Genkwalathins A and B,new lathyrane-type diterpenes from Daphne genkwa |
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| Authors: | Nguyen Van Minh Baek-Soo Han Ha-Young Choi JeongSu Byun Ji-Su Park |
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| Institution: | 1. Superbacteria Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon, Republic of Korea;2. College of Pharmacy, Chungnam National University, Daejeon, Republic of Korea;3. Metabolic Regulation Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon, Republic of Korea;4. Department of Bio-Molecular Science, KRIBB School of Bioscience, Korea University of Science and Technology (UST), Daejeon, Republic of Korea |
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| Abstract: | Screening for new natural anti-neuroinflammatory compounds was performed with the traditional folk medicine Genkwa Flos, which potently inhibited nitric oxide (NO) production by LPS-activated microglial BV-2 cells. Two new lathyrane-type diterpenes, genkwalathins A (1) and B (2), and 14 known daphnane-type diterpenes (3–16) were isolated. The lathyrane-type diterpenes were isolated for the first time from the Thymelaeaceae family in this study. Compounds 1 and 2 moderately inhibited LPS-induced NO production in BV-2 cells without affecting cell viability, while six daphnane-type diterpenes (3, 4, 6, 7, 9 and 10) potently reduced NO production with IC50 values less than 1 μM, although they did display weak cytotoxicity. A structure–activity relationship study on the daphnane-type diterpenes indicated that the stereochemistry at C-19, the benzoate group at C-20, and the epoxide moiety could be important for their anti-neuroinflammatory effects. |
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| Keywords: | Daphne genkwa Genkwa Flos lathyrane-type diterpene daphnane-type diterpene anti-neuroinflammatory |
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