Yamada Takeshi, Iritani Masashi, Ohishi Hirohumi, Tanaka Kayo, Minoura Katsuhiko, Doi Mitsunobu, Numata Atsushi
Osaka University of Pharmaceutical Sciences, 4-20-1, Nasahara, Takatsuki, Osaka 569-1094, Japan.
Org Biomol Chem. 2007 Dec 21;5(24):3979-86. doi: 10.1039/b713060k. Epub 2007 Oct 26.
Pericosines A-E 1-5 have been isolated from a strain of Periconia byssoides originally separated from the sea hare Aplysia kurodai. Among them, pericosines C 3 and E 5 were separated as enantiomeric mixtures. Their stereostructures, except for compound 1, have been elucidated or identified on the basis of spectroscopic analyses, including 1D and 2D NMR techniques, and X-ray analysis. In addition, conformation for all the compounds has been discussed. Compounds 1-3 exhibited significant growth inhibition against tumour cell lines. Pericosine A 1 also showed significant in vivo tumour inhibitory activity. In addition, compound inhibited the protein kinase EGFR and topoisomerase II.
从最初从日本黑兔蛞蝓分离出的一种缢缩围丛梗孢菌株中分离得到了围丛梗孢菌素A-E(1-5)。其中,围丛梗孢菌素C(3)和E(5)是以对映体混合物形式分离得到的。除化合物1外,它们的立体结构已通过包括一维和二维核磁共振技术以及X射线分析在内的光谱分析得以阐明或鉴定。此外,还讨论了所有化合物的构象。化合物1-3对肿瘤细胞系表现出显著的生长抑制作用。围丛梗孢菌素A(1)在体内也显示出显著的肿瘤抑制活性。此外,该化合物还抑制蛋白激酶表皮生长因子受体(EGFR)和拓扑异构酶II。