Quang Tran Hong, Ngan Nguyen Thi Thanh, Yoon Chi-Su, Cho Kwang-Ho, Kang Dae Gill, Lee Ho Sub, Kim Youn-Chul, Oh Hyuncheol
College of Pharmacy, Wonkwang University, Iksan 570-749, Korea.
Institute of Marine Biochemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Caugiay, Hanoi 10000, Vietnam.
Molecules. 2015 Jun 17;20(6):11173-83. doi: 10.3390/molecules200611173.
A chemical investigation of the methanol extract from the roots of Cudrania tricuspidata resulted in the isolation of 16 compounds, including prenylated xanthones 1-9 and flavonoids 10-16. Their structures were identified by NMR spectroscopy and mass spectrometry and comparisons with published data. Compounds 1-9 and 13-16 significantly inhibited PTP1B activity in a dose dependent manner, with IC50 values ranging from 1.9-13.6 μM. Prenylated xanthones showed stronger PTP1B inhibitory effects than the flavonoids, suggesting that they may be promising targets for the future discovery of novel PTP1B inhibitors. Furthermore, kinetic analyses indicated that compounds 1 and 13 inhibited PTP1B in a noncompetitive manner; therefore, they may be potential lead compounds in the development of anti-obesity and -diabetic agents.
对柘树根甲醇提取物进行化学研究，从中分离出16种化合物，包括异戊烯基取代的呫吨酮1 - 9和黄酮类化合物10 - 16。通过核磁共振光谱、质谱分析并与已发表数据进行比较确定了它们的结构。化合物1 - 9和13 - 16以剂量依赖性方式显著抑制蛋白酪氨酸磷酸酶1B（PTP1B）的活性，半数抑制浓度（IC50）值范围为1.9 - 13.6μM。异戊烯基取代的呫吨酮比黄酮类化合物表现出更强的PTP1B抑制作用，表明它们可能是未来发现新型PTP1B抑制剂的有前景的靶点。此外，动力学分析表明化合物1和13以非竞争性方式抑制PTP1B；因此，它们可能是开发抗肥胖和抗糖尿病药物的潜在先导化合物。
