提高先导化合物活性重现性试验

摘要

In view of the instable reproducibility of re-fermentation activities in screening of lead compounds, the effects of storage time on the reproducibility of activity in screening process were studied. Several batches of re-fermentation samples were used to test against 3 insecticide targets and 4 herbicide targets. The results showed that in screening of strains in stor-age for 1 year, about 60% of screening samples lost their initial activities, but in screening of strains with half a year's storage, only about 40% of strains lost activities. Adjusting re-fermentation intervals according to the results, and changing the concentrated re-fermentation into a decentralized re-fermentation in synchronization, the re-fermentation in accordance with the preliminary screening concluded that about 81.56% strains could realize the preliminary screening activity, which greatly improved the detection efficiency of alternative compounds.%针对先导化合物筛选中出现的重复发酵活性重现性不稳定的问题，研究了筛选流程中菌种保藏时间对活性重现的影响，使用不同批次的重复发酵样品对3个杀虫活性筛选靶标和4个除草活性筛选靶标进行了试验。结果表明，使用保藏时间超过一年的菌种进行复筛，60%左右初筛样品失去原来的活性；而使用保藏时间在半年左右的菌种进行复筛，只有40%左右的菌株失去活性。根据这一结果，调整了筛选流程中重复发酵的间隔时间，变集中进行重复发酵为分散同步发酵，根据初筛结果同步进行的重复发酵，81.56%菌株的初筛活性可以重现，大大提高了备选化合物的检出效率。