4-酰基吡唑啉酮-5缩γ-氨基丁酸衍生物的合成及对白玉菇菌丝脱氢酶活性影响  

Synthesis of the derivatives from 4-acylpyrazolone-5 and γ-aminobutyric acid and their effects on the dehydrogenase activity of Hypsizygus marmoreus mycelia

作　　者：王鑫 史芯沂美 谢芬兰 付壮 朱华玲 班立桐 Wang Xin;Shi Xinyimei;Xie Fenlan;Fu Zhuang;Zhu Hualing;Ban Litong(Tianjin Agricultural University,College of Basic Sciences,Tianjin 300392,China;Tianjin Agricultural University,College of Agronomy and Resource Environment,Tianjin 300392,China)

机构地区：[1]天津农学院基础科学学院,天津300392 [2]天津农学院农学与资源环境学院,天津300392

出　　处：《天津农学院学报》2022年第2期1-6,共6页Journal of Tianjin Agricultural University

基　　金：天津市大学生创新创业训练计划项目(202010061058);天津市蔬菜产业技术体系创新团队项目(ITTVRS2017015)。

摘　　要：采用结构拼接法设计合成了4-三氟乙酰-3-甲基-1-苯基-5-吡唑啉酮缩γ-氨基丁酸(L1)、1-苯基-3-甲基-4-苯甲酰基-5-吡唑啉酮缩γ-氨基丁酸(L2)两种新配体,以及两个配体的Ca、Zn配合物。采用红外分光光度法和紫外分光光度法对合成的6种化合物进行了结构表征,采用MTT法测定了6种化合物对白玉菇菌丝脱氢酶活性的影响。结果表明:6种化合物对白玉菇菌丝脱氢酶的活性均有抑制作用,其中配体L2对白玉菇菌丝脱氢酶活性的抑制能力最强,配体L1最差;采用分子对接法研究了菌丝脱氢酶与原始配体泛醌,以及配体L1和L2的相互作用,发现两个新配体与菌丝脱氢酶的结合能力均好于原始配体泛醌,且配体L2好于配体L1。该结果与MTT试验结果一致,说明配体L1和配体L2可能是通过与泛醌进行结合竞争表现出对琥珀酸脱氢酶的抑制活性。A new ligand(L1)derived from γ-aminobutyric acid and 4-trifluoroacetyl-3-methyl-1-phenyl-5-pyrazolone, and a new ligand(L2)derived from γ-aminobutyric acid and 1-phenyl-3-methyl-4-benzoyl-5-pyrazolone were synthesized and characterized by IR and UV, so did their Ca, Zn complexes. The inhibititted effect of the compounds on the mycelium dehydrogenase activity of Hypsizygus marmoreus was determined by MTT methods. The results showed that ligand L2 had stronger inhibitition ability to mycelium dehydrogenase while ligand L1 was the weaker. Molecular docking method was used to analysize the interaction of the mycelium dehydrogenase and the ligands. The results suggested that the two new ligands showed higher interactions to mycelium dehydrogenase than original ubiquinone, and ligand L2 showed higher interactions to mycelium dehydrogenase than ligand L1.

关 键 词：γ-氨基丁酸 衍生物 合成 表征 白玉菇 菌丝脱氢酶活性 

分 类 号：O621.1[理学—有机化学]