Design, synthesis, and in vitro anti-inflammatory activity of novel matrine derivatives
10.12206/j.issn.2097-2024.202503005
- VernacularTitle:新型苦参碱衍生物的设计合成与体外抗炎活性研究
- Author:
Yifei LU
1
;
Jia SONG
2
;
Hongxia SHEN
1
;
Qingjie ZHAO
3
Author Information
1. School of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350100 China.
2. School of Pharmacy, Naval Medical University, Shanghai 200433 China.
3. School of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350100 China;School of Pharmacy, Naval Medical University, Shanghai 200433 China.
- Publication Type:Originalarticles
- Keywords:
matrine;
derivatives;
synthesis;
structure-activity relationship;
in vitro anti-inflammatory activity
- From:
Journal of Pharmaceutical Practice and Service
2026;44(7):346-352
- CountryChina
- Language:Chinese
-
Abstract:
Objective The alkaloids contained in the Chinese herb Sophora flavescens have good anti-inflammatory activity. To investigate the structure-activity relationship between the novel matrine and the anti-inflammatory activity by modifying the structure of matrine. Methods Fourteen novel matrine derivatives were obtained by chemical modification using matrine as the lead compound with matrine and M19 as positive controls. The cytotoxicity of matrine derivatives against RAW264.7 cells was detected by the cell counting kit 8 （CCK8） assay, and the relative amount of NO produced by matrine derivatives against lipopolysaccharide （LPS）-induced inflammation model of RAW264.7 cells was detected using an NO assay kit. The enzyme-linked immunosorbent assay （Elisa） was used to detect the secretion of interleukin-6 （IL-6） and tumor necrosis factor alpha （TNF-α） by matrine derivatives in LPS-induced inflammation model of RAW264.7 cells. Results The novel matrine derivatives all exhibited lower cytotoxicity compared with M19. The NO inhibition rates of the novel matrine derivatives were all higher than that of matrine, and some were higher than that of M19, with compound A12 having the highest NO inhibition rate. Compounds A11 and A12 showed higher IL-6 inhibition than the control M19. Additionally, compound A12 had higher TNF-α inhibition than M19. Conclusion Compound A12 inhibited the strongest inhibition of NO, IL-6 and TNF-α release and had the best anti-inflammatory activity, which provided an important lead compound for this subsequent in-depth study.
