• 제목/요약/키워드: cholesterol acytransferase (ACAT)

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Human Acyl-CoA: Cholesterol Acyltransferase Inhibitory Effect of Flavonoids from Roots of Glycine max (L.) Merr

  • Lee, Jin-Hwan;Seo, Woo-Duck;Jeong, Seong-Hun;Jeong, Tae-Sook;Lee, Woo-Song;Park, Ki-Hun
    • Journal of Applied Biological Chemistry
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    • 제49권2호
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    • pp.57-61
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    • 2006
  • Isoflavones 1-3 and pterocarpans 4-8 were isolated from methanol extract of roots of Glycine max. In inhibitory effect against human acyl-CoA:cholesterol acytransferase (ACAT)-1 and ACAT-2, glyceollin I 5 showed potent hACAT-1 ($IC_{50}=299.0{\mu}M$) and hACAT-2 ($IC_{50}=82.7{\mu}M$) inhibitory activities.

Human Acyl-CoA: Cholesterol Acyltransferase (hACAT) Inhibitory Activities of Triterpenoids from Roots of Glycine max (L.) Merr

  • Lee, Jin-Hwan;Ryu, Young-Bae;Lee, Byong-Won;Kim, Jin-Hyo;Lee, Woo-Song;Park, Yong-Dae;Jeong, Tae-Sook;Park, Ki-Hun
    • Bulletin of the Korean Chemical Society
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    • 제29권3호
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    • pp.615-619
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    • 2008
  • Eight triterpenoids, six lanostanes 1-6, one lupenane 7, and one oleanane 8, were isolated by bioactivity-guided fractionation of the ethylacetate extract from roots of Glycine max (L.) Merr. All isolated compounds were examined for their inhibitory activities against human ACAT-1 (hACAT-1) and human ACAT-2 (hACAT-2). Among them, three triterpenoids showed potent hACAT inhibitory activities, (24R)-ethylcholest-5-ene-3,7-diol (1) and 3b -hydroxylup-20(29)-en-28-oic acid (7) exhibited more potent inhibitory activity against hACAT-1 (1: IC50 = 25.0 1.2 and 7: IC50 = 11.5 0.4 m M) than hACAT-2 (1: IC50 = 102.0 5.4 and 7: IC50 = 33.9 3.7 m M), respectively. Interestingly, 5a ,8a -epidioxy-24(R)-methylcholesta-6,22-diene-3b -ol (4) has proven to be a specific inhibitor against hACAT-1 (IC50 = 38.7 0.8 m M) compared to hACAT-2 (IC50 >200). In conclusion, this is the first study to demonstrate that triterpenoids of G. max have potent inhibitory activities against hACAT-1 and hACAT-2.