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Polypeptide carrying melittin, nano-particles carrying melittin, and applications thereof

A nanoparticle, melittin technology, applied in the fields of biological science and drug carriers, can solve the problems of difficult to achieve therapeutic effect, difficult to effectively spread tumors, environmental damage, etc., achieve excellent physical and chemical properties, facilitate large-scale production, avoid The effect of direct contact

Inactive Publication Date: 2013-05-01
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this type of PFC particle size is relatively large, between 200-300nm, and cannot pass through the gaps (20-40nm) of dense network collagen fibers in solid tumors, and it is difficult to effectively diffuse into the interior of the tumor, especially for blood vessels. Abundant solid tumors, it is difficult to achieve the expected therapeutic effect
Moreover, the metabolism, excretion and biological toxicity of PFC particles in the human body need further experimental verification; in addition, as a greenhouse gas material, the extensive application of perfluorocarbons will also bring environmental damage

Method used

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  • Polypeptide carrying melittin, nano-particles carrying melittin, and applications thereof
  • Polypeptide carrying melittin, nano-particles carrying melittin, and applications thereof
  • Polypeptide carrying melittin, nano-particles carrying melittin, and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The polypeptide carrying melittin is composed of α-helical polypeptide, connecting sequence and melittin connected in series in the form of covalent bonds. The amino acid sequence of the α-helical polypeptide in this example is: DWFKAFYDKVAEKFKEAF, the amino acid sequence of the connecting sequence is GSG, and the amino acid sequence of melittin is: GIGAVLKVLTTGLPALISWIKRKRQQ. The amino acid sequence of the melittin-carrying polypeptide is described in SEQ ID NO.1 in the sequence listing.

[0037] Preparation of nanoparticles carrying melittin, the steps are:

[0038] 1) Add 3 μmol DMPC

[0039](1,2-dimyristoyl-sn-glycero-3-phosphocholine), 0.2 μmol cholesterol ester (Cholesteryl oleate, referred to as C.O) in chloroform solution is fully mixed in a glass test tube, and the test tube mouth is sealed with a sealing film;

[0040] 2) Dry the chloroform in the test tube in a steady nitrogen flow, so that the mixture in step 1) can form a thin film at the bottom of the te...

Embodiment 2

[0050] The comparison between the nanoparticles carrying melittin prepared in Example 1 and free melittin for hemolytic performance can be found in Figure 8 . Figure 8 showed that the hemolysis rate of nanoparticles loaded with melittin did not reach 10% when the concentration of melittin reached 60 μM, while the free melittin was close to 100% at 1 μM. It is proved that the nanoparticles carrying melittin can effectively reduce the hemolytic performance of melittin, and will not destroy red blood cells after intravenous injection, which provides a basis for its application in living treatment.

[0051] Comparison of melittin-loaded nanoparticles and free melittin in terms of cell killing ability Figure 9 . pass Figure 9 Compared with the cell proliferation experiment, it can be seen that the nanoparticles carrying melittin can reduce the damage of melittin to cells, and then can protect the normal cells of the body from damage during the application process in vivo, ef...

Embodiment 3

[0053] The nanoparticles carrying melittin prepared in Example 1 treat tumor models in vivo:

[0054] A B16 subcutaneous tumor model was constructed. Digest B16 cells, wash twice with sterilized PBS, then count the cells, and finally set the cell concentration to 8×10 6 a / L. C57BL / 6 mice were anesthetized, and the tumor cell solution was injected subcutaneously at the root of the mouse's left leg with an injection volume of 100 μl. The inoculation date was set as the 0th day, and the subsequent dates were respectively recorded as the 1st, 2nd, 3rd... days. On the 4th day, the rats were stratified and randomly grouped according to the needs, and the recommended number of each group was not less than 5.

[0055] Tail vein injections were started on day 5. Before injection, mark each mouse, weigh the weight of each mouse, and record it in a pre-established form.

[0056] In the Control group, only sterilized PBS was injected into the tail vein, and the injection volume was 0...

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Abstract

The invention discloses a polypeptide carrying melittin, nano-particles carrying melittin, and applications thereof. The invention belongs to the field of biological science and drug carriers. The peptide is composed of alpha helical polypeptide, connection sequence, and melittin which are connected in series with a covalent bond form. The nano-particles are formed through three effective bonding manners of polypeptides, phospholipids, and cholesterol esters carrying melittin. With the nano-particles prepared from the polypeptide carrying melittin, toxic and side effects of melittin against bodies can be effectively reduced, and effects can be performed specifically at diseased areas such as tumors. The nano-particles can be used in clinical treatments.

Description

technical field [0001] The invention belongs to the fields of biological sciences and drug carriers, and in particular relates to a polypeptide carrying melittin, nanoparticles carrying melittin and applications thereof. Background technique [0002] Melittin (GIGAVLKVLTTGLPALISWIKRKRQQ) is an amphipathic α-helical polypeptide, which is the main active ingredient in bee venom, accounting for 40%-60% of its dry weight. Melittin has high activity, has broad-spectrum antibacterial function, can play its role in a very short time, and its efficiency is hundreds of times that of ordinary antibiotics. Melittin is highly destructive to cell membrane structures, including plasma membranes and membrane structures of some intracellular organelles. Its mechanism of action is mainly to embed into the membrane structure through its amphiphilic structure, and then punch holes in the membrane, causing the membrane structure to rupture, and the changes in the internal and external environm...

Claims

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Application Information

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IPC IPC(8): C07K19/00A61K9/14A61K38/10A61K47/48A61P35/00
CPCC07K14/435C07K2319/00C07K19/00A61K9/16C07K14/43572A61K9/127A61K9/51A61K47/62A61P35/00
Inventor 骆清铭张智红黄川
Owner HUAZHONG UNIV OF SCI & TECH
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