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Hybrid flavan-chalcones, aromatase and lipoxygenase inhibitors, from Desmos cochinchinensis
Authors:Bajgai Santi Prasad  Prachyawarakorn Vilailak  Mahidol Chulabhorn  Ruchirawat Somsak  Kittakoop Prasat
Affiliation:aChulabhorn Graduate Institute, and the Center for Environmental Health, Toxicology and Management of Chemicals (ETM), Chemical Biology Program, Vibhavadi-Rangsit Road, Bangkok 10210, Thailand;bChulabhorn Research Institute, Vibhavadi-Rangsit Road, Bangkok 10210, Thailand;cChulabhorn Research Centre, Institute of Molecular Biosciences, Mahidol University, Thailand
Abstract:Hybrid flavan-chalcones, desmosflavans A (1) and B (2), together with three known compounds, cardamonin (3), pinocembrin (4) and chrysin (5), were isolated from leaves of Desmos cochinchinensis. Cardamonin (3) and chrysin (5) exhibited potent antioxidant activity with 15.0 and 12.2 ORAC units. Desmosflavans A (1) and B (2), pinocembrin (4), and chrysin (5) were found to be inhibitors of aromatase with respective IC50 values of 1.8, 3.3, 0.9, and 0.8 μM. Desmosflavan A (1) inhibited lipoxygenase with the IC50 value of 4.4 μM. Desmosflavan A (1) exhibited cytotoxic activity with IC50 values of 0.29–3.75 μg/mL, while desmosflavan B (2) showed IC50 values of 1.71–27.0 μg/mL.
Keywords:Desmos cochinchinensis   Annonaceae   Flavan   Chalcone   Aromatase inhibitor   Lipoxygenase inhibitor   Antioxidant activity   Cytotoxic activity   Cancer chemoprevention
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