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Functionalized nano graphene oxide supported insulin derivative material, preparation method thereof and application in preparation of medicine for treating diabetes

A technology of insulin derivatives and nano-graphite oxide, which is applied in drug combinations, metabolic diseases, and pharmaceutical formulations, can solve undiscovered problems and achieve the effects of simple steps, alleviating physical and mental pain, and inhibiting the aggregation of hIAPP

Inactive Publication Date: 2015-09-23
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, no reports have been found about the use of aminated polyethylene glycol-functionalized nano-graphene oxide-loaded insulin derivatives in inhibiting diabetes

Method used

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  • Functionalized nano graphene oxide supported insulin derivative material, preparation method thereof and application in preparation of medicine for treating diabetes
  • Functionalized nano graphene oxide supported insulin derivative material, preparation method thereof and application in preparation of medicine for treating diabetes
  • Functionalized nano graphene oxide supported insulin derivative material, preparation method thereof and application in preparation of medicine for treating diabetes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] (1) Preparation of nano-graphene oxide

[0038]Adopt conventional Hummers method to prepare graphene oxide, weigh 3g natural graphite powder and 18g potassium permanganate and mix evenly, add concentrated sulfuric acid 360mL and concentrated phosphoric acid 40mL mixed acid (volume ratio 9:1), stir and heat to keep the heating temperature of reactant Reaction between 35 ~ 40 ℃ for 1h. Then the reactant was rapidly heated to 50°C and the reaction was continued for 12h. After the reaction was completed, it was naturally cooled to room temperature. Quickly add 100mL of ice water into the above system, stir for 5min and then dropwise add 4mL of 30% H 2 o 2 The solution turned from black to khaki. Let it stand for 2 hours, pass through a metal standard test screen (W.S.Tyler, 300 μm), centrifuge the filtrate at 15,000 rpm for 30 minutes, discard the supernatant, and wash the lower layer of solid matter twice with 200 mL of water, 200 mL of 30% HCl and 200 mL of ethanol ,...

Embodiment 2

[0044] (1) the preparation of nanometer graphene oxide is the same as embodiment 1;

[0045] (2) the preparation of aminated polyethylene glycol functionalized nano-graphene oxide is the same as in Example 1;

[0046] (3) Preparation of Aminated Polyethylene Glycol Functionalized Nano Graphene Oxide Loaded Insulin Derivative Materials

[0047] 10 mg of nGOPEG prepared in step (2) was weighed and dissolved in 10 mL of PBS to prepare a 1 mg / mL solution. Dissolve 2 mg of insulin-derived short peptide EALYLV (relative molecular weight: 707) with 1 mL of PBS, and divide 1 mL of the solution into 5 parts, each with a concentration of 2.83×10 -3 mol / L as a stock solution. Ultrasonic disperse 10mL of nGOPEG solution at 570W for 10min, then add 20mg EDC·HCl and 40mg NHS to maintain the pH value of the solution at about 7, then add 400μM EALYLV stock solution with a rubber dropper, and stir the reaction at 25°C for 2h . After the reaction was completed, centrifuge at 6000 rpm for 30...

Embodiment 3

[0049] (1) the preparation of nanometer graphene oxide is the same as embodiment 1;

[0050] (2) the preparation of aminated polyethylene glycol functionalized nano-graphene oxide is the same as in Example 1;

[0051] (3) Preparation of Aminated Polyethylene Glycol Functionalized Nano Graphene Oxide Loaded Insulin Derivative Materials

[0052] 20 mg of nGOPEG prepared in step (2) was weighed and dissolved in 10 mL of PBS to prepare a 1 mg / mL solution. Dissolve 2 mg of insulin-derived short peptide EALYLV (relative molecular weight: 707) with 1 mL of PBS, and divide 1 mL of the solution into 5 parts, each with a concentration of 1.83×10 -3 mol / L as a stock solution. Ultrasonic disperse 10mL of nGOPEG solution at 300W for 10min, then add 40mg EDC·HCl and 80mg NHS to maintain the pH value of the solution at about 7, then add 400μM EALYLV stock solution with a rubber dropper, and stir the reaction at 25°C for 2h . After the reaction was completed, centrifuge at 6000 rpm for 30...

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Abstract

The invention belongs to the technical field of preparation of medicine for treating diabetes, and discloses an amino polyethylene glycol functionalized nano graphene oxide supported insulin derivative material, a preparation method thereof and application thereof in preparation of the medicine for treating diabetes mellitus type 2. The material is prepared through the method including the following steps: adding amino polyethylene glycol into a graphene oxide solution, then adding 1-ethyl-(3-dimethyl aminopropyl) carbonyl diimine hydrochloride and N-hydroxysuccinimide, adjusting the pH, stirring while reacting, and separating in a centrifugal manner, so as to obtain amino polyethylene glycol modified nano graphene oxide; dispersing amino polyethylene glycol modified nano graphene oxide into a solution, adding 1-ethyl-(3-dimethyl aminopropyl) carbonyl diimine hydrochloride and N-hydroxysuccinimide, dropwise adding an insulin derivative, and stirring while reacting, so as to obtain the amino polyethylene glycol functionalized nano graphene oxide supported insulin derivative material. The material provided by the invention can significantly inhibit human pancreas islet amyloid protein aggregation.

Description

technical field [0001] The invention belongs to the technical field of preparing drugs for treating diabetes, and in particular relates to an aminated polyethylene glycol functionalized nano-graphene oxide-loaded insulin derivative material (nGOPEGEALYLV, nGOPEGE for short) and a preparation method thereof and a method for preparing a drug for treating type 2 diabetes in the application. Background technique [0002] Diabetes mellitus (DM) is an endocrine and metabolic disease characterized by elevated blood sugar, which is caused by multiple pathogenic factors such as genetic factors, environmental factors, and behavior. Diabetes has become a worldwide public health problem in the 21st century. Insulin is currently an effective drug for the treatment of diabetes, but it can only temporarily alleviate the patient's blood sugar elevation through injection. Long-term injection will not only have a serious impact on the patient's body and mind, but will also bring a heavy econ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K38/28A61K47/10A61P3/10
Inventor 刘杰周贤波俆桃远
Owner JINAN UNIVERSITY
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