Human ACAT-1 and -2 inhibitory activities of saucerneol B, manassantin A and B isolated from Saururus chinensis

Compounds 1– 3 isolated from the methanolic extracts of Saururus chinensis root inhibited hACAT-1 and hACAT-2 activities. The EtOAc-soluble fraction, which contained compounds 1– 3, of methanol extracts of S. chinensis exhibited strong cholesterol-lowering effect in high cholesterol-fed mice. The se...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2004-06, Vol.14 (12), p.3109-3112
Hauptverfasser: Lee, Woo Song, Lee, Dae-Woo, Baek, Young-Il, An, So-Jin, Cho, Kyung-Hyun, Choi, Yang-Kyu, Kim, Hyoung-Chin, Park, Ho-Yong, Bae, Ki-Hwan, Jeong, Tae-Sook
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container_end_page 3112
container_issue 12
container_start_page 3109
container_title Bioorganic & medicinal chemistry letters
container_volume 14
creator Lee, Woo Song
Lee, Dae-Woo
Baek, Young-Il
An, So-Jin
Cho, Kyung-Hyun
Choi, Yang-Kyu
Kim, Hyoung-Chin
Park, Ho-Yong
Bae, Ki-Hwan
Jeong, Tae-Sook
description Compounds 1– 3 isolated from the methanolic extracts of Saururus chinensis root inhibited hACAT-1 and hACAT-2 activities. The EtOAc-soluble fraction, which contained compounds 1– 3, of methanol extracts of S. chinensis exhibited strong cholesterol-lowering effect in high cholesterol-fed mice. The sesquineolignan, saucerneol B ( 1), and dineolignans, manassantin A ( 2), and manassantin B ( 3), were isolated from the methanol extracts of Saururus chinensis root and elucidated by their spectroscopic data analysis. Compounds 1– 3 inhibited hACAT-1 and hACAT-2 with IC 50 values of 43.0 and 124.0 μM for 1, of 39.0 and 8.0 μM for 2, of 82.0 μM and only 32% inhibition at 1 mM for 3, respectively. The EtOAc-soluble fraction, which contained compounds 1– 3, of methanol extracts of S. chinensis exhibited strong cholesterol-lowering effect in high cholesterol-fed mice.
doi_str_mv 10.1016/j.bmcl.2004.04.023
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subjects Animals
Biological and medical sciences
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - isolation & purification
Enzyme Inhibitors - pharmacology
Furans - chemistry
Furans - isolation & purification
Furans - pharmacology
hACAT-1 and hACAT-2
Humans
Hypocholesterolemic activity
Inhibitor
Lignans
Lignans - chemistry
Lignans - isolation & purification
Lignans - pharmacology
Male
Medical sciences
Mice
Mice, Inbred C57BL
Miscellaneous
Pharmacology. Drug treatments
Plant Extracts - chemistry
Plant Extracts - isolation & purification
Plant Extracts - pharmacology
Plant Roots
S. chinensis
Saururaceae
Sterol O-Acyltransferase - antagonists & inhibitors
Sterol O-Acyltransferase - metabolism
Sterol O-Acyltransferase 2
title Human ACAT-1 and -2 inhibitory activities of saucerneol B, manassantin A and B isolated from Saururus chinensis
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