Lin Pingfa, Shi Mianmian, Wang Feifei, Lin Yong, Zheng Yongbiao
School of Pharmacy, Fujian Health College, Fuzhou 350101, China.
College of Life Sciences, Fujian Normal University, Fuzhou 350117, China.
Molecules. 2025 Apr 30;30(9):1993. doi: 10.3390/molecules30091993.
Marine are an important source of naturally occurring active compounds. Out of 23 marine strains, 1 strain of sp. FJ0218 was selected for its high activity in inhibiting α-glucosidase. Two polyketides, phaeochromycins D () and E (), were isolated from the fermentation broth of this strain using bioactivity-guided column chromatography over RP-18, Sephadex LH-20, and silica gel. Their structures were determined using NMR data, HR-EI-MS, and single-crystal X-ray crystallography. Phaeochromycins D () and E () exhibited inhibitory activity against α-glucosidase, with IC values of 10 mM and 25 mM, respectively. Lineweaver-Burk plots revealed that phaeochromycin E () acts as an uncompetitive inhibitor, while phaeochromycin D () acts as a non-competitive inhibitor. These findings suggest that there is potential for the pharmacological regulation of glucose levels through the use of polyketide phaeochromycins, emphasizing their significant impact on glucose management.
海洋生物是天然活性化合物的重要来源。在23株海洋菌株中，筛选出1株sp. FJ0218菌株，因其对α-葡萄糖苷酶具有高抑制活性。使用RP - 18、Sephadex LH - 20和硅胶进行生物活性导向柱色谱法，从该菌株的发酵液中分离出两种聚酮化合物，即嗜铬霉素D（）和E（）。利用核磁共振数据、高分辨电子轰击质谱和单晶X射线晶体学确定了它们的结构。嗜铬霉素D（）和E（）对α-葡萄糖苷酶表现出抑制活性，IC值分别为10 mM和25 mM。Lineweaver - Burk图显示，嗜铬霉素E（）作为非竞争性抑制剂起作用，而嗜铬霉素D（）作为竞争性抑制剂起作用。这些发现表明，通过使用聚酮化合物嗜铬霉素对血糖水平进行药理调节具有潜力，强调了它们对血糖管理的重大影响。
