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Hesperidin and hesperetin as inhibitor of acyl coa-cholesterol-o-acyltransferase, inhibitor of macrophage-lipid complex accumulation on the arterial wall and preventive agent

An acyltransferase, hesperetin technology is used as an acyl CoA-cholesterol-O-acyltransferase inhibitor, an inhibitor of macrophage-lipid complex accumulation on the arterial wall, and the prevention or treatment of liver disease In the field of hesperidin or hesperetin, no one has reported that ACAT inhibits active macrophage-lipid complex accumulation and inhibits active liver disease prevention or treatment activity.

Inactive Publication Date: 2000-12-27
KOREA INST OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, no one has reported the ACAT inhibitory activity of hesperidin or hesperetin, the macrophage-lipid complex accumulation inhibitory activity, and the preventive or therapeutic activity against liver diseases

Method used

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  • Hesperidin and hesperetin as inhibitor of acyl coa-cholesterol-o-acyltransferase, inhibitor of macrophage-lipid complex accumulation on the arterial wall and preventive agent
  • Hesperidin and hesperetin as inhibitor of acyl coa-cholesterol-o-acyltransferase, inhibitor of macrophage-lipid complex accumulation on the arterial wall and preventive agent
  • Hesperidin and hesperetin as inhibitor of acyl coa-cholesterol-o-acyltransferase, inhibitor of macrophage-lipid complex accumulation on the arterial wall and preventive agent

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] In addition, the percentages of solids in solid mixtures, liquids in liquids, and solids in liquids below are calculated in wt / wt, vol / vol, and wt / vol, respectively, and all reactions are carried out at room temperature unless otherwise There are instructions. Embodiment 1: extract hesperidin from orange peel

[0035] The peels of citrus (Cheju Island, Korea), citron (Jeollanamdo, Korea) and orange, grapefruit and lemon (California, CA, USA) were dried at room temperature and then pulverized into powders with a particle size of 100-200 μm. 50 ml of methanol was added to 500 mg of each of the above orange peel powders, followed by extraction in a water bath at 50° C. for 6 hours. The resulting extract was cooled, then filtered, and methanol was added to the filtrate to a volume of 50 ml.

[0036] In order to confirm the content of hesperidin in the extract prepared as above, 0.5 μl of the extract was subjected to high-performance liquid chromatography (HPLC) analysis, ...

Embodiment 3

[0041] Thirty 4-week-old Sprague-Dawley rats (Taihanlaboratory animal center, Korea) weighing 90-110 g were randomly divided into 3 diet groups. Rats in the three groups were fed with three different high-cholesterol diets, namely AIN-76 laboratory animal diet (ICN Biochemicals, Cleveland, OH, USA) containing 1% cholesterol (control group), and 1% cholesterol plus 0.1% hesperidin or hesperetin. The composition of the feed used by the three groups is shown in Table II below.

[0042] feed ingredients

[0043] Rats were fed ad libitum with the specific diet and water for 6 weeks, the intake was recorded daily, then weighed every 7 days, and the recorded data were analyzed. All rats showed normal growth rates, and there were no significant differences in food intake and weight gain among the three groups. Embodiment 4: Determination of total cholesterol, HDL-cholesterol and neutral lipid content in plasma

Embodiment 4

[0044] The effect of administration of hesperidin or hesperetin on plasma cholesterol and neutral lipid levels in rats was determined as follows.

[0045] Blood samples were collected from the rats of the above three groups, and plasma HDL components were separated therefrom using HDL-cholesterol reagent (Sigma Chemical Co., Cat. No. 352-3) containing glucose sulfate. Total cholesterol and HDL-cholesterol concentrations were measured using Sigma Diagnostic Kit Cat. No. 352-100 (Sigma Chemical Co., USA) (Allain et al., Clin. Chem., 20, 470-475 (1974)). The neutral lipid concentration was determined using Sigma Diagnostic Kit Cat. No. 339-50 (Sigma Chemical Co., USA) (Bucolo, G. and David, H., Clin. Chem., 19, 476-482 (1973)). The results are shown in Table III, wherein, compared with the rats in the control group, the total plasma cholesterol concentrations of the rats fed with hesperidin and hesperetin decreased by 32% and 18%, respectively.

[0046] Group

[0047]...

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Abstract

The present invention relates to uses of hesperidin or hesperetin for inhibiting the activity of acyl CoA-cholesterol-o-acyltransferase, inhibiting the accumulation of macrophage-lipid complex on the arterial endothelium, and preventing or treating hepatic diseases in a mammal.

Description

field of invention [0001] The present invention relates to hesperidin and hesperetin inhibiting the activity of acyl CoA-cholesterol-O-acyltransferase (ACAT) in mammals, inhibiting the accumulation of macrophage-lipid complexes on the arterial wall, and preventing or Application in the treatment of liver diseases. Background of the invention [0002] In recent years, coronary cardiovascular circulation diseases, such as atherosclerosis and hypercholesterolemia, have gradually become the main cause of death. It has been reported that elevated plasma cholesterol concentration leads to the deposition of fat, macrophages and foam cells on the vessel wall, and this deposition leads to plaque formation and thus atherosclerosis (Ross, R., Nature, 362 , 801-809 (1993)). One of the methods to reduce plasma cholesterol concentration is diet method to reduce cholesterol and lipid intake. Another approach is to inhibit the absorption of cholesterol by inhibiting the enzymes involved ...

Claims

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Application Information

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IPC IPC(8): A23C9/152A21D13/00A23G3/00A23G3/34A23L1/30A23L2/52A23L2/56A23L13/00A23L27/60A61K31/35A61K31/352A61K31/7048A61K36/00A61P1/16A61P3/06A61P43/00C12G3/00
CPCA23V2002/00A23L2/56A61K36/00A23L1/3002A23L33/105A61P1/16A61P3/06A61P43/00A61K2300/00A23V2250/2116
Inventor 卜成海郑泰淑崔明淑文锡植权容国李恩淑玄柄和崔良圭李哲浩裴基焕朴镛福李准圣孙光熙权炳穆金永国崔度一金成郁黄仁奎安贞娥朴永培金孝洙崔盛俊
Owner KOREA INST OF SCI & TECH
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