提高先导化合物活性重现性试验
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摘要
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。
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 storage 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.
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 storage 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.
引文
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[2]逄森,袁会珠,李保同,等.利用96孔板建立除草剂微量活体筛选方法初探[J].农药学学报,2005,7(4):334-338,
[3]许勇华,台方俊,陈杰.新农药创制中除草活性评价程序及方法概述[J].现代农药,2009(5):17-20.
[4]王成菊,张文吉.杀虫剂生物测定方法浅谈[J].农药科学与管理,1999,20(3):28-29.
[5]侯华民,黄春霞.试谈新型杀虫化合物的生物活性测定[J].浙江化工,2000,31(S1):123-125.