Amakusamine from a Psammocinia sp. Sponge: Isolation, Synthesis, and SAR Study on the Inhibition of RANKL-Induced Formation of Multinuclear Osteoclasts
Amakusamine from a Psammocinia sp. Sponge: Isolation, Synthesis, and SAR Study on the Inhibition of RANKL-Induced Formation of Multinuclear Osteoclasts
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天草胺 (Amakusamine)，来自 Psammocinia sp.。
DOI：
10.1021/acs.jnatprod.1c00758
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发表时间：
2021
影响因子：
5.1
通讯作者：
Tsukamoto Sachiko
中科院分区：
文献类型：
--
作者：
Maeyama Yuka;Nakashima Yuta;Kato Hikaru;Hitora Yuki;Maki Kazuhiko;Inada Natsumi;Murakami Shunya;Inazumi Tomoaki;Ise Yuji;Sugimoto Yukihiko;Ishikawa Hayato;Tsukamoto Sachiko
从雪莲属海绵中分离得到一个简单的亚甲二氧基二溴吲哚生物碱--阿马库斯胺(1)，其结构经波谱数据、含时密度泛函理论计算和合成确证。化合物1抑制核因子受体激活剂κB配体诱导的多核破骨细胞的形成，其IC50值为10.5μM。并用合成的衍生物研究了1的构效关系。
A simple methylenedioxy dibromoindole alkaloid, amakusamine (1), was isolated from a marine sponge of the genusPsammocinia, and its structure was determined from spectroscopic data, time-dependent density-functional theory calculations, and synthesis. Compound1inhibited the receptor activator of nuclear factor-κB ligand (RANKL)-induced formation of multinuclear osteoclasts with an IC50value of 10.5 μM in RAW264 cells. The structure–activity relationship of1was also investigated with synthetic derivatives.