ReferenceID 2869
Sinomenine increases the methylation level at specific GCG site in mPGES-1 promoter to facilitate its specific inhibitory effect on mPGES-1
Biochim Biophys Acta Gene Regul Mech
Prostaglandin E 2 (PGE 2 ) in cancer and inflammatory diseases is a key mediator of disease progression. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used to inhibit the expression of PGE 2 by depressing cyc
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Record Fields
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- Reference Id
- 2869
- Evidence Id
- 19459
- Core Evidence Id
- 19459
- Source Reference Id
- 5723
- Herb2 Reference Id
- HBREF006520
- Subject Paper Key
- HBIN044111_35417776
- Pubmed Id
- 35417776
- Doi
- 10.1016/j.bbagrm.2022.194813
- Paper Title
- Sinomenine increases the methylation level at specific GCG site in mPGES-1 promoter to facilitate its specific inhibitory effect on mPGES-1
- Paper Abstract
- Prostaglandin E 2 (PGE 2 ) in cancer and inflammatory diseases is a key mediator of disease progression. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used to inhibit the expression of PGE 2 by depressing cyclooxygenase (COX) in inflammatory treatments. However, the inhibition to COXs may cause serious side effects. Thus, it is urgent to develop new anti-inflammatory drugs aiming new targets to inhibit PGE 2 production. Microsomal prostaglandin E synthase 1 (mPGES-1) catalyzes the final step of PGE 2 biosynthesis. Therefore, the selective inhibition of mPGES-1 has become a promising strategy in the treatments of cancer and inflammatory diseases. Our previous studies confirmed that sinomenine (SIN) is a specific mPGES-1 inhibitor. However, the exact mechanism by which SIN inhibits mPGES-1 remains unknown. This study aimed to explain the regulation effect of SIN to mPGES-1 gene expression by its DNA methylation induction effect. We found that the demethylating agent 5-azacytidine (5-AzaC) reversed the inhibitory effect of SIN to mPGES-1. Besides, SIN selectively increased the methylation level of the promoter region in the mPGES-1 gene while the pretreatment of 5-AzaC suppressed this effect. The results also shows that pretreatment with SIN increased the methylation level of specific GCG sites in the promoter region of mPGES-1. This specific methylation site may become a new biomarker for predicting and diagnosing RA and cancer with high expression of mPGES-1. Also, our research provides new ideas and solutions for clinical diagnosis and treatment of diseases related to mPGES-1 and for targeted methylation strategy in drug development.
- Journal
- Biochim Biophys Acta Gene Regul Mech
- Publish Year
- 2022
- Experiment Subject
- Experiment Type
- Cell Experiment
- Phenotype Related
- Cancer; Inflammatory Diseases
- Paper Title Cn
- Paper Title En
- Sinomenine increases the methylation level at specific GCG site in mPGES-1 promoter to facilitate its specific inhibitory effect on mPGES-1
- Bilingual Status
- semi_complete