β-氨基丁酸-大黄酸耦合物的合成、生物活性及韧皮部传导性  

Synthesis ofβ-aminobutyric acid-Rhein conjugates and their bioactivity and phloem translocation

作　　者：胡慈银 王锦鹏 肖永欣 李俊凯[1,2] HU Ciyin;WANG Jinpeng;XIAO Yongxin;LI Junkai(School of Agriculture,Yangtze University,Jingzhou 434025,Hubei Province,China;Institute of pesticides,Yangtze University,Jingzhou 434025,Hubei Province,China)

机构地区：[1]长江大学农学院,湖北荆州434025 [2]长江大学农药研究所,湖北荆州434025

出　　处：《农药学学报》2023年第4期808-816,共9页Chinese Journal of Pesticide Science

基　　金：国家自然科学基金项目(31672069).

摘　　要：氨基酸-农药耦合物能够改善母体农药的内吸传导性,提高农药的使用效率,减少因没有到达靶标造成的浪费及对环境的污染。本研究以天然产物大黄酸为先导化合物、以β-氨基丁酸为导向基团,设计、合成了4个目标化合物,并检测了其对6种植物病原菌的抑菌活性,以及对小麦植株苯丙氨酸解氨酶(PAL)和过氧化物酶(POD)活性的影响及在蓖麻幼苗中的韧皮部传导性。结果表明,化合物4b(浓度0.5 mmol/L)不仅对水稻纹枯病菌Rhizoctonia solani Kühn具有一定的抑制活性(菌丝生长抑制率为53.5%),而且具有诱导抗性(持效期近7 d)和韧皮部传导性(渗出液浓度为15.1μmol/L)。该研究为兼具内吸传导性和诱导抗性杀菌剂的开发提供了新思路。Amino-pesticide conjugates enable to improve the systemic conductivity of parent ingredients,increase utilization efficiency,and decrease the waste that was caused by the unreached target and thus pollution to the environment.In this study,four target compounds were designed and synthesized using the natural product Rhein as the leading compound andβ-aminobutyric acid(BABA)as the directing group,and their antifungal activities against the six plant pathogens,effects on enzymatic activities of the phenylalanine ammonialyase(PAL)and peroxidase(POD)of wheat leaves,which were treated by the compounds,and their phloem translocation in Ricinus seedling were measured.The results showed that compound 4b(concentration at 0.5 mmol/L)had not only an inhibition effect on the Rhizoctonia solani Kühn(the inhibition rate of mycelial growth was 53.5%),but also an inducible resistance(duration was nearly 7 d),and phloem translocation(sap concentration was 15.1μmol/L).This study provides a new idea for developing systemic and inducible fungicides.

关 键 词：β-氨基丁酸-大黄酸耦合物 抑菌活性 诱导抗性 韧皮部传导性 

分 类 号：O626.2[理学—有机化学] TQ455.4[理学—化学]