Complete NMR assignment and absolute configuration of k4610422, a norditerpenoid inhibitor of testosterone-5α-reductase originally from Streptosporangium: rediscovery from a thermophilic Actinomadura
Complete NMR assignment and absolute configuration of k4610422, a norditerpenoid inhibitor of testosterone-5α-reductase originally from Streptosporangium: rediscovery from a thermophilic Actinomadura
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DOI：
10.1038/s41429-019-0231-7
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发表时间：
2020-01-01
影响因子：
3.3
通讯作者：
Igarashi, Yasuhiro
中科院分区：
文献类型：
--
作者：
Akiyama, Hirofumi;Oku, Naoya;Igarashi, Yasuhiro
去甲二萜 k4610422 (1) 是一种睾酮 5 α 还原酶抑制剂，最初从链孢子囊属的嗜温稀有放线菌中发现，是从嗜热放线菌 Actinomadura sp 的培养物提取物中分离出来的。完整的 H-1 和 C-13 NMR 归属以及 1 的绝对构型通过光谱测量（包括 NOESY 和 CD 光谱以及 ECD 计算）得到解决，从而可以建立 (5 R,9 S,10 R,13 S)-构型。化合物1对P388鼠白血病细胞具有中等细胞毒性，IC50为30μM。
A norditerpenoid k4610422 (1), an inhibitor of testosterone-5 alpha-reductase originally discovered from a mesophilic rare actinomycete of the genus Streptosporangium, was isolated from the culture extract of a thermophilic actinomycete Actinomadura sp. The complete H-1 and C-13 NMR assignment and absolute configuration of 1 were addressed by spectroscopic measurements including NOESY and CD spectra coupled with ECD calculation, which allowed to establish the (5 R,9 S,10 R,13 S)-configuration. Compound 1 was moderately cytotoxic against P388 murine leukemia cells with IC50 30 mu M.