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A new isoflavone, milletenol A ( 1 ), along with four known flavonoids ( 2 - 5 ) were isolated from the seeds of Millettia pachycarpa . The structure of 1 was established by extensive spectroscopic methods while known compounds were identified by comparisons with literature data. Compound 1 and 2 showed significant anti-inflammatory activities against nitric oxide production in LPS-induced RAW264.7 macrophages. The state of CuSO 4 -stimulated inflammation was effectively alleviated by compound 1 in zebrafish. However, no significant cytotoxicity against human breast cancer cells was observed among all isolates.

Millettia pachycarpa Benth, a widely used anthelminthic drug in folk, is rich in flavonoids with various bioactivities. This study aimed to identify active flavonoids with anti-Alzheimer's disease (AD) effect from its seeds by a bioassay-guided isolation. A novel rotenoid with unusual oxidative ring-opening skeleton (10) and nine known flavonoids (1-9) were obtained, and their structures were elucidated by NMR and HR-ESIMS analysis. Among all isolates, 7 and 8 showed selective butyrylcholinesterase (BChE) inhibitory activities (IC 50  = 2.34 and 11.49 μM, respectively), while 3 was classified as a dual-action inhibitor against acetylcholinesterase (AChE) and BChE (IC 50 AChE  = 17.14 μM, IC 50 BChE  = 5.68 μM). Further kinetic study revealed that 3, 7, and 8 were mixed-type BChE inhibitors, but 3 was a competitive AChE inhibitor. Their strong binding affinities to BChE were confirmed by fluorescence quenching analysis. Additionally, 3 and 8 exhibited potent inhibitory effects against β-amyloid peptide aggregation. These results revealed M. pachycarpa could be a valuable source for anti-AD leads development, and compounds 3, 7 and 8 were worthy of further study as multifunctional or specific agents for AD treatment., (Copyright © 2019 Elsevier Ltd. All rights reserved.)