Curcuminoid analogs inhibit nitric oxide production from LPS-activated microglial cells

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...

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Bibliographic Details
Main Authors: Tocharus J., Jamsuwan S., Tocharus C., Changtam C., Suksamrarn A.
Format: Article
Language:English
Published: 2014
Online Access:http://www.scopus.com/inward/record.url?eid=2-s2.0-80053648258&partnerID=40&md5=5144659535c0afc620780200848aafbf
http://www.ncbi.nlm.nih.gov/pubmed/21993909
http://cmuir.cmu.ac.th/handle/6653943832/2984
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Institution: Chiang Mai University
Language: English
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Summary: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. © 2011 The Japanese Society of Pharmacognosy and Springer.