KMID : 0043320070300040412
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Archives of Pharmacal Research 2007 Volume.30 No. 4 p.412 ~ p.418
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Triterpenoids and Diarylheptanoids from Alnus hirsuta Inhibit HIF-1 in AGS Cells
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Jin WenYi
Cai Xing Fu Na Min-Kyun Lee Jung-Joon Bae Ki-Hwan
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Abstract
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Bioassay-guided fractionation and purification of the EtOAc soluble fraction from the MeOH extract of the stem bark of Alnus hirsuta (Betulaceae), using an in vitro HIF-1 assay, led to the isolation of four triterpenoids (1-4) and six diarylheptanoids (5-10). Their structures were determined by comparison with the physicochemical and spectroscopic data in the literature. These compounds were investigated for their effects on the hypoxia-induced HIF-1 activation using an HIF-1a mediated reporter gene assay in AGS cells. Among them, two diarylheptanoids, 2- oxatrycyclo[13.2.2.13,7]eicosa-3,5,7(20),15,17,18-hexaen-10-16-diol (6) and 2-oxatrycyclo [13.2.2.13,7]eicosa-3,5,7-(20),15,17,18-hexaen-10-one (7), inhibited HIF-1 activation dosedependently with IC50 values of 11.2 ¥ìM and 12.3 ¥ìM, respectively. These two compounds had no significant cytotoxicity to the AGS cells at the effective concentration for the inhibition of HIF-1 activation
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KEYWORD
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Alnus hirsuta, Betulaceae, Triterpenoid, Diarylheptanoid, HIF-1 activation
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