• Title/Summary/Keyword: ACAT inhibition assay

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Antiarteriosclerosis Effects of Black Rices Extract (흑미 추출물에 대한 항동맥경화 효과(Notes))

  • Lim, Chi-Hwan;Kim, Jong-Min;Baek, Seung-Hwa
    • Journal of Society of Preventive Korean Medicine
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    • v.12 no.3
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    • pp.91-98
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    • 2008
  • 80% MeOH extract of black rices fractionated with n-hexane, EtOAc, and n-BuOH. Copper-induced LDL oxidation inhibition assay and ACAT inhibition assay examined with fractions. n-Hexane and EtOAc fractions showed high inhibition activity. We divided n-hexane fraction into three sub-layers(H1 - H3) and EtOAc into eight sub-layers(E1 - E8). H1, H2, E6, and E7 are showed higher inhibition activity than standard in Lp-PLA2 inhibition assay and H1 and E6 are showed higher ACAT inhibition activity than standard.

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Biological Activities of Sesquiterpene Lactones isolated from Several Compositae Plants Part 3 -Inhibitory Activity on Nitric Oxide Release and ACAT- (수종의 국화과 식물에서 분리한 Sesquiterpene Lactone들의 생리활성(제3보) -Nitric oxide 방출 및 ACAT 저해활성-)

  • Jang, Dae-Sik;Park, Ki-Hun;Ko, Hack-Lyong;Lee, Hyun-Sun;Kwon, Byoung-Mog;Yang, Min-Suk
    • Korean Journal of Pharmacognosy
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    • v.30 no.1
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    • pp.74-78
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    • 1999
  • Nine sesquiterpene lactones, which were isolated from Hemisteptia lyrata Bunge, Chrysanthemum zawadskii Herbich var. latilobum Kitamura and Chrysanthemum boreale Makino were evaluated for the inhibition upon the nitric oxide release from the Raw cell and for the ACAT (acyl Co A: cholesterol acyltransferase) inhibitory assay. In the nitric oxide release inhibitory experiment, hemistepsin B $(IC_{50}\;=\;0.05\;{\mu}g/ml,\;0.15\;{\mu}M),$ cumambrin B, tulipinolide and costunolide exhibited strong inhibition with $IC_{50}$ values $0.05\;{\mu}g/ml\;(0.15\;{\mu}M),\;0.1\;{\mu}g/ml\;(0.38\;{\mu}M),\;0.2\;{\mu}g/ml\;(0.69\;{\mu}M)$ and $0.2\;{\mu}g/ml(0.86\;{\mu}M),$ respectively. In the ACAT inhibitory assay, angeloylcumambrin B, tigloylcumambrin B, tulipinolide and costunolide exhibited strong inhibition with $IC_{50}$ values $33\;{\mu}g/ml\;(95.4\;{\mu}M),\;22\;{\mu}g/ml\;(63.6\;{\mu}M),\;38\;{\mu}g/ml\;(151\;{\mu}M)$ and $17\;{\mu}g/ml(73.3\;{\mu}M),$ respectively, whereas other compounds did not exhibit significant activity against ACAT above $100\; {\mu}g/ml.$.

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Isolation of Guaianolides with ACAT Inhibitory Activity from the Leaves and Stems of Chrysanthemum boreale Makino (산국의 잎과 줄기에서 ACAT 저해활성을 가지는 Guaianolides의 분리)

  • Lee, Jong Rok;Park, Moon Ki
    • Journal of Environmental Science International
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    • v.26 no.11
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    • pp.1275-1284
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    • 2017
  • Acyltransferase (AT) catalyzes the transfer of an acyl moiety from acyl-coenzyme A (acyl-CoA) to an acceptor. ATs play important roles in the maintenance of homeostasis in the human body and have been linked to various diseases; therefore, several ATs have been proposed as potential targets for the treatment or prevention of such diseases. The AT family includes acyl-CoA:cholesterol AT (ACAT), diacylglycerol AT, and monoacylglycerol AT for the metabolism of lipids. Furthermore, recent molecular biological studies revealed the existence of their isozymes with distinct functions in the body. ACAT plays a critical role in the formation of cholesteryl esters from cholesterol and fatty acids, and is a potential target for treating hypercholesterolemia. During an experiment designed to discover biologically active compounds from herbal medicines, we isolated two known guaianolide sesquiterpene lactones from Chrysanthemum boreale Makino (Compositae). The lactones were characterized from their spectroscopic data (NMR, IR, MASS). These compounds were subjected to ACAT inhibition assay. Here, we report the isolation and structural elucidation of the compounds 8-o-acetyl-2-methoxy-10-hydroxy-3,11(13)-guaiadiene-12,6-olide and 8-acetyl-3,10-hydroxy-4(15),11(13)-guaiadiene-12,6-olide. In the ACAT inhibition assay, compound 1 showed strong inhibitory activity, with an $IC_{50}$ value $45{\mu}g/mL$, whereas compound 2 did not exhibit significant inhibitory activity with an over $100{\mu}g/mL$.