title: A new synthetic 2'-hydroxy-2,4,6-trimethoxy-5',6'-naphthochalcone induces G2/M cell cycle arrest and apoptosis by disrupting the microtubular network of human colon cancer cells.
abstract: Methoxylated chalcones exert antitumor activities. In the present study, we characterized the cytotoxicity of methylated chalcone derivatives against human colon cancer cells. We synthesized a group of methoxychalcones and explored the molecular mechanisms underlying inhibition of tumor growth by these materials. A new synthetic methoxychalcone, 2'-hydroxy-2,4,6-trimethoxy-5',6'-naphthochalcone (named HMNC-74), most effectively inhibited the clonogenicity of SW620 colon cancer cells. Mechanistically, HMNC-74 triggered cell cycle arrest at G2/M phase, followed by an increase in apoptotic cell death. Our results indicate that the cytotoxicity of the novel compound HMNC-74 involves the disruption of microtubular networks.
authors.affiliation: Department of Biological Sciences, College of Biological Science and Biotechnology, Cancer and Metabolism Institute, Konkuk University, Seoul 143-701, Republic of Korea.
authors.forename: Jong Min
authors.initials: JM
authors.lastname: Lee
authors.affiliation: Department of Biological Sciences, College of Biological Science and Biotechnology, Cancer and Metabolism Institute, Konkuk University, Seoul 143-701, Republic of Korea.
authors.forename: Mi So
authors.initials: MS
authors.lastname: Lee
authors.affiliation: Department of Applied Chemistry, Dongduk Women's University, Seoul 136-714, Republic of Korea.
authors.forename: Dongsoo
authors.initials: D
authors.lastname: Koh
authors.affiliation: Department of Biological Sciences, College of Biological Science and Biotechnology, Cancer and Metabolism Institute, Konkuk University, Seoul 143-701, Republic of Korea.
authors.forename: Young Han
authors.initials: YH
authors.lastname: Lee
authors.affiliation: Division of Bioscience and Biotechnology, BMIC, Konkuk University, Seoul 143-701, Republic of Korea. Electronic address: yoongho@konkuk.ac.kr.
authors.forename: Yoongho
authors.initials: Y
authors.lastname: Lim
authors.affiliation: Department of Biological Sciences, College of Biological Science and Biotechnology, Cancer and Metabolism Institute, Konkuk University, Seoul 143-701, Republic of Korea. Electronic address: shinsy@konkuk.ac.kr.
authors.forename: Soon Young
authors.initials: SY
authors.lastname: Shin
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D002599:Chalcone / Q000031:analogs & derivatives* / Q000494:pharmacology; D047188:Chalcones / Q000494:pharmacology*; D003110:Colonic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D059565:G2 Phase Cell Cycle Checkpoints / Q000187:drug effects; D045325:HCT116 Cells; D006801:Humans; D059566:M Phase Cell Cycle Checkpoints / Q000187:drug effects; D008870:Microtubules / Q000187:drug effects / Q000473:pathology
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones; D002599:Chalcone
keywords: 2′-Hydroxy-2,4,6-trimethoxy-5′,6′-naphthochalcone; Apoptosis; Caspase-2; G2/M arrest; Tubulin polymerization