Abstract:
Two new compounds, kinanthraquinone C (1) and kinanthraquinone D (2), were isolated along with two known compounds, kinanthraquinone (3) and kinanthraquinone B (4), produced by the heterologous expression of the kiq biosynthetic gene cluster and its pathway-specific regulator, kiqA, in Streptomyces lividans TK23. The chemical structures of compounds 1 and 2 were determined using mass spectrometry and nuclear magnetic resonance analyses. To examine a biosynthetic pathway of compounds 1 and 2, incubation experiments were conducted using S. lividans TK23 to supply the compounds 3 and 4. These experiments indicated that compounds 3 and 4 were converted to compounds 2 and 1, respectively, by the endogenous enzymes of S. lividans TK23. Compounds 2, 3, and 4 had antimalarial activities at half-maximal inhibitory concentration values of 0.91, 1.2, and 15 μM, respectively, without cytotoxicity up to 30 μM.
摘要:
两个新化合物,金蒽醌C(1)和金蒽醌D(2),与两种已知化合物一起分离,金蒽醌(3)和金蒽醌B(4),由kiq生物合成基因簇及其途径特异性调节因子的异源表达产生,kiqA,在淡化链霉菌TK23中。使用质谱和核磁共振分析确定化合物1和2的化学结构。为了检查化合物1和2的生物合成途径,使用猪链球菌TK23进行孵育实验以提供化合物3和4。这些实验表明,化合物3和4分别转化为化合物2和1,通过S.lividansTK23的内源性酶。化合物2、3和4在半最大抑制浓度值为0.91、1.2和15μM时具有抗疟活性。分别,无细胞毒性高达30μM。