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.
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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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