Molecular Design,Synthesis And Bioactivity Of AVG Functional Analogue Based On ACS

Postharvest horticultural crops will be affected by itself and environment of ethylene, leading fruits decay, softening, shorten the shelf life, so that the value of goods greatly reduced.Aminoethoxyvinylglycine (AVG) is an ethylene synthesis inhibitor found in recent years that blocks SAM attacking PLP cofactors and inhibiting the synthesis of ethylene. However, AVG fermentation yield is low, the high cost of synthesis greatly limits the popularization and application of AVG. In this study, we designed and synthesized 17 AVG analogs based on the tomato ACS enzyme "1IAY, and the apple ACS enzyme "1YNU", and preliminarily determined their fresh-keeping activity on cherry tomato and apple. It is expected to develop a new class of ethylene synthesis inhibitors . The main results are as follows:1. The scoring function was used to predict the activity, and 17 AVG functional analogues were screened and synthesized. Confirmed by nuclear magnetic, high resolution mass spectrometry structure. The effects of target compounds on the fresh-keeping activity of cherry tomatoes and apples were also preliminary screened.The results showed that compounds 2c, 2e, 2i,2h and 2n had better activity on the preservation of cherry tomatoes, The effect of 2n was the best,and the fruit firmness remained at 8.05 kg.cm-2, the ethylene production was only 9.13 nL·mL-1·h-1 on the sixth day after storage. Compounds 2c, 2i and 2j had a higher activity on the preservation of apple fruits. The predicted results are basically consistent with the activity data.2. Taking the green tomato cherry as the experimental material. the changes of the fruit quality during storage after different AVG concentrations were determined. The results showed that ImM AVG had the best effect during storage. The effects of 2c, 2i and 2n on the fruit quality of cherry tomato were studied with ImM concentration. The results showed that the compound 2n had the highest activity. Compared with the blank control compound 2n delayed cherry tomato fruit ethylene synthesis of the peak time of 2-3 days, delayed fruit softening 3-4 days; reduced fruit quality loss, delayed the color Period 3-4 days, inhibited the fruit lycopene content, delayed the total chlorophyll degradation of the fruit.3. The changes of fruit quality during the storage of AVG, 1-methylcyclopropene, bagging and airtight fumigation were studied with 7 ? 8 mature apple fruits. The results showed that 1-methylcyclopropene had the best effect. AVG treatment at 500 ?M dose the best effect. The effects of 2c and 2j on the quality of apple fruits during storage were studied. The results showed that the activity of compound 2j was better than other compounds. After 30 days of storage compared with the control, it can improve the fruit firmness 2.24 kg · cm-2, soluble solid content and fruit weight increased 2.46% and 2.56% respectively.4. Through the molecular docking method, the recognition pattern of compound 2n and ACS was found. The COMFA and COMSIA models were constructed by constructing the structure-activity relationship study. The relationship through the activity verification of some compounds, the predicted results are basically consistent with the test results.