title: 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.affiliation: Aichi Medical University School of Medicine, Nagakute, 480-1195, Japan.
authors.forename: Kulrawee
authors.initials: K
authors.lastname: Sidthipong
authors.forename: Satoru
authors.initials: S
authors.lastname: Todo
authors.forename: Izumi
authors.initials: I
authors.lastname: Takei
authors.forename: Itaru
authors.initials: I
authors.lastname: Kojima
authors.forename: Kazuo
authors.initials: K
authors.lastname: Umezawa
mesh_terms: D000818:Animals; D001549:Benzamides / Q000494:pharmacology*; D002454:Cell Differentiation / Q000187:drug effects; D003512:Cyclohexanones / Q000494:pharmacology*; D003922:Diabetes Mellitus, Type 1 / Q000628:therapy*; D005355:Fibrosis / Q000517:prevention & control; D006801:Humans; D050417:Insulin-Secreting Cells / Q000187:drug effects; D016381:Islets of Langerhans Transplantation; D016328:NF-kappa B / Q000037:antagonists & inhibitors; D014748:Vinca Alkaloids / Q000494:pharmacology*
chemical_list: D001549:Benzamides; D003512:Cyclohexanones; D016328:NF-kappa B; D014748:Vinca Alkaloids; C099167:conophylline; C464444:dehydroxymethylepoxyquinomicin