Yang Liyuan, Lin Jun, Zhou Bin, Liu Yangang, Zhu Baoquan
a School of Pharmacy , Shanghai Jiao Tong University , Shanghai , China.
b State Key Laboratory of New Drug and Pharmaceutical Process , Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry , Shanghai , China.
Nat Prod Res. 2017 Feb;31(4):487-491. doi: 10.1080/14786419.2016.1190719. Epub 2016 Jun 13.
This study aimed to isolate active compounds from traditional Chinese medicinal Taxillus sutchuenensis to inhibit hepatitis C virus (HCV) NS3 protease activity. Under the guidance of bioassay, 10 compounds were isolated from the EtOAc extract fraction, which were identified as inhibitors of HCV NS3 protease. IC values of these compounds were obtained, and a broad degree of anti-HCV activity was observed. The most active compounds were kaempferol-3,7-bisrhamnoside (19.4 μM) and (3S)-3-hydroxy-1,7-bis(4-hydroxy-phenyl)-6E-hepten-5-one (28.7 μM). In conclusion, flavonoids and diarylheptanoids were responsible for the anti-HCV constitution of Taxilli Herba. These inhibitors of HCV NS3 protease might serve as potential candidate of anti-HCV agents.
本研究旨在从传统中药四川桑寄生中分离出活性化合物，以抑制丙型肝炎病毒（HCV）NS3蛋白酶的活性。在生物测定的指导下，从乙酸乙酯提取物部分分离出10种化合物，它们被鉴定为HCV NS3蛋白酶的抑制剂。获得了这些化合物的半数抑制浓度（IC）值，并观察到了广泛的抗HCV活性。活性最强的化合物是山奈酚-3,7-双鼠李糖苷（19.4 μM）和（3S）-3-羟基-1,7-双（4-羟基苯基）-6E-庚烯-5-酮（28.7 μM）。总之，黄酮类化合物和二芳基庚烷类化合物是桑寄生抗HCV成分的原因。这些HCV NS3蛋白酶抑制剂可能作为抗HCV药物的潜在候选物。
