Institute of Pharmaceutical Biology and Biotechnology, Heinrich-Heine-Universität Düsseldorf, 40225 Düsseldorf, Germany; Department of Pharmacognosy, Faculty of Pharmacy, Minia University, 61519 Minia, Egypt.
Institute of Pharmaceutical Biology and Biotechnology, Heinrich-Heine-Universität Düsseldorf, 40225 Düsseldorf, Germany; Department of Pharmacy, Faculty of Health Sciences, Universitas Jenderal Soedirman, Jalan dr. Soeparno, Karangwangkal 53123 Purwokerto, Indonesia.
Bioorg Med Chem. 2019 Sep 1;27(17):3954-3959. doi: 10.1016/j.bmc.2019.07.025. Epub 2019 Jul 12.
Three new cyclic heptapeptides (1-3) together with three known compounds (4-6) were isolated from a solid rice culture of the soil-derived fungus Clonostachys rosea. Fermentation of the fungus on white beans instead of rice afforded a new γ-lactam (7) and a known γ-lactone (8) that were not detected in the former extracts. The structures of the new compounds were elucidated on the basis of 1D and 2D NMR spectra as well as by HRESIMS data. Compounds 1 and 4 exhibited significant cytotoxicity against the L5178Y mouse lymphoma cell line with IC values of 4.1 and 0.1 µM, respectively. Compound 4 also displayed cytotoxicity against the A2780 human ovarian cancer cell line with an IC value of 3.5 µM. The preliminary structure-activity relationships are discussed.
从土壤来源的真菌玫瑰色拟青霉的固体大米培养物中分离得到三个新的环状七肽（1-3）和三个已知化合物（4-6）。真菌在白豆上而不是在大米上发酵得到了一个新的γ-内酰胺（7）和一个已知的γ-内酯（8），这两种化合物在前提取物中均未检测到。新化合物的结构是基于 1D 和 2D NMR 谱以及 HRESIMS 数据阐明的。化合物 1 和 4 对 L5178Y 小鼠淋巴瘤细胞系表现出显著的细胞毒性，IC 值分别为 4.1 和 0.1 µM。化合物 4 对 A2780 人卵巢癌细胞系也表现出细胞毒性，IC 值为 3.5 µM。讨论了初步的结构-活性关系。
