title: Chalcones isolated from Angelica keiskei inhibit cysteine proteases of SARS-CoV.
abstract: Two viral proteases of severe acute respiratory syndrome coronavirus (SARS-CoV), a chymotrypsin-like protease (3CL(pro)) and a papain-like protease (PL(pro)) are attractive targets for the development of anti-SARS drugs. In this study, nine alkylated chalcones (1-9) and four coumarins (10-13) were isolated from Angelica keiskei, and the inhibitory activities of these constituents against SARS-CoV proteases (3CL(pro) and PL(pro)) were determined (cell-free/based). Of the isolated alkylated chalcones, chalcone 6, containing the perhydroxyl group, exhibited the most potent 3CL(pro) and PL(pro) inhibitory activity with IC50 values of 11.4 and 1.2 µM. Our detailed protein-inhibitor mechanistic analysis of these species indicated that the chalcones exhibited competitive inhibition characteristics to the SARS-CoV 3CL(pro), whereas noncompetitive inhibition was observed with the SARS-CoV PL(pro).
authors: a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .
authors: Ji-Young
authors: JY
authors: Park
authors: a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .
authors: Jin-A
authors: JA
authors: Ko
authors: b Division of Applied Life Science (BK21 program, IALS) , Graduate School of Gyeongsang National University , Jinju , Republic of Korea , and.
authors: Dae Wook
authors: DW
authors: Kim
authors: c Department of Food Science & Technology and Functional Food Research Center , Chonnam National University , Gwangju , Republic of Korea.
authors: Young Min
authors: YM
authors: Kim
authors: a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .
authors: Hyung-Jun
authors: HJ
authors: Kwon
authors: a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .
authors: Hyung Jae
authors: HJ
authors: Jeong
authors: a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .
authors: Cha Young
authors: CY
authors: Kim
authors: b Division of Applied Life Science (BK21 program, IALS) , Graduate School of Gyeongsang National University , Jinju , Republic of Korea , and.
authors: Ki Hun
authors: KH
authors: Park
authors: a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .
authors: Woo Song
authors: WS
authors: Lee
authors: a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .
authors: Young Bae
authors: YB
authors: Ryu
mesh_terms: D029969:Angelica / Q000737:chemistry*; D000998:Antiviral Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D047188:Chalcones / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D057056:Cysteine Proteases / Q000378:metabolism*; D015853:Cysteine Proteinase Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D045473:Severe acute respiratory syndrome-related coronavirus / Q000187:drug effects / Q000201:enzymology*; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D047188:Chalcones; D015853:Cysteine Proteinase Inhibitors; D057056:Cysteine Proteases
keywords: 3CLpro; Angelica keiskei; PLpro; SARS-CoV; chalcone