title: Curcuminoid analogs inhibit nitric oxide production from LPS-activated microglial cells.
abstract: The chemically modified analogs, the demethylated analogs 4-6, the tetrahydro analogs 7-9 and the hexahydro analogs 10-12, of curcumin (1), demethoxycurcumin (2) and bisdemethoxycurcumin (3) were evaluated for their inhibitory activity on lipopolysaccharide activated nitric oxide (NO) production in HAPI microglial cells. Di-O-demethylcurcumin (5) and O-demethyldemethoxycurcumin (6) are the two most potent compounds that inhibited NO production. The analogs 5 and 6 were twofold and almost twofold more active than the parent curcuminoids 1 and 2, respectively. Moreover, the mRNA expression level of inducible NO synthase was inhibited by these two compounds. The strong neuroprotective activity of analogs 5 and 6 provide potential alternative compounds to be developed as therapeutics for neurological disorders associated with activated microglia.
authors: Department of Physiology, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand. sukbunteung@hotmail.com
authors: Jiraporn
authors: J
authors: Tocharus
authors: Sataporn
authors: S
authors: Jamsuwan
authors: Chainarong
authors: C
authors: Tocharus
authors: Chatchawan
authors: C
authors: Changtam
authors: Apichart
authors: A
authors: Suksamrarn
mesh_terms: D000818:Animals; D002460:Cell Line; D003474:Curcumin / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D036381:Diarylheptanoids; D008070:Lipopolysaccharides / Q000494:pharmacology*; D017628:Microglia / Q000187:drug effects* / Q000378:metabolism*; D009569:Nitric Oxide / Q000096:biosynthesis*; D052247:Nitric Oxide Synthase Type II / Q000378:metabolism; D051381:Rats
chemical_list: D036381:Diarylheptanoids; D008070:Lipopolysaccharides; D009569:Nitric Oxide; D052247:Nitric Oxide Synthase Type II; D003474:Curcumin; C050229:demethoxycurcumin