Inhibition of cellular and animal inflammatory disease models by nf-κb inhibitor dhmeq

Jun Ma, Yuyang Zhang, Takeshi Sugai, Tetsuo Kubota, Hiroshi Keino, Magdy El-Salhy, Michitaka Ozaki, Kazuo Umezawa

Research output: Contribution to journalReview articlepeer-review

3 Citations (Scopus)

Abstract

General inflammatory diseases include skin inflammation, rheumatoid arthritis, inflammatory bowel diseases, sepsis, arteriosclerosis, and asthma. Although these diseases have been extensively studied, most of them are still difficult to treat. Meanwhile, NF-κB is a transcription factor promoting the expression of many inflammatory mediators. NF-κB is likely to be involved in the mechanism of most inflammatory diseases. We discovered a specific NF-κB inhibitor, dehydroxymethylepoxyquinomicin (DHMEQ), about 20 years ago by molecular design from a natural product. It directly binds to and inactivates NF-κB components. It has been widely used to suppress cellular and animal inflammatory disease models and was shown to be potent in vivo anti-inflammatory activity without any toxicity. We have prepared ointment of DHMEQ for the treatment of severe skin inflammation. It inhibited inflammatory cytokine expressions and lowered the clinical score in mouse models of atopic dermatitis. Intraperitoneal (IP) administration of DHMEQ ameliorated various disease models of inflammation, such as rheumatoid arthritis, sepsis, and also graft rejection. It has been suggested that inflammatory cells in the peritoneal cavity would be important for most peripheral inflammation. In the present review, we describe the synthesis, mechanism of action, and cellular and in vivo anti-inflammatory activities and discuss the clinical use of DHMEQ for inflammatory diseases.

Original languageEnglish
Article number2271
JournalCells
Volume10
Issue number9
DOIs
Publication statusPublished - 2021 Sep

Keywords

  • DHMEQ
  • Inflammation
  • Intraperitoneal administration
  • NF-κB
  • Ointment
  • Tacrolimus
  • Transplantation

ASJC Scopus subject areas

  • Medicine(all)

Fingerprint

Dive into the research topics of 'Inhibition of cellular and animal inflammatory disease models by nf-κb inhibitor dhmeq'. Together they form a unique fingerprint.

Cite this