Loukaci A, Kayser O, Bindseil K, Siems K, Frevert J, Abreu P M
Departamento de Química, Centro de Química Fina e Biotecnologia, FCT-UNL, 2825-114 Caparica, Portugal, Freie Universität Berlin, Königin-Luise Strasse, 2-4, D-14195 Berlin, Germany.
J Nat Prod. 2000 Jan;63(1):52-6. doi: 10.1021/np990332l.
Bioassay-guided fractionation of an extract of Holarrhena floribunda stem, has led to the isolation of the new trichothecenes, 8-dihydrotrichothecinol A (1), loukacinol A (2), and loukacinol B (3), and the known compounds, trichothecolone (4), trichothecin (5), trichothecinol A (6), rosenonolactone (7), 6beta-hydroxyrosenonolactone (8), and rosololactone (9). The structures were determined by spectral and chemical methods, and absolute configurations were established by a modified Horeau's method using HPLC. Compounds 1 and 6 exhibited significant cytotoxicity against several human tumor cell lines, whereas compound 8 showed moderate and weak antileishmanial activity toward extracellular and intracellular Leishmania donovani, respectively.
对非洲止泻木茎提取物进行生物测定导向的分级分离,已分离出新型单端孢霉烯族毒素8-二氢单端孢霉烯醇A(1)、卢卡霉素A(2)和卢卡霉素B(3),以及已知化合物单端孢菌酮(4)、单端孢霉毒素(5)、单端孢霉烯醇A(6)、玫瑰内酯(7)、6β-羟基玫瑰内酯(8)和玫瑰醇内酯(9)。通过光谱和化学方法确定了其结构,并使用高效液相色谱法通过改良的霍劳法确定了绝对构型。化合物1和6对几种人类肿瘤细胞系表现出显著的细胞毒性,而化合物8分别对细胞外和细胞内杜氏利什曼原虫显示出中等和较弱的抗利什曼活性。