Graduate School of Infection Control Sciences, Kitasato University, Tokyo, Japan.
J Antibiot (Tokyo). 2011 Apr;64(4):303-7. doi: 10.1038/ja.2011.16. Epub 2011 Mar 9.
Three novel antitrypanosomal alkaloids, named spoxazomicins A-C, were isolated by silica gel column chromatography and HPLC from the culture broth of a new endophytic actinomycete species, Streptosporangium oxazolinicum K07-0460(T). The structures of the spoxazomicins were elucidated by NMR and X-ray crystal analyses and shown to be new types of pyochelin family antibiotic. Spoxazomicin A showed potent and selective antitrypanosomal activity with an IC₅₀ value of 0.11 μg ml⁻¹ in vitro without cytotoxicity against MRC-5 cells (IC₅₀=27.8 μg ml⁻¹).
三种新型抗锥虫生物碱,命名为 spoxazomicins A-C,从新型内生放线菌 Streptosporangium oxazolinicum K07-0460(T) 的发酵液中通过硅胶柱色谱和 HPLC 分离得到。通过 NMR 和 X 射线晶体分析阐明了 spoxazomicins 的结构,它们是新型的焦脱镁叶绿酸家族抗生素。Spoxazomicin A 表现出强大而选择性的抗锥虫活性,在体外的 IC₅₀ 值为 0.11μg ml⁻¹,对 MRC-5 细胞没有细胞毒性(IC₅₀=27.8μg ml⁻¹)。