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Antitumor nanometer medicine and preparation method thereof

A nano-drug, anti-tumor technology, applied in the field of medicine, to achieve good tumor suppression effect

Active Publication Date: 2020-02-07
江苏恒泰生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Surgical treatment has strong limitations depending on the physique of the patient and postoperative recovery problems.

Method used

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  • Antitumor nanometer medicine and preparation method thereof
  • Antitumor nanometer medicine and preparation method thereof
  • Antitumor nanometer medicine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Such as figure 1 As shown, the first aspect of the present invention is a preparation method of anti-tumor nano-medicine, which specifically includes the following steps: using Fmoc-solid-phase synthesis method to introduce CRB into the capping of short peptide X-YpYY, and synthesize short peptide CRB-YpYY;

[0033] Using the method of polypeptide self-assembly, add PBS solution to the short peptide CRB-YpYY, and use carbonate solution to adjust the pH to 7.0~8.0; after that, add 1U / mL~3U / mL alkaline phosphatase to catalyze it Store overnight under the condition of ℃~6℃ to obtain the anti-tumor nano-medicine.

[0034] It should be noted that the Fmoc-solid-phase synthesis method is used to introduce CRB at the end of the short peptide X-YpYY, and the synthesis of the short peptide CRB-YpYY includes: introducing the short peptide X-YpYY at the second phosphorylation site into the CRB, to synthesize the short peptide CRB-YpYY

[0035] Specifically, the first step: using...

Embodiment 2

[0079] The reference compound CRB-pYYY(pY1) was synthesized according to the preparation method in Example 1, and the specific steps will not be repeated, and reference is made to the above description.

[0080] The first step, synthetic reference compound CRB-pYYY (pY1) with Fmoc-solid-phase synthesis method, structural formula is as follows:

[0081]

[0082] The characterization data for this structure are as follows:

[0083]1H NMR (300MHz, DMSO) δ7.16 (d, J = 8.4Hz, 1H), 7.09–6.83 (m, 4H), 6.58 (dd, J = 12.2, 5.8Hz, 3H), 4.40 (s, 2H) ,2.98(s,1H),2.82(d,J=27.4Hz,2H),2.66(s,1H),2.26(s,1H),1.97(s,1H),1.56(s,1H).

[0084] In the second step, take 5mg of the short peptide CRB-pYYY and place it in a 4mL glass bottle, then add PBS solution (pH=7.4) to make up to a total volume of 1mL, and adjust the pH value to 7.4 with 1M sodium carbonate solution. Mix well and sonicate at room temperature to dissolve completely, add 1U / mL alkaline phosphatase and store at 4°C overnight to...

Embodiment 3

[0088] The reference compound CRB-YYpY(pY3) was synthesized according to the preparation method of Example 1, the specific steps will not be described in detail, refer to the above description.

[0089] The specific structural formula is as follows:

[0090]

[0091] The characterization data for this structure are as follows:

[0092] 1 H NMR (300MHz, DMSO) δ7.16 (d, J = 8.4Hz, 1H), 7.09–6.83 (m, 4H), 6.58 (dd, J = 12.2, 5.8Hz, 3H), 4.40 (s, 2H) ,2.98(s,1H),2.82(d,J=27.4Hz,2H),2.66(s,1H),2.26(s,1H),1.97(s,1H),1.56(s,1H).

[0093] In the second step, take 5mg of the short peptide CRB-YYpY and place it in a 4mL glass bottle, then add PBS solution (pH=7.4) to make up to a total volume of 1mL, and adjust the pH value to 7.4 with 1M sodium carbonate solution. Mix well and sonicate at room temperature to dissolve completely, add 1U / mL alkaline phosphatase and store at 4°C overnight to obtain a nanostructure drug self-assembled by the polypeptide at the third phosphorylation s...

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Abstract

The invention provides an antitumor nanometer medicine and a preparation method thereof. The preparation method comprises preparation steps of synthesizing short chain polypeptide CRB-YpYY by an Fmoc-solid phase synthesis method; adding a PBS solution to the short chain polypeptide CRB-YpYY by a polypeptide self-assembly method, and adjusting pH to be 7.0-8.0 with a carbonate solution; and then adding 1U / mL-3U / mL alkaline phosphatase, performing catalysis, performing placing under the condition of 2-6 DEG C, and performing staying overnight for storage so as to obtain the antitumor nanometermedicine. The nanometer medicine is gel, and besides, the pattern of the nanometer medicine under an electron microscope is fibrous. Through comparing short chain polypeptides at different phosphorylation sites and using a clinical antitumor medicine chlorambucil (CRB) as an end sealing base group, different precursor molecules can form nanometer medicines having different patterns under the catalysis effect of the alkaline phosphatase (ALP), and only nanometer fibers formed through catalysis of the short chain polypeptide (pY2) at the second phosphorylation site have better antitumor effects,and show better cancer cell restraining effects at in vitro experiment.

Description

technical field [0001] The invention relates to a medicine, in particular to an anti-tumor nano-medicine and a preparation method of the anti-tumor medicine. Background technique [0002] Cancer is one of the major diseases that threaten human health and development, and its incidence is still increasing rapidly around the world. In addition to the impact on human health, cancer also poses a great threat to the world economy and security. At present, the situation of cancer prevention and control in my country is still very severe, with about 3.1 million new cancer cases and 2.5 million deaths every year. In the past 20 years, the incidence of cancer in my country has been increasing year by year, and the incidence of lung cancer, breast cancer, liver cancer, colon cancer, gastric cancer, esophageal cancer, and cervical cancer in my country will continue to rise. Therefore, it has become urgent to explore and develop more powerful cancer treatment methods to curb the occur...

Claims

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Application Information

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IPC IPC(8): A61K47/64A61K31/196A61P35/00C07K5/02C07K1/04C07K1/06
CPCA61K47/64A61K31/196A61P35/00C07K5/02Y02P20/55
Inventor 杨志谋梁春惠
Owner 江苏恒泰生物科技有限公司
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