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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 29, Number 3
BKCSDE 29(3)
March 20, 2008

Title	Human Acyl-CoA: Cholesterol Acyltransferase (hACAT) Inhibitory Activities of Triterpenoids from Roots of Glycine max (L.) Merr.
Author	Jin Hwan Lee, Young Bae Ryu, Byong Won Lee, Jin Hyo Kim, Woo Song Lee, Yong-Dae Park, Tae-Sook Jeong, Ki Hun Park*
Keywords	Glycine max, Root, Human acyl-CoA: cholesterol acytransferase (hACAT), Triterpenoid, Atherosclerosis
Abstract	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 3β-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 μ M) than hACAT-2 (1: IC₅₀ = 102.0 ± 5.4 and 7: IC₅₀ = 33.9 ± 3.7 μ M), respectively. Interestingly, 5α ,8α -epidioxy-24(R)-methylcholesta-6,22-diene-3β -ol (4) has proven to be a specific inhibitor against hACAT-1 (IC₅₀ = 38.7 ± 0.8 μM) 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.
Page	615 - 619
Full Text	PDF

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