Abstract
Eight furoquinoline alkaloids were purified from two plants belonging to the Rutaceae family. Kokusaginine, skimmianine, evolitrine, and confusameline were purified fromMelicope confusa, and haplopine, robustine, dictamine, and γ-fagarine fromDictamnus albus. In this study, the eight furoquinoline alkaloids were examined for, inhibitory potency against human phosphodiesterase 5 (hPDE5A)in vitro. DNA encoding the catalytic domain of human PDE5A was amplified from the mRNA of T24 cells by RT-PCR and was fused to GST in an expression vector. GST-tagged PDE5A was then purified by glutathione affinity chromatography and used in inhibition assays. Of the eight alkaloids, γ-fagarine was the most potent inhibitor of PDE5A, and its single methoxy group at the C-8 position was shown to be critical for inhibitory activity. These results clearly illustrate the relationship between PDE5A inhibition and the methoxy group position in furoquinoline alkaloids.
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Nam, Kw., Je, KH., Shin, YJ. et al. Inhibitory effects of furoquinoline alkaloids fromMelicope confusa andDictamnus albus against human phosphodiesterase 5 (hPDE5A)in vitro . Arch Pharm Res 28, 675–679 (2005). https://doi.org/10.1007/BF02969357
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DOI: https://doi.org/10.1007/BF02969357