Activity evaluation and mechanism study of antibacterial-anti-inflammatory bifunctional Dioscoreae Nipponicae Rhizoma natural components targeting regulatory protein posttranslational modification
10.16438/j.0513-4870.2024-0428
- VernacularTitle:抗菌-抗炎双功能穿龙薯蓣天然产物靶向调节蛋白质翻译后修饰的活性评价及机制研究
- Author:
Ru-xu SHEN
1
;
Zi-chen YE
2
;
Jia-qi ZHAO
1
;
Qian ZHANG
3
;
Hai-feng TANG
3
;
Di QU
4
Author Information
1. School of Life Sciences, Liaoning University, Shenyang
2. Department of Health Service, Medical Service Training Base, Air Force Medical University, Xi'an
3. Department of Chinese Materia Medica and Natural Medicines, School of Pharmacy, Air Force Medical University, Xi'an
4. Department of Clinical Pharmacy, General Hospital of Western Theater Command, Chengdu; Pancreatic Injury and Repair Key Laboratory of Sichuan Province, General Hospital of Western Theater Command, Chengdu
- Publication Type:Research Article
- Keywords:
natural product;
italic>Dioscorea nipponica Rhizoma;
antibacterial and anti-inflammatory;
sepsis;
target prediction;
protein post-translational modification
- From:
Acta Pharmaceutica Sinica
2024;59(11):2981-2989
- CountryChina
- Language:Chinese
-
Abstract:
The phenomenon of bacterial drug resistance is becoming more and more serious. Natural products, as an important resource for drug discovery, can play a role by regulating protein post-translational modifications related to bacterial infection and inflammatory responses. This provides a valuable compound library for the research and development of new antibacterial drugs. In this present research, dioscin and diosgenin were isolated and identified from Dioscorea nipponica Rhizoma, which both exhibited antibacterial activities, with stronger inhibitory on Gram-positive bacteria (G+) than Gram-negative bacteria (G-). Compared these two compounds, diosgenin showed stronger antibacterial activity than dioscin. In vivo experiments confirmed that diosgenin provided better protection against MRSA-induced sepsis in mice compared to dioscin, which could significantly improve survival rates, reduce bacterial colony counts in infected organs, alleviate pathological damage, and decrease inflammatory cytokine levels in mice. The in vivo study was approved by the Animal Ethics Committee of the PLA Air Force Military Medical University (Grant No. 20230188). Network pharmacology results also revealed that diosgenin could target inflammatory pathways, exerting dual antibacterial and anti-inflammatory activities during bacterial infection therapy.
