Center for Marine Natural Products and Drug Discovery, School of Earth and Environmental Sciences, Seoul National University , NS-80, Seoul, 151-747, Korea.
J Nat Prod. 2012 Dec 28;75(12):2049-54. doi: 10.1021/np300544a. Epub 2012 Nov 12.
Six new (1, 2, and 5-8) and three known (3, 4, and 9) butenolide metabolites were isolated from the tunicate Pseudodistoma antinboja by activity-guided fractionations. The structures were elucidated by combined NMR and MS spectroscopic methods. These compounds were evaluated for their antibacterial activity, and most of them exhibited moderate to significant activity that selectively targeted Gram-positive strains and did not exhibit cytotoxicity in the MTT assay at 100 μM. Cadiolides 5-9 in particular exhibited significant antibacterial activity that was comparable to or even better than those of marketed drugs such as vancomycin and linezolid against all of the drug-resistant strains tested.
六种新的(1、2 和 5-8)和三种已知的(3、4 和 9)丁烯内酯代谢物通过活性导向分离从被囊动物 Pseudodistoma antinboja 中分离出来。通过组合 NMR 和 MS 光谱方法阐明了这些化合物的结构。评估了这些化合物的抗菌活性,其中大多数表现出中等至显著的活性,选择性针对革兰氏阳性菌株,并且在 100 μM 时在 MTT 测定中没有细胞毒性。特别是 cadiolides 5-9 表现出显著的抗菌活性,与市售药物如万古霉素和利奈唑胺相当,甚至优于所有测试的耐药菌株。