Compsn. contg. cinnamic acid derivatives for preventing or treating elevated blood lipid level-releated diseases
A technology of cinnamic acid derivatives and compositions, which can be used in drug combinations, cardiovascular system diseases, medical preparations containing active ingredients, etc., and can solve problems such as expensive drugs and adverse side effects of the central nervous system
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Embodiment 1
[0033] Further, the percentages given below for solids in solid mixtures, for liquids in liquids, and for solids in liquids are based on wt / wt, vol / vol, and wt / vol respectively, and unless otherwise stated, all reactions are at room temperature next. Example 1: Toxicity of Oral Administration of 4-Hydroxycinnamic Acid
[0034] Twelve 7-week-old specific pathogen-free ICR female mice, including 6 female mice weighing about 25-29 g and 6 male mice weighing about 34-38 g, were kept at an ambient temperature of 22±1°C , relative humidity 55±5% and photoperiod 12L / 12D. Feed (Cheiljedang Co., rat and rabbit feed) and water were sterilized and fed to the mice.
[0035] 4-Hydroxycinnamic acid commercially available from Aldrich-Sigma Chemical Co. (St.Louis, MO, U.S.A) was dissolved in 0.5% Tween 80 to a concentration of 100 mg / ml, and then the solution was orally administered in small Rats, the dosage is 0.2ml / 20 g mouse body weight. The solution was administered once to the mice,...
Embodiment 2
[0037] diet group
[0038] During 6 weeks, the rats were allowed to eat the prescribed food and water freely, the daily intake was recorded, and the rats were weighed every 7 days, and then the records were analyzed. All rats showed normal growth rates, and there were no significant differences among the four groups in terms of food intake and weight gain. Step 2: Determination of Total Cholesterol, HDL-Cholesterol, and Neutral Lipids in Blood
[0039] The effects of administration of cinnamic acid derivatives to rats on plasma cholesterol and neutral lipid levels were measured as follows.
[0040] Group
[0041] It can be seen from Table II that compared with the control group, the total plasma cholesterol levels in the 4-hydroxycinnamic acid, 3,4-dihydroxycinnamic acid and 3,4-dihydroxyhydrocinnamic acid groups were reduced by 24%, 13% and 6%. In addition, compared with the control group, the HDL-C / TC ratio in the 4-hydroxycinnamic acid, 3,4-dihydroxyc...
Embodiment 3
[0042] To determine the effect of feeding cinnamic acid derivatives on ACAT activity in rats, microsomes were isolated from ready-to-use liver tissue as the source of the enzyme.
[0043] Each 1g of liver from each group of rats in Example 2 was mixed in 5ml of homogenization medium (0.1MKH 2 PO 4 , pH7.4, 0.1mM EDTA and 10mM β-mercaptoethanol) homogenized. The homogenate was centrifuged at 3,000×g and 4°C for 15 minutes, and the obtained supernatant was centrifuged at 15,000×g and 4°C for 15 minutes to obtain a supernatant. The supernatant was placed in an ultracentrifuge tube (Beckman) and centrifuged at 100,000 × g at 4 °C to obtain a microsomal pellet, which was then suspended in 3 ml of homogenization medium and incubated at 100,000 × g and 4°C for 1 hour. The obtained precipitate was suspended in 1 ml of homogenization medium. The protein concentration in the resulting suspension was measured by Lowry's method and then adjusted to 4-8 mg / ml. The resulting suspension...
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