手性膦酸酯硫脲的抗TMV活性及作用机制研究

On Antiviral Activity and Functional Mechanism of Chiral Thioureas Containing Phosphonate Moiety

采用半叶枯斑法,测定了手性膦酸酯硫脲化合物的抗烟草花叶病毒(TMV)活性,化合物Ⅰ3和Ⅰ14在体积质量分数为500mg/L时对TMV的治疗效率分别为53.2%和56.7%,接近或超过对照药剂宁南霉素(治疗效率为54.3%);通过抗黄瓜花叶病毒(CMV)活性筛选还发现,Ⅰ3和Ⅰ14对CMV的治疗效率分别为53.4%和54.6%,接近对照药宁南霉素(56.3%).在化合物Ⅰ3的作用下,研究了烟草叶片中叶绿素质量分数和3种防御酶(PAL,POD和SOD)活性的变化趋势,结果表明经化合物Ⅰ3处理后烟草植株体内能产生与抗病机制相关的信号,从而启动植株体内一系列的抗病因子,促进烟草体内防御酶系产生,增强了植物的系统抗病性而达到抗TMV的效果.同时,通过分子对接考察了化合物Ⅰ3和Ⅰ14作用于病毒大分子TMV可能的活性靶标,说明氢键在抗病毒活性中发挥重要的作用.

A half-leaf method has been used to determine the in vivo curative,protective and inactivation efficacies of title products anti-TMV（or CMV）at the concentration of 0.5mg/mL.The results show that compoundsⅠ3and Ⅰ14possess good anti-TMV and anti-CMV activity,the anti-TMV curative rates are53.2% and 56.7%,respectively;and anti-CMV curative rates are 53.4%and 54.6%,respectively,which are near or exceed that of the commercial control Ningnanmycin.In enzyme activity method,chlorophyll,PAL,POD,SOD contents inⅠ3-treated tobacco show some definite trend within a certain period of time.It has been found that compoundⅠ3could increase the chlorophyll content of tobacco leaves and the activity of three defense enzymes such as PAL,POD and SOD.Furthermore,the targets of anti-TMV activities possibly have been discovered with compoundsⅠ3（orⅠ14）and TMV by molecular docking.