Unlock instant, AI-driven research and patent intelligence for your innovation.
Preparation method of Hainantoxin-III
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
A Hainan tarantula and toxin technology, applied in the field of solid-phase peptide synthesis, can solve the problems of limited research and application, difficulty in obtaining natural toxins, etc.
Inactive Publication Date: 2015-09-09
HUNAN INSTITUTE OF SCIENCE AND TECHNOLOGY
View PDF0 Cites 4 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
Problems solved by technology
[0004] Hainan tarantula toxin III, as a highly specific voltage-gated sodium channel Nav1.7 inhibitor, is expected to form a new type of analgesicdrug. However, the natural toxin of Hainan tarantula toxin III is very difficult to obtain, which limits its Research and application, the present invention provides a large-scale preparation method for the preparation of Hainan tarantula toxin III
Method used
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0026] Example 1 Synthesis of Hainan Tarantula Toxin III Peptide Chain
[0027] Weigh 20 grams of Rink Amide resin with a substitution value of 0.5 mmol / g, expand it in DMF for 30 minutes, drain it, add 30 mL of 20% piperidine for deprotection for 15 minutes, drain it, add 30 mL of DMF to wash once, add 20% piperidine 30 ml was deprotected for 10 minutes, washed 5 times with DMF, and completed Fmoc-Leu-OH, Fmoc-Tyr(tBu)-OH, Fmoc-Val-OH, Fmoc-Lys(Boc)- OH, Fmoc-Cys(Trt)-OH, Fmoc-Trp(Boc)-OH, Fmoc-Lys(Boc)-OH, Fmoc-His(Boc)-OH, Fmoc-Lys(Boc)-OH, Fmoc-Ser (tBu)-OH, Fmoc-Ser(tBu)-OH, Fmoc-Cys(Trt)-OH, Fmoc-Ala-OH, Fmoc-Tyr(tBu)-OH, Fmoc-Asn(Trt)-OH, Fmoc- Pro-OH, Fmoc-Cys(Mmt)-OH, Fmoc-Cys(Trt)-OH, Fmoc-Glu(OtBu)-OH, Fmoc-Asn(Trt)-OH, Fmoc-Lys(Boc)-OH, Fmoc -Gly-OH, Fmoc-Pro-OH, Fmoc-Thr(tBu)-OH, Fmoc-Cys(Trt)-OH, Fmoc-Ser(tBu)-OH, Fmoc-Asp(OtBu)-OH, Fmoc-Gly Coupling of -OH, Fmoc-Phe-OH, Fmoc-Gly-OH, Fmoc-Lys(Boc)-OH, Fmoc-Cys(Mmt)-OH, Fmoc-Gly-OH. The NMM / HATU / HOBt system...
Embodiment 2
[0028] Example 2 Hainan Tarantula Toxin III Peptide Resin Removes Mmt Protection
[0029] Example 1 The synthetic Hainan tarantula toxin III peptide resin was deprotected with 20% piperidine / DMF, washed 5 times with DMF, washed 3 times with DCM, dried with nitrogen, added 600 ml of 3% TFA / DCM solution, and reacted After 10 minutes, remove the solution, wash 5 times with DMF, wash 5 times with DCM, and blow dry with nitrogen.
Embodiment 3
[0030] Example 3 Hainan Tarantula toxin III peptide resin is oxidized by air oxidation to form a pair of disulfide bonds
[0031] Add 1000 milliliters of 0.1 M phosphatebuffer solution to the Hainan arachnid toxin III peptide resin obtained in Example 2, and add 1,000 ml of 0.1 M phosphatebuffer solution to the pH value of 7.5. During the reaction, the air is ventilated, the reaction temperature is room temperature, and the reaction time is determined according to the oxidation process. After 24 hours of reaction, the peptide resin was taken for detection. The peptide resin was washed with water and then added to the DTNB solution. The end point of the reaction was that the solution did not turn yellow.
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
PUM
Login to View More
Abstract
The invention provides a preparation method of Hainantoxin-III and belongs to the field of polypeptide and protein preparation. The Hainantoxin-III is synthesized with a Fmoc solid-phase peptide synthesis method, synthetic resin adopts Rink amide resin, cysteine in the second position and cysteine in the seventeenth position adopt Fmoc-Cys(Mmt)-OH, cysteine in other positions adopts Fmoc-Cys(Trt)-OH, Mnt protection removal is performed by adopting 3% TFA (trifluoroacetic acid) after polypeptide chain synthesis ends, disulfide bonds of cysteine in the second position and cysteine in the seventeenth position are formed with an air oxidation method, polypeptide is removed from the resin through pyrolysis after a first pair of disulfide bonds is formed, a second pair of disulfide bonds and a third pair of disulfide bonds are formed with a solid-phase DTNB (5,5'-Dithiobis-(2-nitrobenzoic acid)) oxidation method, and the Hainantoxin-III with biological activity is finally formed. The biological activity and the natural toxic activity of Hainantoxin-III prepared with the method are consistent, and the synthetic efficiency is high.
Description
technical field [0001] The invention relates to solid-phase polypeptide synthesis, in particular to a solid-phase preparation method of Hainan tarantula toxin III. Background technique [0002] Hainan tarantula toxin III is a polypeptide toxoid molecule isolated from Hainan tarantula, 33 amino acid residues, molecular weight 3609 Da, three pairs of disulfide bonds, Hainan tarantula toxin III is a TTX-S type sodium Channel inhibitors have highly selective inhibitory activity on the voltage-gated sodium channel Nav1.7, and Hainan tarantula toxin III is expected to be developed into a specific Nav1.7 voltage-gated sodium channel inhibitor. [0003] The voltage-gated sodium channel Nav1.7 plays a very important role in the conduction of neuropathic pain and inflammatory pain. Inhibiting the activity of the voltage-gated sodium channel Nav1.7 can inhibit the generation of pain. Therefore, the development of voltage-gated sodium channels Nav1.7 highly selective inhibitors ar...
Claims
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
Application Information
Patent Timeline
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to View More 
Login to View More 
