish" the bio-active components from a complicated mixture library, i.e. TCMs and natural products. After affinity absorption, the high affinity com- ponents were transported to a hyphenated HPLC system to identify the chemical structures. The affinity array could provide the different target affinities of the components in the sample solution. Basing the method, a screening strategy for the angiotensin converting enzyme inhibitor from TCMs was presented.