Angiotensin converting enzyme inhibitory peptide milky white peptide C1 and application thereof

An angiotensin and converting enzyme technology, applied in the field of pharmacology, can solve the problems of reduced activity and loss of analog activity, and achieve the effects of long half-life, easy operation and less side effects

Inactive Publication Date: 2014-07-16
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If a dipeptide is extended from the N-terminal, the inhibitory activity of the corresponding tripeptide is usually enhanced, but if it continues to be extended, the activity will decrease; ②The C-terminal contains phenylalanine, proline, tryptophan, and tyrosine. Peptide or dipeptide, the activity is relatively high; ③The N-terminal is hydrophobic branched-chain amino acids such as valine and isoleucine, the activity is relatively high, while the N-terminal is proline, the activity is reduced; ④There is lysine on the C-terminal residue Acid or arginine, the inhibitory activity of the peptide can be improved, and the positive charge on the guanidine or ε-amino group on the lysine or arginine side chain plays an important role, and the substitution of the C-terminal arginine residue will cause Substantial loss of activity of its analogs

Method used

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  • Angiotensin converting enzyme inhibitory peptide milky white peptide C1 and application thereof
  • Angiotensin converting enzyme inhibitory peptide milky white peptide C1 and application thereof
  • Angiotensin converting enzyme inhibitory peptide milky white peptide C1 and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Synthesis of angiotensin-converting enzyme inhibitory peptide LAP-C1: angiotensin-converting enzyme inhibitory peptide LAP-C1 was synthesized by a solid-phase synthesizer, identified by a mass spectrometer, see the simple diagram figure 1 .

[0021] (1) Synthetic raw materials and related reagents:

[0022] 1).FMOC-Tyr-OH (FMOC-Tyr-OH), FMOC-Thr-OH, FMOC-Asn-OH, FMOC-Pro-OH, FMOC-Lys-OH, FMOC-Leu-OH, FMOC- Phe-OH, FOMC-Asp-OH, FMOC-Met-OH, FMOC-Arg-OH, etc. (Gill Biochemical (Shanghai) Co., Ltd.)

[0023] 2). Benzotriazole-N, N, N', N'-tetramethyluronium hexafluorophosphate (HBTU) (Gill Biochemical (Shanghai) Co., Ltd.)

[0024] 3).NMM (Sinopharm Group Shanghai Chemical Reagent Company)

[0025] 4). Dimethylformamide (DMF) (Dikma company)

[0026] 5).DCM (Dikma Company)

[0027] 6). Acetonitrile (Fisher company)

[0028] 7).FMOC-Tyr-Wang-Resin (FMOC-Tyr-Wang-Resin) (Gill Biochemical (Shanghai) Co., Ltd.)

[0029] 8). Piperidine (Sinopharm Shanghai Chemical Reagen...

Embodiment 2

[0049] IC50 value of LAP-C1 inhibiting ACE activity in vitro

[0050]The activity of LAP-C1 in inhibiting angiotensin-converting enzyme was determined by direct injection and isocratic elution using a high-pressure liquid chromatography analyzer. Results In the analysis of the control group a (LAP-C1 was replaced by buffer), the concentration (1.523mmol / L) of the substrate hippuryl histidyl leucine (SIGMA H1635) (HHL) before the injection was higher than that of the HHL standard (0.29mmol / L) nearly 5 times higher, figure 2 It is Hip 0.112mmol / L and HHL 0.29mmol / L standard spectrum. image 3 Control group a: 50ul ACE + 10ul buffer + 200ul HHL (1.523mmol / L) + 250HCL, angiotensin converting enzyme activity map. image 3 The peak area of ​​the peak at 17.743 minutes and figure 2 about 1.8 times higher than figure 2 The peak area of ​​the peak at 6.43 minutes and image 3 It is about 2.9 times higher than the comprehensive figure 2 , image 3 The results shown suggest th...

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PUM

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Abstract

The invention belongs to the technical field of pharmacology and particularly discloses an angiotensin converting enzyme inhibitory peptide milky white peptide C1 with pressure lowering effect and an application thereof. The amino acid sequence of the angiotensin converting enzyme inhibitory peptide LAP-C1 is Leu-Arg-Pro-Val-Ala-Ala-Pro, the activity IC for inhibiting angiotensin converting enzymes in vitro is 50-18.06 muM, and the inhibitory peptide has an effect of lowering pressure and can be used as a medicament for treating and preventing hypertension. The angiotensin converting enzyme inhibitory peptide LAP-C1 has stronger effect of lowering pressure and long half-life period. The administration times of a patient can be reduced, the obedience of the patient is improved, and medical fees are saved.

Description

technical field [0001] The invention belongs to the technical field of pharmacology, and relates to an angiotensin-converting enzyme inhibitory peptide lactalbumin C1 (LAP-C1) with antihypertensive effect and application thereof. Background technique [0002] Hypertension is one of the most common cardiovascular diseases. Controlling the development of hypertension can help reduce the risk of cardiovascular system diseases. In this etiology, the renin-angiotensin booster enzyme system is one of the most important factors in the pathogenesis of hypertension. At present, there are many chemicals acting on this link. Although the curative effect is good, they all have different degrees of toxic and side effects. In recent years, angiotensin-converting enzyme inhibitory peptide derived from natural food protein has attracted much attention because of its non-toxic side effects and is expected to become an ideal choice for controlling the course of hypertension, and is becoming ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06
Inventor 罗明方宏
Owner TONGJI UNIV
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