来自韩国海绵Placospongia sp.的核因子κB受体激活剂配体诱导破骨细胞分化抑制剂普拉可替林A
Placotylene A, an inhibitor of the receptor activator of nuclear factor-κB ligand-induced osteoclast differentiation, from a Korean sponge Placospongia sp.
作者信息
Kim Hiyoung, Kim Kwang-Jin, Yeon Jeong-Tae, Kim Seong Hwan, Won Dong Hwan, Choi Hyukjae, Nam Sang-Jip, Son Young-Jin, Kang Heonjoong
机构信息
Center for Marine Natural Products and Drug Discovery, School of Earth and Environmental Sciences, Seoul National University, NS-80, Seoul 151-747, Korea.
Department of Pharmacy, Sunchon National University, 315 Maegok-dong, Suncheon, Jeollanam-do 540-742, Korea.
出版信息
Mar Drugs. 2014 Apr 3;12(4):2054-65. doi: 10.3390/md12042054.
A new inhibitor, placotylene A (1), of the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclast differentiation, and a regioisomer of placotylene A, placotylene B (2), were isolated from a Korean marine sponge Placospongia sp. The chemical structures of placotylenes A and B were elucidated on the basis of 1D and 2D NMR, along with MS spectral analysis and revealed as an iodinated polyacetylene class of natural products. Placotylene A (1) displayed inhibitory activity against RANKL-induced osteoclast differentiation at 10 μM while placotylene B (2) did not show any significant activity up to 100 μM, respectively.
从韩国海洋海绵Placospongia sp.中分离出一种新型核因子κB受体活化因子配体（RANKL）诱导破骨细胞分化的抑制剂——普拉可替林A（1），以及普拉可替林A的区域异构体普拉可替林B（2）。基于一维和二维核磁共振以及质谱光谱分析阐明了普拉可替林A和B的化学结构，结果显示它们属于碘化聚乙炔类天然产物。普拉可替林A（1）在10 μM时对RANKL诱导的破骨细胞分化表现出抑制活性，而普拉可替林B（2）在高达100 μM时未显示任何显著活性。
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