title: Antitumor agents. Part 218: Cappamensin A, a new In vitro anticancer principle, from Capparis sikkimensis.
abstract: A new inhibitor of in vitro tumor cell replication, cappamensin A (1) (2H-1,4-benzoxazin-3(4H)-one, 6-methoxy-2-methyl-4-carbaldehyde), was isolated from the roots of Capparis sikkimensis subsp. formosana using bioactivity-guided fractionation. The structure of 1 was established by spectroscopic methods, including 2D NMR analyses. Compound 1 displayed significant in vitro anticancer activity against ovarian (1A9), lung (A549), ileocecal (HCT-8), breast (MCF-7), nasopharyngeal (KB), and vincristine resistant (KB-VIN) human tumor cell lines with ED(50) values </=4 microgram/mL (mean GI(50) value of 15.1 microM).
authors.affiliation: Natural Products Laboratory, School of Pharmacy, University of North Carolina, 27599, Chapel Hill, NC, USA.
authors.forename: Jiu Hong
authors.initials: JH
authors.lastname: Wu
authors.forename: Fang Rong
authors.initials: FR
authors.lastname: Chang
authors.forename: Ken ichiro
authors.initials: Ki
authors.lastname: Hayashi
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Shiraki
authors.forename: Chih Chuang
authors.initials: CC
authors.lastname: Liaw
authors.forename: Yuka
authors.initials: Y
authors.lastname: Nakanishi
authors.forename: Kenneth F
authors.initials: KF
authors.lastname: Bastow
authors.forename: Donglei
authors.initials: D
authors.lastname: Yu
authors.forename: Ih Sheng
authors.initials: IS
authors.lastname: Chen
authors.forename: Kuo Hsiung
authors.initials: KH
authors.lastname: Lee
mesh_terms: D000447:Aldehydes / Q000737:chemistry* / Q000494:pharmacology*; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000494:pharmacology*; D048588:Benzoxazines; D031484:Capparis / Q000737:chemistry*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D010078:Oxazines / Q000737:chemistry* / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: C481964:2H-1,4-benzoxazin-3(4H)-one, 6-methoxy-2-methyl-4-carbaldehyde; D000447:Aldehydes; D000972:Antineoplastic Agents, Phytogenic; D048588:Benzoxazines; D010078:Oxazines