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Dipeptide TE with dual functions of lowering blood pressure and lowering blood fat and application thereof

A lipid-lowering, dual-function technology applied in the field of active dipeptides

Active Publication Date: 2014-04-23
创客商盟有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] According to existing drug reports, except for traditional Chinese medicines, drugs that have both blood pressure and blood fat lowering effects are rare

Method used

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  • Dipeptide TE with dual functions of lowering blood pressure and lowering blood fat and application thereof
  • Dipeptide TE with dual functions of lowering blood pressure and lowering blood fat and application thereof
  • Dipeptide TE with dual functions of lowering blood pressure and lowering blood fat and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] 1) ACE inhibitory activity of dipeptide TE at a concentration of 1.0 mg / mL:

[0059] Chromatographic conditions: Solvent I is 0.05% trifluoroacetic acid (TFA) and 0.05% triethylamine (TTA) dissolved in deionized water (that is, every liter of solvent I contains 0.5mL of trifluoroacetic acid and 0.5mL of triethylamine ), solvent II is 100% chromatographically pure acetonitrile. The ratio of solvent Ⅰ to solvent Ⅱ is 70%: 30% (volume ratio), ultimate3000 Diane liquid chromatograph, and the chromatographic column is waters Symmetry C 18 5μm 4.6×250mm, the flow rate is 0.5mL / min, the injection volume is 10μL, the detection wavelength is 225nm, and the detection column temperature is 30°C.

[0060] Detection method: The dipeptide TE obtained by chemical synthesis is tested for activity (the detection method is the same as above). At this time, the TE concentration was 1.0 mg / mL.

[0061] Results: The ACE inhibitory activity of dipeptide TE was 85.86% at 1.0 mg / mL.

[00...

Embodiment 2

[0067] 1) ACE inhibitory activity of dipeptide TE at a concentration of 2.0 mg / mL:

[0068] Chromatographic conditions: solvent Ⅰ is 0.05% trifluoroacetic acid (TFA) and 0.05% triethylamine (TTA) dissolved in deionized water; solvent Ⅱ is 100% chromatographically pure acetonitrile. The ratio of solvent Ⅰ to solvent Ⅱ is 70%: 30%, the ultimate3000 Diane liquid chromatograph, the chromatographic column is waters Symmetry C 18 5μm 4.6×250mm, the flow rate is 0.5mL / min, the injection volume is 10μL, the detection wavelength is 225nm, and the detection column temperature is 30°C.

[0069] Detection method: The dipeptide TE obtained by chemical synthesis is tested for activity (the detection method is the same as above). At this time, the TE concentration was 2.0 mg / mL.

[0070] Results: The ACE inhibitory activity of dipeptide TE at 2.0 mg / mL was 97.51%.

[0071] 2) HMG-CoA reductase inhibitory activity of dipeptide TE at a concentration of 2.0 mg / mL:

[0072] Chromatographic ...

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Abstract

The invention belongs to the field of biotechnologies, particularly relates to a dipeptide which can be combined with angiotensin converting enzyme (ACE), can inhibit the activity of ACE and can inhibit the activity of 3-hydroxyl-3-methyl-glutaryl coenzyme A (HMG-CoA) reductase, and specifically discloses a dipeptide TE with dual functions of lowering blood pressure and lowering blood fat. The amino acid sequence of the dipeptide TE is Thr-Glu. The invention further simultaneously provides application of the dipeptide TE in the preparation of ACE inhibition peptides and / or HMG-CoA reductase inhibition peptides.

Description

technical field [0001] The invention belongs to the field of biotechnology, and particularly relates to an angiotensin-converting enzyme that can bind to angiotensin-converting enzyme, inhibit its activity, and can also inhibit the activity of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase of dipeptides. Background technique [0002] Angiotensin converting enzyme (Angiotensin converting enzyme, ACE, EC3.4.15.1, once used in the literature as kininaseIl, dipeptidyl carboxypeptidase I, etc.) is a dicarboxypeptidase, which is a key enzyme leading to high blood pressure. It passes Hydrolysis converts angiotensin I to angiotensin II, and at the same time, ACE can also inactivate bradykinin, both of which can lead to vasoconstriction and thus hypertension. Therefore, ACE is considered to be an important factor causing hypertension. Studies have found that angiotensin-converting enzyme inhibitors (ACEI) can lower blood pressure by inhibiting the activity of ACE. ACE i...

Claims

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Application Information

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IPC IPC(8): C07K5/062A61K38/05A61P9/12A61P3/06
Inventor 王楠王伟张玉杨玉英
Owner 创客商盟有限公司
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