Platelet-activating factor (PAF) receptor binding antagonists from Alpinia officinarum.
The bioassay-guided purification of ether extracts of Alpinia officinarum led to the isolation of two new compounds 6-hydroxy-1,7-diphenyl-4-en-3-heptanone (1) and 6-(2-hydroxy-phenyl)-4-methoxy-2-pyrone (4) as well as three known compounds 1,7-diphenyl-4-en-3-heptanone (2), 1,7-diphenyl-5-methoxy-3-heptanone (3), and apigenin (5). Their structures were established on the basis of spectral methods. All three diarylheptanoids 1, 2, and 3 exhibited potent PAF receptor binding inhibitory activities with an IC(50) of 1.3, 5.0, and 1.6 microM, respectively. These studies have identified diarylheptanoids as a novel class of potent PAF antagonists.
Fan
Gao-Jun
GJ
Natural Products Research Institute, Seoul National University, 28 Yungun-dong, Jongro-gu, Seoul 110-460, Republic of Korea.
Kang
Young-Hwa
YH
Han
Yong Nam
YN
Han
Byung Hoon
BH
D032429:Alpinia / Q000737:chemistry*; D015394:Molecular Structure; D010980:Platelet Membrane Glycoproteins / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D011485:Protein Binding; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors* / Q000378:metabolism*
D010980:Platelet Membrane Glycoproteins; D043562:Receptors, G-Protein-Coupled; C039351:platelet activating factor receptor