实验总结摘要
2020-03-02 04:07:14 来源：范文大全收藏下载本文
实验总结
本实验室前期开展松香酸的分离、以及香豆素的合成工作，过程中发现松香酸以及香豆素都有优良的灭菌活性、一定程度的杀线虫活性；合作单位一直来在开发植物源农药，近年来着力开发治疗杀松线虫病的农药。双发利用各自的优势，开展先导化合物糖苷化修饰、生物活性筛选研究工作。
利用脱氢松香酸为原料合成12,14-二羟基脱氢松香酸。羟基化脱氢松香酸在抗菌、杀虫等方面有所提高。筛选具有抗原活性的纤维二糖元、麦芽糖元、木二糖元和木三糖元、壳聚糖（包括壳寡糖）。将12,14-二羟基脱氢松香酸与糖元缩合成糖苷，经过柱色谱分离纯化，并经过谱学鉴定。对目标产物的杀松线虫、灭菌活性进行筛选。采用浸渍法测定抗松线虫活性。目标产物糖苷的杀松线虫活性：1h LC50，19.2至34.2 μg/ml不等，最小抑菌浓度（Pantoea toletana）5.5至12 μg/mL不等。部分产物已经在林区进行树干基部打孔注入试验，超过目前合作企业的产品，效果良好。
还合成系列香豆素及其衍生物，从中筛选选出7-羟基-4-甲基香豆素具有良好的抗菌杀松线虫活性，在甲醛和有机伯胺或有机仲胺的作用下，经胺甲基化反应制得所需香豆素衍生物杀松线虫活性进一步提高。松材线虫线虫浸渍在香豆素及其衍生物溶液中的校正死亡率（24h，100 mg/L）5.88至38.83%不等，部分产物的活性超过天然成分补骨脂素。
目前，羟基脱氢松香酸糖苷合成收率低，杂质多，有待改进；而香豆素及其衍生物的合成产量与纯度均高。
In the proce of separation of abietic acid and synthesis of coumarin, we found rosin acid and coumarin has excellent bactericidal activity, a certain degree of nematocidal activity; the cooperative unit has been woking for decades in developing plant origin pesticides, and in recent years focusing on the development of treating pine nematode disease.Taking the respective advantages, wo carry out jointly the research work in lead compound modification, biological activity screening.12,14-Dihydroxyldehydroabietic acid is synthesized from dehydroabietic acid.The antibacterial and nematocidal activities of 12,14-dihydroxyldehydroabietic acid has been improved.Antigenic activity of cellose, maltose, xylobiose, xylotriose, chitosan (including chitosan oligosaccharides) are screened.12,14-Dihydroxyldehydroabietic acid glycosides are synthesized by condensation of glycogen and aglycone, separated and purified by chromatograph, and comfirmed by spectrum.The target products are screened for nematocidal and sterilization activities.Nematocidal activity is determined by dipping method.The activity of the target product glycosides (LC50, 1h) ranged from 19.2 to 34.2 g/ml, and the minimal inhibitory concentration (toletana Pantoea) ranged from 5.5 to 12 g/mL.Part of the product has been used in tree trunk hole injection test in forest, the effect is medium.
Novel uncyclized dialkylamido and cyclized benzo[1,3]xazin derivatives of coumarin were synthesized efficently
via
Mannich
reaction
from
the
starting
materials
of 4-methyl-7-hydroxylcoumarin, amine and formaldehyde.Both of uncyclized and cyclized reaction conditions were mild, and the cyclized reactions underwent easier than uncyclized ones.The coumarins derivatives showed nematocidal activities in vitro against Bursaphelenchus xylophilus, with mortality ranging from 5.88 to 23.43(3) to 38.83(3)% at concentrations of 100 mg/L.Part of the coumarin products show the nematocidal activity more than natural pytoproduct of Fructus Psoraleae.
At present, the synthesis of the acid glycosides is low in yield, and the impurities are much; whereas the synthesis of coumarine is high in yield and purity.
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