Design, synthesis, and antifungal mechanism of carbaline fluorescent probes
10.16438/j.0513-4870.2023-1009
- VernacularTitle:咔啉类荧光探针的设计、合成和抗真菌作用机制研究
- Author:
Xiao-qing WANG
1
;
Ji YANG
2
;
Qiao SHI
2
;
Dong-jian XU
2
;
Na LIU
2
;
Chun-quan SHENG
3
Author Information
1. Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, China
2. School of Pharmacy, Second Military Medical University (Naval Medical University), Shanghai 200433, China
3. Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, China; School of Pharmacy, Second Military Medical University (Naval Medical University), Shanghai 200433, China
- Publication Type:Research Article
- Keywords:
carboline compound;
italic>Cryptococcus neoformans;
fluorescence probe;
subcellular localization;
reactive oxygen species
- From:
Acta Pharmaceutica Sinica
2024;59(3):643-650
- CountryChina
- Language:Chinese
-
Abstract:
Three carboline fluorescent probes F1-F3 were designed and synthesized, based on lead compound JYJ-19, an antifungal compound discovered previously by our group. The antifungal activity in vitro results showed that compound F1 had moderate antifungal activity (MIC80 = 32 μg·mL-1). The stokes shift of F1 is 70 nm. The fluorescent probe F1 has good optical properties and can be used for fluorescence imaging research. Subcellular localization experiments results showed that F1 was enriched in the mitochondria of fungal cells. The detection of intracellular reactive oxygen species levels shows that JYJ-19 enhances intracellular reactive oxygen species levels. The above results indicated that carboline compounds could exert antifungal effects by acting on fungal mitochondria.
