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Bioorganic and Medicinal Chemistry Letters 2016-09

Flavonoids and biphenylneolignans with anti-inflammatory activity from the stems of Millettia griffithii.

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Huan Tang
He-Ying Pei
Tai-Jin Wang
Kai Chen
Bo Wu
Qiu-Nan Yang
Qiang Zhang
Jian-Hong Yang
Xiao-Yan Wang
Ming-Hai Tang

Ključne riječi

Sažetak

Five new flavonoids, griffinones A-E (1-5), a new biphenylneolignan, griffilignan A (6) and ten known compounds were isolated from the n-hexane and EtOAc extracts of Millettia griffithii. The structures of the new compounds were determined by 1D and 2D NMR, and by HRMS. The anti-inflammatory activity of the isolated compounds was evaluated on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells. Among the isolated compounds, compounds 1, 2 and 14 showed significant anti-inflammatory activity with IC50 values of 20.4, 2.1 and 35.7μM, respectively and no obvious toxicities were observed at 100μM. Western blot and PCR assay further showed that inhibition of nitric oxide production by compound 2 was associated with suppression of iNOS expression. Modeling studies suggested that the amino group, phenyl ring as well as the isopentenyl tails of compound 2 could help bind to iNOs.

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