Evaluation of antimicrobial activity of milk exosomes loaded with rifamycin S derivative
10.3867/j.issn.1000-3002.2025.03.006
- VernacularTitle:牛奶外泌体负载利福霉素S衍生物的抗菌活性评价
- Author:
Zhanqun YANG
1
;
Xiang LI
;
Chenghua LIU
;
Mengzhu ZHENG
;
Shiyong FAN
;
Yuchao DONG
;
Zihao WANG
;
Jian LIN
;
Guang YANG
;
Long CHEN
Author Information
1. 北京大学第三医院药学部,北京 100191
- Publication Type:Journal Article
- Keywords:
rifamycin S derivatives;
Staphylococcus aureus;
Pseudomonas aeruginosa;
exosome;
antimicrobial activity
- From:
Chinese Journal of Pharmacology and Toxicology
2025;39(3):208-215
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To design and synthesize rifamycin S derivatives and load them into milk exosomes to evaluate their in vitro antimicrobial activity.METHODS Rifamycin S derivatives were synthe-sized and characterized by mass spectrometry and NMR.Using the dilution assay method,the inhibitory activity of each rifamycin S derivatives molecule against Staphylococcus aureus and Pseudomonas aerugi-nosa was determined,and the IC50 was calculated.Derivatives molecules with excellent antimicrobial activity were selected and loaded into milk exosomes using the ultrasonication method,resulting in the preparation of milk exosome-loaded rifamycin S derivatives.The antimicrobial activity against Staphylo-coccus aureus was determined using the dilution assay method.The inhibitory effect of the exosome-loaded rifamycin S derivatives on Staphylococcus aureus residing within macrophages was detected using the plate colony counting method.RESULTS Three rifamycin S derivatives were successfully designed and synthesized,which demonstrated superior antimicrobial activity against Staphylococcus aureus(the parent compound's antimicrobial activity is merely from 1/20 to 1/80 of that of the three rifamycin S derivatives)and Pseudomonas aeruginosa(the parent compound's antimicrobial activity is only 1/14 and 1/9 of that of compound 1 and compound 3)compared to the parent compound.The loading of milk exosomes with the rifamycin S derivatives compound 3 was successfully achieved,with a loading efficiency of 10.9％.The antimicrobial activity of the compound after exosome loading was significantly enhanced against Staphylococcus aureus in vitro and against Staphylococcus aureus residing within macrophages(P＜0.01).CONCLUSION The designed and synthesized derivatives of rifamycin S possess stronger anti-microbial activity,and their antibacterial efficacy against both extracellular and intracellular bacteria can be further enhanced after loading into exosomes.
