从红树林内生真菌 16-5c 中分离得到的新型二酮哌嗪生物碱的结构鉴定及抗糖尿病活性
Isolation, Structural Characterization and Antidiabetic Activity of New Diketopiperazine Alkaloids from Mangrove Endophytic Fungus sp. 16-5c.
机构信息
Guangzhou Key Laboratory of Analytical Chemistry for Biomedicine, School of Chemistry, South China Normal University, Guangzhou 510006, China.
出版信息
Mar Drugs. 2021 Jul 20;19(7):402. doi: 10.3390/md19070402.
Six new DIKETOPIPERAZINE alkaloids aspergiamides A-F (-), together with ten known alkaloids (-), were isolated from the mangrove endophytic fungus sp. 16-5c. The structures of the new compounds were elucidated based on 1D/2D NMR spectroscopic and HR-ESIMS data analyses. The absolute configurations of aspergiamides A-F were established based on the experimental and calculated ECD data. All the compounds were evaluated for the antidiabetic activity against α-glucosidase and PTP1B enzyme. The bioassay results disclosed compounds and exhibited significant α-glucosidase inhibitory with IC values of 18.2 and 7.6 μM, respectively; compounds , , and exhibited moderate α-glucosidase inhibition with IC values ranging from 40.7 to 83.9 μM; while no compounds showed obvious PTP1B enzyme inhibition activity.
从红树林内生真菌 sp. 16-5c 中分离得到 6 个新的二酮哌嗪生物碱 Aspergiamides A-F(-)，以及 10 个已知生物碱(-)。根据 1D/2D NMR 光谱和 HR-ESIMS 数据分析，确定了新化合物的结构。基于实验和计算 ECD 数据，确定了 Aspergiamides A-F 的绝对构型。所有化合物均进行了抗α-葡萄糖苷酶和 PTP1B 酶的抗糖尿病活性评价。生物测定结果显示，化合物 和 对α-葡萄糖苷酶表现出显著的抑制活性，IC 值分别为 18.2 和 7.6 μM；化合物 、 、 和 对α-葡萄糖苷酶表现出中等抑制活性，IC 值范围为 40.7 至 83.9 μM；而没有化合物表现出明显的 PTP1B 酶抑制活性。
Zotero 插件