title: SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii.
abstract: Quinone-methide triterpenes, celastrol (1), pristimerin (2), tingenone (3), and iguesterin (4) were isolated from Triterygium regelii and dihydrocelastrol (5) was synthesized by hydrogenation under palladium catalyst. Isolated quinone-methide triterpenes (1-4) and 5 were evaluated for SARS-CoV 3CL(pro) inhibitory activities and showed potent inhibitory activities with IC(50) values of 10.3, 5.5, 9.9, and 2.6 microM, respectively, whereas the corresponding 5 having phenol moiety was observed in low activity (IC(50)=21.7 microM). As a result, quinone-methide moiety in A-ring and more hydrophobic E-ring assist to exhibit potent activity. Also, all quinone-methide triterpenes 1-4 have proven to be competitive by the kinetic analysis.
authors.affiliation: Eco-Friendly Biomaterial Research Center, Korea Research Institute of Bioscience and Biotechnology, Jeongeup, Republic of Korea.
authors.forename: Young Bae
authors.initials: YB
authors.lastname: Ryu
authors.forename: Su-Jin
authors.initials: SJ
authors.lastname: Park
authors.forename: Young Min
authors.initials: YM
authors.lastname: Kim
authors.forename: Ju-Yeon
authors.initials: JY
authors.lastname: Lee
authors.forename: Woo Duck
authors.initials: WD
authors.lastname: Seo
authors.forename: Jong Sun
authors.initials: JS
authors.lastname: Chang
authors.forename: Ki Hun
authors.initials: KH
authors.lastname: Park
authors.forename: Mun-Chual
authors.initials: MC
authors.lastname: Rho
authors.forename: Woo Song
authors.initials: WS
authors.lastname: Lee
mesh_terms: D000998:Antiviral Agents / Q000494:pharmacology*; D016227:Benzoquinones / Q000737:chemistry*; D008958:Models, Molecular; D010936:Plant Extracts / Q000494:pharmacology*; D045473:Severe acute respiratory syndrome-related coronavirus / Q000187:drug effects*; D029757:Tripterygium / Q000737:chemistry*; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000998:Antiviral Agents; D016227:Benzoquinones; D010936:Plant Extracts; D014315:Triterpenes; C004532:quinone