title: Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells.
abstract: Eight chalcone analogues were prepared and evaluated for their cytotoxic effects in human hepatoma HepG2 cells. Compound 5 had a potent cytotoxic effect. The percentage of apoptotic cells was significantly higher in compound 5-treated cells than in control cells. Exposure to compound 5 for 24h induced cleavage of caspase-8 and -3, and poly (ADP-ribose) polymerase (PARP). Our findings suggest that compound 5 is the active chalcone analogue that contributes to cell death in HepG2 cells via the extrinsic apoptotic pathway.
authors.affiliation: Department of Surgery, Gangneung Asan Hospital, University of Ulsan College of Medicine, Gangneung 210-711, Republic of Korea.
authors.forename: Cheon-Soo
authors.initials: CS
authors.lastname: Park
authors.affiliation: Department of Hematology and Oncology, Gangneung Asan Hospital, University of Ulsan College of Medicine, Gangneung 210-711, Republic of Korea.
authors.forename: Yongchel
authors.initials: Y
authors.lastname: Ahn
authors.affiliation: College of Korean Medicine, Gachon University, Seongnam 461-701, Republic of Korea.
authors.forename: Dahae
authors.initials: D
authors.lastname: Lee
authors.affiliation: Department of Chemistry, Gangneung Wonju National University, Gangneung 210-340, Republic of Korea; Natural Product Research Center, Korea Institute of Science and Technology, Gangneung 210-340, Republic of Korea.
authors.forename: Sung Won
authors.initials: SW
authors.lastname: Moon
authors.affiliation: Natural Product Research Laboratory, School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
authors.forename: Ki Hyun
authors.initials: KH
authors.lastname: Kim
authors.affiliation: College of Korean Medicine, Gachon University, Seongnam 461-701, Republic of Korea.
authors.forename: Noriko
authors.initials: N
authors.lastname: Yamabe
authors.affiliation: College of Korean Medicine, Gachon University, Seongnam 461-701, Republic of Korea.
authors.forename: Gwi Seo
authors.initials: GS
authors.lastname: Hwang
authors.affiliation: Department of Surgery, Gangneung Asan Hospital, University of Ulsan College of Medicine, Gangneung 210-711, Republic of Korea.
authors.forename: Hyuk Jai
authors.initials: HJ
authors.lastname: Jang
authors.affiliation: Department of Oral Anatomy, College of Dentistry, Gangneung Wonju National University, 201-340, Republic of Korea.
authors.forename: Heesu
authors.initials: H
authors.lastname: Lee
authors.affiliation: College of Korean Medicine, Gachon University, Seongnam 461-701, Republic of Korea. Electronic address: kkang@gachon.ac.kr.
authors.forename: Ki Sung
authors.initials: KS
authors.lastname: Kang
authors.affiliation: Natural Product Research Center, Korea Institute of Science and Technology, Gangneung 210-340, Republic of Korea; Department of Biological Chemistry, University of Science and Technology (UST), Daejeon 305-333, Republic of Korea. Electronic address: jwlee5@kist.re.kr.
authors.forename: Jae Wook
authors.initials: JW
authors.lastname: Lee
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D006528:Carcinoma, Hepatocellular / Q000378:metabolism / Q000473:pathology; D053148:Caspase 3 / Q000378:metabolism; D053181:Caspase 8 / Q000378:metabolism; D002470:Cell Survival / Q000187:drug effects; D002599:Chalcone / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D056945:Hep G2 Cells; D006801:Humans; D008113:Liver Neoplasms / Q000378:metabolism / Q000473:pathology; D011065:Poly(ADP-ribose) Polymerases / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D002599:Chalcone; D011065:Poly(ADP-ribose) Polymerases; D053148:Caspase 3; D053181:Caspase 8
keywords: Anticancer; Apoptosis; Chalcone; HepG2