State Key Laboratory of Bioactive Substance and Function of Natural Medicines, CAMS Key Laboratory of Enzyme and Biocatalysis of Natural Drugs, NHC Key Laboratory of Biosynthesis of Natural Products, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, CAMS Key Laboratory of Enzyme and Biocatalysis of Natural Drugs, NHC Key Laboratory of Biosynthesis of Natural Products, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.
Fitoterapia. 2020 Oct;146:104682. doi: 10.1016/j.fitote.2020.104682. Epub 2020 Jul 3.
Six new Diels-Alder type adducts, morusalisins A-F (1-6), were isolated from Morus alba cell cultures. The structures of 1-6 were determined by extensive spectroscopic data analysis, including HRESIMS, NMR, and ECD experiments. Furthermore, compounds 1-6 exhibited potent protein tyrosine phosphatase 1B (PTP1B) inhibitory activity with IC values ranging from 1.14 to 2.24 μM, making them promising as bioactive compounds for anti-diabetic drug discovery.
从桑椹细胞培养物中分离得到了 6 种新的 Diels-Alder 型加合物，morusalisins A-F（1-6）。通过包括 HRESIMS、NMR 和 ECD 实验在内的广泛光谱数据分析确定了 1-6 的结构。此外，化合物 1-6 对蛋白酪氨酸磷酸酶 1B（PTP1B）具有很强的抑制活性，IC 值范围为 1.14-2.24 μM，有望成为抗糖尿病药物发现的有价值的生物活性化合物。
