ReferenceID 5127

Dioscin ameliorates murine ulcerative colitis by regulating macrophage polarization

Pharmacol Res

Restoring immune balance by targeting macrophage polarization is a potentially valuable therapeutic strategy for ulcerative colitis (UC). Dioscin is a steroidal saponin with potent anti-inflammatory, immunoregulatory, an

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Reference Id
5127
Evidence Id
21717
Core Evidence Id
21717
Source Reference Id
3537
Herb2 Reference Id
HBREF004334
Subject Paper Key
HBIN024134_34343656
Pubmed Id
34343656
Doi
10.1016/j.phrs.2021.105796
Paper Title
Dioscin ameliorates murine ulcerative colitis by regulating macrophage polarization
Paper Abstract
Restoring immune balance by targeting macrophage polarization is a potentially valuable therapeutic strategy for ulcerative colitis (UC). Dioscin is a steroidal saponin with potent anti-inflammatory, immunoregulatory, and hypolipidemic effects. This study examined the protective effect of Dioscin on UC in mice and explored the underlying mechanisms. Mice were induced colitis by dextran sulfate sodium (DSS) and concurrently treated with Dioscin oral administration. RAW264.7 cells were skewed to M1 macrophage polarization by lipopolysaccharide (LPS) and interferon-gamma (INF-gamma) in vitro, and received Dioscin treatment. The results showed that Dioscin ameliorated colitis in mice, reduced macrophage M1 polarization, but markedly promoted M2 polarization in mice colon. Dioscin inhibited mammalian target rapamycin complex 1 (mTORC1)/hypoxia-inducible factor-1alpha (HIF-1alpha) signaling and restrained glycolysis in RAW264.7; however, it activated mammalian target rapamycin complex 2 (mTORC2)/peroxisome proliferator-activated receptor-gamma (PPAR-gamma) signal and facilitated fatty acid oxidation (FAO). The modulation of mTORs signaling may inhibit M1, but promote M2 polarization. Furthermore, the effect of Dioscin on M2 polarization was neutralized by the FAO inhibitor Etomoxir and the mTORC2 inhibitor JR-AB2-011. In parallel, the inhibitory effect of Dioscin on M1 polarization was mitigated by the mTORC1 agonist L-leucine. Both JR-AB2-011 and L-leucine blocked the therapeutic effect of Dioscin in mice with UC. Therefore, Dioscin ameliorated UC in mice, possibly by restraining M1, while skewing M2 polarization of macrophages. Regulation of mTORC1/HIF-1alpha and mTORC2/PPAR-gamma signals is a possible mechanism by which Dioscin inhibited aerobic glycolysis and promoted FAO of macrophages. In summary, Dioscin protected mice against DSS-induced UC by regulating mTOR signaling, thereby adjusting macrophage metabolism and polarization.
Journal
Pharmacol Res
Publish Year
2021
Experiment Subject
mouse; raw264.7 cells
Experiment Type
Animal Experiment
Phenotype Related
Ulcerative Colitis; Colitis
Paper Title Cn
Paper Title En
Dioscin ameliorates murine ulcerative colitis by regulating macrophage polarization
Bilingual Status
semi_complete