College of Chemical Engineering, Department of Pharmaceutical Engineering, Northwest University, Xi'an, China.
CAS Key Laboratory of Tropical Marine Bio-resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou, China.
Nat Prod Res. 2022 Mar;36(5):1197-1204. doi: 10.1080/14786419.2020.1864632. Epub 2020 Dec 24.
A new diketopiperazine, cyclo-(-8-acetoxyl-Pro--Leu) (), together with eight known compounds (-) including three enterotoxins (-), four diketopiperazines (-) and maltol (), were isolated from the mangrove derived-soil sp. SCSIO 41400. The planar structures of all compounds were determined from analysis of NMR spectra, MS, optical rotation and comparing with literature data. The absolute configuration of compound was assigned by electronic circular dichroism (ECD). The isolated compounds (-) were tested for their acetyl cholinesterase (AChE) and pancreatic lipase (PL) enzyme inhibitory activities. Among them, the new diketopiperazine () displayed preferable PL enzyme inhibitory activity with IC value of 27.3 μg/mL, while compounds , and showed weak PL enzyme inhibitory activity. Further molecular docking simulation exhibited that compound could be well bind with the catalytic pocket of the PL. Besides, compound showed moderate antibacterial activity against with MIC value of 12.5 μg/mL, which was comparable to that of the positive control ampicillin with MIC value of 3.125 μg/mL.
从红树林来源的土壤中分离得到一株真菌 SCSIO 41400，从中分离得到一个新的二酮哌嗪化合物，环-(-8-乙酰氧基-Pro--Leu)()，以及另外 8 个已知化合物（-），包括 3 种肠毒素（-）、4 种二酮哌嗪（-）和麦芽酚（）。所有化合物的平面结构均通过 NMR 光谱、MS、旋光和与文献数据的比较来确定。通过电子圆二色性（ECD）确定了化合物的绝对构型。对分离得到的化合物（-）进行乙酰胆碱酯酶（AChE）和胰脂肪酶（PL）酶抑制活性测试。其中，新的二酮哌嗪（）对 PL 酶表现出较好的抑制活性，IC 值为 27.3 μ g/mL，而化合物、和则表现出较弱的 PL 酶抑制活性。进一步的分子对接模拟表明，化合物可以很好地与 PL 的催化口袋结合。此外，化合物对显示出中等的抗菌活性，MIC 值为 12.5 μ g/mL，与阳性对照氨苄西林的 MIC 值（3.125 μ g/mL）相当。
