Antitumor agents. Part 218: Cappamensin A, a new In vitro anticancer principle, from Capparis sikkimensis.
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).
Wu
Jiu Hong
JH
Natural Products Laboratory, School of Pharmacy, University of North Carolina, 27599, Chapel Hill, NC, USA.
Chang
Fang Rong
FR
Hayashi
Ken ichiro
Ki
Shiraki
Hiroaki
H
Liaw
Chih Chuang
CC
Nakanishi
Yuka
Y
Bastow
Kenneth F
KF
Yu
Donglei
D
Chen
Ih Sheng
IS
Lee
Kuo Hsiung
KH
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
C481964:2H-1,4-benzoxazin-3(4H)-one, 6-methoxy-2-methyl-4-carbaldehyde; D000447:Aldehydes; D000972:Antineoplastic Agents, Phytogenic; D048588:Benzoxazines; D010078:Oxazines