从苦槛蓝木材中分离得到的三种新的苦木苦味素及其抗 Vpr 活性。
Three new quassinoids isolated from the wood of Picrasma javanica and their anti-Vpr activities.
机构信息
Institute of Natural Medicine, University of Toyama, 2630-Sugitani, Toyama, 930-0194, Japan.
Department of Chemistry, University of Yangon, Yangon, 11041, Myanmar.
出版信息
J Nat Med. 2020 Jun;74(3):571-578. doi: 10.1007/s11418-020-01411-y. Epub 2020 Apr 23.
Three new quassinoids, javanicinols A and B (1 and 2) and 4-keto-(16S)-methoxyjavanicin B (3), together with three known quassinoids (4-6) were isolated from the chloroform-soluble fraction of the methanol extract of the Picrasma javanica wood. The structures of 1-3 were determined by spectroscopic analyses, including 1D and 2D NMR, HRESIMS, and CD. The anti-HIV-1 viral protein R (Vpr) assay revealed that 1 and 2 exhibited potent anti-Vpr activities at 1.25 μM. Furthermore, the assay also revealed the potent anti-Vpr activities of (16R)-methoxyjavanicin B (7) and (16S)-methoxyjavanicin B (8), which were previously isolated from the Picrasma javanica wood.
从苦槛蓝木材的甲醇提取物的氯仿可溶部分分离得到三个新的苦木苦味素，即 javanicinols A 和 B（1 和 2）和 4-酮-（16S）-甲氧基苦木苦味素 B（3），以及三个已知的苦木苦味素（4-6）。通过光谱分析，包括 1D 和 2D NMR、HRESIMS 和 CD，确定了 1-3 的结构。抗 HIV-1 病毒蛋白 R（Vpr）测定显示，1 和 2 在 1.25 μM 时表现出很强的抗 Vpr 活性。此外，该测定还显示了先前从苦槛蓝木材中分离得到的（16R）-甲氧基苦木苦味素 B（7）和（16S）-甲氧基苦木苦味素 B（8）具有很强的抗 Vpr 活性。
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