Archives of Pharmacal Research

The Pharmaceutical Society of Korea (대한약학회)
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Tissue Factor Inhibitory Flavonoids from the Fruits of Chaenomeles sinensis

  • Lee, Ming-Hong (Natural Products Research Institute, Seoul National University) ;
  • Son, Yeon-Kyoung (Natural Products Research Institute, Seoul National University) ;
  • Han, Yong-Nam (Natural Products Research Institute and College of Pharmacy, Seoul National University)
  • Published : 2002.12.01
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Abstract

Tissue factor (TF, tissue thromboplastin or coagulation factor III) accelerates the blood clotting, activating both the intrinsic and the extrinsic pathways to serve as a cofactor. In order to isolate TF inhibitors from the fruits of Chaenomeles sinensis, an activity-guided purification utilizing a bio-assay method of prothrombin time prolongation, was carried out to yield five active flavoniods such as hovetrichoside C (1) ($IC_{50}$ = 14.0 $\mu$g), luteolin-7-Ο-$\beta$-D-glucuronide (3) ($IC_{50}$ = 31.9$\mu$g), hyperin (4) ($IC_{50}$ = 20.8 $\mu$g), avicularin (6) ($IC_{50}$ = 54.8 $\mu$g) and quercitrin (10) ($IC_{50}$ = 135.7 $\mu$g), along with other inactive compounds such as ($\pm$)-(2E,4E)-Ο-$\beta$-D-glucopyranosyl-4'-hydroxy-$\beta$-ionylideneacetic acid ester (2), genistein-7-Ο-$\beta$-D-glucopyranoside (5), luteolin-3'-methoxy-4'-Ο-$\beta$-D-glucopyranoside (7), luteolin-7-Ο-$\beta$-D-glucuronide methyl ester (8), tricetin-3'-methoxy-4'-Ο-$\beta$-D-glucopyranoside (selagin-4'-Ο-$\beta$-D-glucopyranoside) (9), (-)-epicatechin (11), luteolin-4'-Ο-$\beta$-D-glucopyranoside (12) and apigenin-7-Ο-$\beta$-D-glucuronide methyl ester (13). The structures of the isolated compounds were elucidated through spectral analysis. Among them, compounds 1 to 9, 12 and 13 were isolated for the first time from the fruits of this plant and the compound 9 is a new flavonoid.

Keywords

References

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