Anti-inflammatory and antitumor-promoting effects of the triterpene acids from the leaves of Eriobotrya japonica.
Sixteen triterpene acids, viz., five of the oleanane-type (1-5), nine of the ursane-type (6-14), and two of the lupane-type (15, 16), were isolated and identified from the ethyl acetate-soluble fraction of the methanol extract of the leaves of loquat, Eriobotrya japonica LINDL. (Rosaceae). Twelve of these compounds, 1-4, 6, 8-13, and 15, were evaluated for their inhibitory effects on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation (1 microg/ear) in mice. All the compounds tested showed a marked anti-inflammatory effect, with a 50% inhibitory dose (ID50) of 0.03-0.43 mg per ear. In addition, an evaluation against the Epstein-Barr virus early antigen (EBV-EA) activation induced by TPA for all of the compounds, 12 and 13 showed potent inhibitory effects on EBV-EA induction. Furthermore, euscaphic acid (12) exhibited marked antitumor-promoting activity in an in vivo two-stage carcinogenesis test of mouse tumor by using 7,12-dimethylbenz[a]anthracene (DMBA) as an initiator and TPA as a promoter.
Banno
Norihiro
N
Ichimaru Pharcos Company Ltd; 318-1 Asaki, Motosu, gifu 501-0475, Japan.
Akihisa
Toshihiro
T
Tokuda
Harukuni
H
Yasukawa
Ken
K
Taguchi
Yosuke
Y
Akazawa
Hiroyuki
H
Ukiya
Motohiko
M
Kimura
Yumiko
Y
Suzuki
Takashi
T
Nishino
Hoyoku
H
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000302:isolation & purification / Q000494:pharmacology*; D016588:Anticarcinogenic Agents / Q000302:isolation & purification / Q000494:pharmacology*; D002851:Chromatography, High Pressure Liquid; D031983:Eriobotrya / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D010212:Papilloma / Q000517:prevention & control; D018515:Plant Leaves / Q000737:chemistry*; D012878:Skin Neoplasms / Q000517:prevention & control; D021241:Spectrometry, Mass, Electrospray Ionization; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology*
D000893:Anti-Inflammatory Agents; D016588:Anticarcinogenic Agents; D014315:Triterpenes; D013755:Tetradecanoylphorbol Acetate