摘要
Our previous study found that 1-(4-bromophenyl)-5-phenyl-1H-1,2,3-triazole (BPT) exhibited very low toxicity and higher biology activity. In the present study, BPT was used to investigate its mechanism against Colletotrichum gloeosporioides in mango by chemical proteomics and chemicobiological methods. The experimental results of some phenotypic traits and cytotoxicity indicated that there are some changes in permeability of the cell membranes and BPT has fungistatic activity with lower cytotoxicity. Next, a biotin probe named BPTN with a higher activity (EC 50 value of 11.08 mg/L) than that of BPT(EC 50 value of 14.13 mg/L) was designed and synthesized by the chemical proteomics approach. The major differentially expressed proteins between BPT or BPTN and Colletotrichum gloeosporioides were identified and analyzed by Matrix-assisted laser desorption time-of-flight mass spectrometry (MALDI-TOF-MS) and bioinformatics. The results indicated that there are 25 differentially expressed proteins in Colletotrichum gloeosporioides under BPT intervention, and 29 target proteins in Colletotrichum gloeosporioides captured by BPTN. For BPTN-anthracnose system, the protein No. 8 belonged to cytochrome P450 proteins (CYP) family can be taken as a target protein of BPTN, which confirmed by bioinformatics analysis. Further, a classic fungal target protein of triazoles, sterol 14α-demethylase (CYP51) was used to verify the interaction in the presence of BPT by various spectroscopic and molecular docking methods. The results showed that BPT exhibited strong interactions with CYP51 and it was predominantly driven by hydrophobic forces and hydrogen bonds. The present study has significant theoretical and practical implications for the development of novel 1,2,3-triazole antifungal agents.
危险品化学品经营许可证(带存储)