Activity of compounds from Taxillus sutchuenensis as inhibitors of HCV NS3 serine protease.
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. IC50values 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.
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.
Liyuan
L
Yang
b State Key Laboratory of New Drug and Pharmaceutical Process , Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry , Shanghai , China.
Jun
J
Lin
b State Key Laboratory of New Drug and Pharmaceutical Process , Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry , Shanghai , China.
Bin
B
Zhou
a School of Pharmacy , Shanghai Jiao Tong University , Shanghai , China.
Yangang
Y
Liu
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.
Baoquan
B
Zhu
D000998:Antiviral Agents / Q000494:pharmacology*; D005419:Flavonoids / Q000494:pharmacology; D028183:Loranthaceae / Q000737:chemistry*; D010936:Plant Extracts / Q000494:pharmacology*; D015842:Serine Proteinase Inhibitors / Q000494:pharmacology*; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*; D012697:Serine Endopeptidases; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases
D000998:Antiviral Agents; D005419:Flavonoids; D010936:Plant Extracts; D015842:Serine Proteinase Inhibitors; D017361:Viral Nonstructural Proteins; C084422:NS3 protein, hepatitis C virus; D012697:Serine Endopeptidases; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases
Antiviral; HCV NS3 protease; Taxillus sutchuenensis (Lecomte) Danser; inhibitor