Structure modification of cis-stilbenoids from the tubers of Scirpus yagara and their anti-inflammatory activities / 中国药学杂志

ABSTRACT

OBJECTIVE: To synthesize cis-stilbenoids derivatives and investigate their anti-inflammatory activities in vitro. METHODS: Sciryagarol I(1) from the tuber of Scirpus yagara, was used as a primary material. The synthetic derivatives were obtained via methyltion, acetylation, and demethylation. MTT assay was used to detect the effects of compound 1, its synthetic derivatives 3-5 and sciryagarol II(2) on RAW264.7 cells viability. And the inhibitory activities of compounds 1-5 against TNF-α and IL-6 production in LPS- and Pam3csk4-activated RAW264.7 cells were evaluated by ELISA assay. RESULTS: The compounds 3-5 were synthesized, and their structures were characterized by 1H-NMR and HRESI-MS spectra. ELISA assay showed that compounds 1, 2 and 5 significantly inhibited the production of TNF-α and IL-6 from LPS- and Pam3csk4-stimulated RAW264.7 cells. CONCLUSION: Three novel compounds 3-5 are synthesized. The number of phenolic hydroxyl in the structure of cis-stilbenoids may be related to their anti-inflammatory activities.