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

• Main Authors: Tocharus,J., Jamsuwan,S., Tocharus,C., Changtam,C., Suksamrarn,A.
• Format: Article
• Published: Springer Verlag 2015
• Subjects: Drug Discovery; Pharmaceutical Science; Organic Chemistry; Complementary and Alternative Medicine
• Online Access: http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84863506806&origin=inward; http://cmuir.cmu.ac.th/handle/6653943832/38211
• Institution: Chiang Mai University

The chemically modified analogs, the demethy-lated 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. © The Japanese Society of Pharmacognosy and Springer 2011.