Screening of new bioactive metabolites for diabetes therapy.

Abstract

Microorganisms and plants produce bioactive metabolites that are potentially useful in the treatment of disease. We have designed and synthesized DHMEQ as a specific inhibitor of NF-κB based on the structure of epoxyquinomicin. It directly binds to NF-κB components to inhibit DNA-binding and was shown to be endowed with inhibiting activity in various inflammatory and cancer models in experimental animals. It was also effective to improve the success of islet transplantation especially when administered to donor mice. We have also isolated from the leaves of Ervatamia microphylla conophylline, a compound that induces differentiation of beta cells from the precursor cells and was recently found to suppress islet fibrosis in diabetes model rats.

• Authors: Kulrawee Sidthipong, Satoru Todo, Izumi Takei, Itaru Kojima, Kazuo Umezawa
• Journal: Internal and emergency medicine (Intern Emerg Med) Vol. 8 Suppl 1 Pg. S57-9 (Apr 2013) ISSN: 1970-9366 [Electronic] Italy
• PMID: 23504230 (Publication Type: Journal Article, Review)

Chemical References

• Benzamides
• Cyclohexanones
• NF-kappa B
• Vinca Alkaloids
• conophylline
• dehydroxymethylepoxyquinomicin

Topics

• Animals
• Benzamides (pharmacology)
• Cell Differentiation (drug effects)
• Cyclohexanones (pharmacology)
• Diabetes Mellitus, Type 1 (therapy)
• Fibrosis (prevention & control)
• Humans
• Insulin-Secreting Cells (drug effects)
• Islets of Langerhans Transplantation
• NF-kappa B (antagonists & inhibitors)
• Vinca Alkaloids (pharmacology)