Anti-platelet aggregation peptide and application thereof

A technology of platelet aggregation and polypeptides, which is applied in the field of medicine and chemical industry, can solve the problems of degradation and stable existence for a long time, and achieve strong activity and strong anti-platelet aggregation effect

Active Publication Date: 2011-04-20
JIANGSU CAREFREE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The self-assembled short peptides of D-type amino acids generally cannot be degraded by L-type enzymes (Luo Z., Zhao X., Zhang S.Macromol.Biosci.[J], 2008, 8(8):785-791), stable in vivo relatively long time

Method used

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  • Anti-platelet aggregation peptide and application thereof
  • Anti-platelet aggregation peptide and application thereof

Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment 1

[0048] Specific Example 1 Synthesis of (D) Pyr-(L) Asn-(L) Trp

[0049] (1) Activation of resin

[0050] Weigh 1.01g of 2-chlorotrityl chloride resin into a small beaker, add DMF to swell for 30 minutes, pour out half the volume of DMF, add an equal volume of DCM to swell for 30 minutes, pour it into a sand funnel, and then suck it dry. Preparation of deprotection solution during activation: Take 6ml of piperidine (Pip) and pour it into a brown bottle, then add 24ml of DMF, mix and place.

[0051] (2), preparation of Fmoc-(L)Trp(Boc)-resin

[0052] Weigh Fmoc-(L)Trp(Boc)-OH 1.74g and dissolve with DMF, after the dissolution is complete. After the reaction device was connected, the nitrogen was blown, and the DMF solution of Fmoc-Trp(Boc)-OH was added to the resin-containing sand funnel, and then 1.2ml of DIEA was added, and the reaction was carried out at room temperature for 2 hours.

[0053] (3), deprotection

[0054] After the reaction, the resin was filtered to dryness...

Embodiment 2

[0071] Example 2 Synthesis of (D)Pyr-(L)Trp-(D)Asn

[0072] Using Fmoc-(D)Asn(Trt)-OH, Fmoc-(L)Trp(Boc)- and (D)Pyr as raw materials according to the method of Example 1, synthesize (D)Pyr-(L)Trp-(D) ) Asn.

Embodiment 3

[0073] Example 3 Synthesis of (D)Pyr-(D)Trp-(L)Asn

[0074] Using Fmoc-(L)Asn(Trt)-OH, Fmoc-(D)Trp(Boc)- and (D)Pyr as raw materials according to the method of Example 1, synthesized to obtain (D)Pyr-(D)Trp-(L ) Asn.

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Abstract

The invention provides an anti-platelet aggregation optically active polypeptide compound. The compound consists of three amino acids, namely levorotatory or dextrorotatory tryptophan, asparagine and pyroglutamic acid, and is used for treating platelet aggregation-related heart cerebrovascular diseases, such as ischemic stroke, inflammation, asthma and the like.

Description

[0001] The invention relates to a polypeptide substance with optical activity and its application in cardiovascular and cerebrovascular, belonging to the field of medicine and chemical industry. Background technique [0002] Platelets have a specific morphological structure and biochemical composition, and have a relatively constant number in normal blood (for example, the number of platelets in humans is 100,000 to 300,000 per cubic millimeter). The main function of platelets is to promote hemostasis and accelerate coagulation. The function of maintaining the integrity of capillary walls. Hyperplatelet aggregation is a very important factor in causing and aggravating myocardial ischemia. Platelets are activated to aggregate. In addition to participating in thrombus formation, the increase of TXA2 level during aggregation can also cause coronary artery spasm, cause microthrombus, form myocardial microvascular blockage, and obstruct myocardial microcirculation. Diseases with i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/097A61K38/06A61P9/10A61P11/06A61P29/00
Inventor 秦引林孔毅
Owner JIANGSU CAREFREE PHARM CO LTD
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