Use of alpha-amylase inribitor in medicine for preventing and treating hyper lipermia and athereosclerosis

An amylase inhibitor and atherosclerosis technology, which is applied in the field of application of α-amylase inhibitors in the preparation of drugs for the prevention and treatment of hyperlipidemia and atherosclerosis, can solve the problem of lowering total blood cholesterol, coronary heart disease Unsatisfactory prevention and treatment of heart disease, obvious adverse drug reactions and other problems, to achieve good tolerance

Inactive Publication Date: 2006-08-09
NANJING TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

(4) Phenoxy acids: Clofibrate (clofibrate (clofibrate) was first used. Although it has a certain effect on blood lipid regulation, the effect on the prevention and treatment of coronary heart disease is not ideal, and the adverse drug reactions are obvious, and even increase the mortality rate.
(5) Polyunsaturated fatty acids: present in a variety of vegetable oils, but their blood lipid-regulating and anti-atherogenic effects are not certain, and they are only used for adjuvant therapy
The lipid-regulating effect of this type of drug is mainly to reduce blood triglycerides, and its clinical anti-atherogenic effect needs further large-scale research
(7) Other lipid-lowering drugs: Probucol (probucol) can lower blood total cholesterol and blood triglycerides, but the disadvantage is that it can also lower high-density lipoprotein cholesterol
[0008] The α-amylase inhibitor extracted from natural plants by the School of Pharmacy and Life Sciences of Nanjing University of Technology using a two-phase extraction system (see the publication number CN1597944A for details, the application number is 200410041455.4, and the name is "A two-phase extraction system and The method of using this system to separate and purify α-amylase inhibitors"), compared with the current clinical similar drugs, has the advantages of pure natural, non-toxic, less side effects, good tolerance, suitable for long-term use by patients, etc., but this The patent does not disclose the application of the extracted α-amylase inhibitor in the prevention and treatment of hyperlipidemia and atherosclerosis. The present invention conducts further research on this basis

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Effect of α-amylase inhibitors on prevention of hyperlipidemia

[0023] 50 male SD rats were randomly divided into 5 groups, 10 in each group. Normal control group: fed with normal feed; high-fat model group: fed with high-fat feed; α-amylase inhibitor low, medium, and high dose groups: rats fed with high-fat feed were gavaged with α-amylase inhibition Dosage 25, 50, 100mg / kg, continuous administration for 9 weeks. After 6 weeks and 9 weeks of administration, the rats were fasted for 12 hours, blood was taken from the orbit of the rats, and the contents of TC, TG, HDL-C and LDL-C were measured with a kit, and according to AI=(TC-HDL -C) / HDL-C, to calculate the atherosclerosis index. The results are shown in Table 1 and Table 2.

[0024] group

dosage

(mg / kg)

TC

(mmol / L)

TG

(mmol / L)

HDL-C

(mmol / L)

LDL-C

(mmol / L)

AI

normal group

1.77±0.12

1.40±0.03

1.06±0.055

1.57±...

Embodiment 2

[0031] Example 2: Anti-atherosclerotic effect of α-amylase inhibitors

[0032] After 63 days of administration according to the administration method of Example 1 (i.e. after the last administration), the MDA concentration and SOD activity in rat serum and liver were measured, and hemorheology examination was performed simultaneously. In addition, cut out the aortic arch, stained with HE, and observed the atherosclerotic lesion with light microscope. the result shows:

[0033] (1) The high-dose group of α-amylase inhibitors can significantly reduce rat serum and liver MDA, and significantly increase SOD activity (p<0.05), indicating that α-amylase inhibitors have a certain antioxidant capacity (results see table 3).

[0034] group

dosage

(mg / kg)

serum

the liver

MDA

(μmol / L)

SOD

(NU / mL)

MDA

(μmol / L)

SOD

(NU / mg)

normal group

6.95±0.12

145.5±6.6

5.29±0.15

7.26±0.11

High ...

Embodiment 3

[0040] Example 3: Effects of α-amylase inhibitors on blood lipid regulation

[0041] 50 high-fat rats were divided into: high-fat model group, positive control group (evening primrose oil 2.5mg / kg), α-amylase inhibitor low, medium and high dose groups (25,50,100mg / kg ). The positive control group and the α-amylase inhibitor low, medium and high dose groups were administered once a day for 3 consecutive weeks. Serum TC, TG, HDL-C, LDL-C concentrations, liver fat (TC, TG) and liver weight were measured, and liver weight / body weight was calculated. The results are shown in Table 5 and Table 6.

[0042] (1) Effects on serum lipids:

[0043] group

dosage

(mg / kg)

TC

(mmol / L)

TG

(mmol / L)

HDL-C

(mmol / L)

LDL-C

(mmol / L)

normal group

2.35±0.06

1.35+0.06

1.39±0.17

1.27±0.079

High fat model group

6.01±0.14#

2.11±010#

0.58±0.057

5.63±0.44#

positive control grou...

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PUM

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Abstract

The invention discloses the application of an alpha-amylase inhibitor in preparing a medicine for preventing and curing hyperlipidemia and atherosclerosis, where the medicine can prevent and cure hyperlipidemia and atherosclerosis, safe, nontoxic, having good endurance and especially suitable to be applied long term.

Description

technical field [0001] The present invention relates to the application of alpha-amylase inhibitor, in particular to the application of the alpha-amylase inhibitor extracted from natural plants in the preparation of drugs for preventing and treating hyperlipidemia and atherosclerosis. Background technique [0002] Hyperlipidemia is a general term for hypercholesterolemia and hypertriglyceridemia. Blood lipids take cholesteryl ester (CE) and triglyceride (TG) as the core, outsourcing cholesterol (CH) and phospholipid (PL) to form spherical particles, and then combine with apolipoprotein (Apo) to form lipoprotein (LP) dissolved in Plasma for transport and metabolism. LP can be divided into chylomicrons (CM), very low density lipoprotein (VLDL), intermediate density lipoprotein (IDL), low density lipoprotein (LDL) and high density lipoprotein (HDL). Blood lipids or LP often exceed the normal limit, that is, total cholesterol (TC), TG, and LDL cholesterol (LDL-C) are higher th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/899A61K38/56A61P3/06
Inventor 应汉杰欧阳平凯张琪
Owner NANJING TECH UNIV
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