• Applied Biological Chemistry
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• 제42권4호
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• pp.351-355
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• 1999

갈화로부터 항치매 효과를 기대할 수 있는 prolyl endopeptidase(PEP) 저해제를 분리하기 위하여 갈화의 methanol 추출물을 chloroform 및 ethyl acetate로 분배추출 후 chloroform 가용성 분획에 대하여 silica gel, Sephadex LH-20 column chromatography 및 RP-HPLC를 행한 결과, $FeCl_3$,에 양성 반음을 나타내는 4종의 화합물을 얻었다. 이들을 $^1H-$, $^{13}C-$, $^2D-NMR$ 및 MS 등을 이용하여 분석한 결과, 각각 tectorigenin, genistein, 5,7-dihydroxy-4',6-dimethoxyisoflavone, 5-hydroxy-6,7,4'-trimethoxyisoflavone으로 동정하었으며 HMBC, HMQC를 통하여 $^{13}C-NMR$ signal들을 assign함으로써 기 보고된 data들의 오류를 바로잡았다. PEP에 대한 이 화합물들의 $IC_{50}$값은 각각 5.30 ppm$(17.7\;{\mu}M)$, 10.39 ppm$(38.5\;{\mu}M)$, 13.92 ppm$(44.3\;{\mu}M)$, 20.61 ppm$(62.8\;{\mu}M)$이었다.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1995년도 춘계학술대회
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• pp.47-49
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• 1995

• Food Science and Biotechnology
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• 제15권4호
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• pp.617-624
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• 2006

Various plant phenolics were assessed for (${\beta}$-secretase (BACE1) inhibitory activity in order to screen for anti-dementia agents. Among 39 phenolics, eight compounds, 1,2,3-trigalloyl glucopyranoside, acetonyl geraniin, euphorscopin, furosine, helioscopinin A, helioscopinin B, jolkinin, and rugosin E exhibited strong inhibition of BACE1 with $IC_{50}$ values of $5.87{\times}10^{-8}-54.93{\times}10^{-6}\;M$. Among them, rugosin E was the most potent ($IC_{50}$ $5.87{\times}10^{-8}\;M$). The active compounds were shown to be non-competitive inhibitors by Dixon plot. All the phenolic BACE1 inhibitors except furosin also suppressed prolyl endopeptidase (PEP) activity. However, these phenolic compounds caused less inhibition of ${\alpha}$-secretase (tumor necrosis factor a converting enzyme; TACE) and no significant inhibition of other serine proteases such as trypsin, chymotrypsin, and elastase was seen, demonstrating that they are relatively specific to both BACE1 and PEP. No significant structure-activity relationships were found.