Complete NMR assignment and absolute configuration of k4610422, a norditerpenoid inhibitor of testosterone-5α-reductase originally from Streptosporangium: rediscovery from a thermophilic Actinomadura.,The Journal of Antibiotics

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Complete NMR assignment and absolute configuration of k4610422, a norditerpenoid inhibitor of testosterone-5α-reductase originally from Streptosporangium: rediscovery from a thermophilic Actinomadura.
The Journal of Antibiotics ( IF 2.1 ) Pub Date : 2019-09-03 , DOI: 10.1038/s41429-019-0231-7
Hirofumi Akiyama ₁ , Naoya Oku ₁ , Enjuro Harunari ₁ , Watanalai Panbangred _{2,

3} , Yasuhiro Igarashi ₁

Affiliation

A norditerpenoid k4610422 (1), an inhibitor of testosterone-5α-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 ¹H and ¹³C 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 μM.

中文翻译：

完整的NMR分配和k4610422的绝对构型，k4610422是最初来自链霉菌属的睾丸激素5α-还原酶的去甲萜类抑制剂：从嗜热猕猴桃属植物中重新发现。

从嗜热放线菌Actinomadura sp。的培养物提取物中分离出最初从链霉菌属（Streptosporangium）属的嗜温稀有放线菌中发现的睾丸激素5α-还原酶抑制剂norditerpenoid k4610422（1）。通过光谱测量（包括NOESY和CD光谱以及ECD计算）解决了¹ H和¹³ C NMR的完整配位和1的绝对构型，从而确定了（5 R，9 S，10 R，13 S）-构型。化合物1具有IC ₅₀ 30μM对P388鼠白血病细胞的中等细胞毒性。

更新日期：2020-01-16

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