| Autor: |
Ding YY; School of Pharmacy, Lanzhou University, Lanzhou 730000, China., Jin YR; School of Pharmacy, Lanzhou University, Lanzhou 730000, China., Luo XF; School of Pharmacy, Lanzhou University, Lanzhou 730000, China., Zhang SY; Key Laboratory of Vector Biology and Pathogen Control of Zhejiang Province, College of Life Science, Huzhou University, Huzhou 313000, China., Dai TL; School of Pharmacy, Lanzhou University, Lanzhou 730000, China., Ma L; School of Pharmacy, Lanzhou University, Lanzhou 730000, China., Zhang ZJ; School of Pharmacy, Lanzhou University, Lanzhou 730000, China., Wu ZR; Key Laboratory of Vector Biology and Pathogen Control of Zhejiang Province, College of Life Science, Huzhou University, Huzhou 313000, China., Jin CX; School of Pharmacy, Lanzhou University, Lanzhou 730000, China., Liu YQ; School of Pharmacy, Lanzhou University, Lanzhou 730000, China.; Key Laboratory of Vector Biology and Pathogen Control of Zhejiang Province, College of Life Science, Huzhou University, Huzhou 313000, China.; State Key Laboratory of Grassland Agro-ecosystems, Lanzhou University, Lanzhou 730000, China. |
| Abstrakt: |
This research adopted the Fischer indole synthesis method to continue constructing a novel drug-like chemical entity based on the guidance of isocryptolepine and obtained four series of derivatives: Y , Da , Db , and Dc . The antimicrobial activity of these derivatives against plant pathogens was further evaluated. The results showed that Dc-2 had the best antifungal effect against Botrytis cinerea , and its EC 50 value was up to 1.29 μg/mL. In addition, an in vivo activity test showed that the protective effect of Dc-2 on apples was 82.2% at 200 μg/mL, which was better than that of Pyrimethanil (45.4%). Meanwhile, it was found by scanning electron microscopy and transmission electron microscopy that the compound Dc-2 affected the morphology of mycelia. The compound Dc-2 was found to damage the cell membrane by PI and ROS staining. Through experiments such as leakage of cell contents, it was found that the compound Dc-2 changed the permeability of the cell membrane and caused the leakage of substances in the cell. According to the above studies, compound Dc-2 can be used as a candidate lead compound for further structural optimization and development. |
