来自面包树叶子的新香叶木黄酮。
New geranyl flavonoids from the leaves of Artocarpus communis.
机构信息
Graduate School of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-honmachi, Kumamoto, 862-0973, Japan.
Faculty of Fisheries and Marine Science, Sam Ratulangi University, Kampus Bahu, Manado, 95115, Indonesia.
出版信息
J Nat Med. 2018 Jun;72(3):632-640. doi: 10.1007/s11418-018-1192-z. Epub 2018 Feb 24.
Four new geranyl flavonoids 1-4 and four known flavonoids 5-8 were obtained from the leaves of Artocarpus communis collected in Indonesia. The planar structures of flavonoids were elucidated by analyses of MS and NMR spectroscopic data. Absolute configurations of 1 and 2 were determined by ECD spectroscopy. Analyses by HPLC with a chiral-phase column and ECD spectra confirmed that 3 and 4 were stereoisomeric mixtures and 7 and 8 were racemic mixtures. The compounds obtained in this study inhibited the enzymatic activities of ubiquitin-specific protease 7 (USP7) and the chymotrypsin-like activity of the proteasome. Among the geranyl flavonoids tested in this experiment, the USP7 inhibitory activity of 6 (IC value, 0.094 μM) was 55 times more potent than the commercially available positive control, P5091 (IC value, 5.2 μM).
从印度尼西亚采集的面包树叶片中分离得到了 4 个新的香叶基黄酮类化合物 1-4 和 4 个已知的黄酮类化合物 5-8。通过 MS 和 NMR 光谱数据分析阐明了黄酮类化合物的平面结构。通过 ECD 光谱确定了 1 和 2 的绝对构型。通过 HPLC 与手性柱和 ECD 光谱分析证实，3 和 4 为立体异构体混合物，7 和 8 为外消旋混合物。本研究获得的化合物抑制了泛素特异性蛋白酶 7（USP7）的酶活性和蛋白酶体的糜蛋白酶样活性。在本实验中测试的香叶基黄酮类化合物中，6（IC 值，0.094 μM）对 USP7 的抑制活性比市售阳性对照 P5091（IC 值，5.2 μM）强 55 倍。
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