Application of polypeptide analogue in anti-wrinkle and anti-aging
A technology of analogs and peptides, applied in the application field of peptide analogs in anti-wrinkle and anti-aging, can solve the problems of ineffective release of neurotransmitters from vesicles and weakened muscle contraction, so as to achieve better anti-wrinkle and anti-aging, and reduce chronic inflammation. , better effect
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Examples
Embodiment 1
[0059] Example 1: Preparation of Argireline-MYMD
[0060] Argireline-MYMD, molecular weight 1019.15, has the following structure:
[0061]
[0062] The preparation method of Argireline-MYMD specifically includes:
[0063] 1.1. Weigh 4 g (1 mmol) of RinkAmide Resin resin (Sub=0.25 mmol / g) into the reaction column, wash with DMF three times, and then swell with DMF for 30 minutes. Then use DBLK to remove the Fmoc protecting group, wash 6 times with DMF, weigh 3.9 g (6 mmol) of Fmoc-Arg(Pbf)-OH and 0.9 g (6.6 mmol) of HOBt, dissolve in DMF, and add them in an ice-water bath at 0°C. 1.2 g of DIC (9 mmol) was activated for 5 minutes and added to the reaction column. After 2 hours of reaction, the test result of ninhydrin was negative (the resin was colorless and transparent), and then the Fmoc protecting group was removed with DBLK. Repeat the above operation, according to the sequence coupling Fmoc-Arg(Pbf)-OH, Fmoc-Glu(OtBu)-OH, Fmoc-Met-OH, Fmoc-Glu(OtBu)-OH, Fmoc-Glu(OtBu)...
Embodiment 2
[0065] Example 2: Preparation of Pentapeptide-MYMD
[0066] Pentapeptide-MYMD, molecular weight 974.26, has the following structure:
[0067]
[0068] The preparation method of Pentapeptide-MYMD specifically includes:
[0069] 2.1. Weigh 3.3 g (1 mmol) of Fmoc-Ser(tBu)-Wang Resin (Sub=0.30 mmol / g) into the reaction column, wash with DMF 3 times, and swell with DMF for 30 minutes. Then use DBLK to remove the Fmoc protecting group, wash 6 times with DMF, weigh 3.9 g (6 mmol) of Fmoc-Lys(Boc)-OH and 0.9 g (6.6 mmol) of HOBt, dissolve in DMF, and add them in an ice-water bath at 0°C. 1.2 g of DIC (9 mmol) was activated for 5 minutes and added to the reaction column. After 2 hours of reaction, the test result of ninhydrin was negative (the resin was colorless and transparent), and then the Fmoc protecting group was removed with DBLK. Repeat the above operation, according to the sequence coupling Fmoc-Thr(tBu)-OH, Fmoc-Thr(tBu)-OH, Fmoc-Lys(Alloc)-OH, Palmitoyl chloride, after ...
Embodiment 3
[0072] Example 3: Preparation of SYN-AKE-MYMD
[0073] SYN-AKE-MYMD, molecular weight 547.66, has the following structure:
[0074]
[0075] The preparation method of SYN-AKE-MYMD specifically includes:
[0076] 3.1. Add 4 g of RinkAmide Resin resin (1 mmol, resin substitution value is 0.25 mmol / g) into the reactor, swell with DMF for 1 hour after washing, filter with suction, add 20% piperidine / DMF solution, and take 4-hydroxymethyl 0.9 g of phenylacetic acid and 0.9 g of HOBT, dissolve at low temperature, slowly add 1.2 g of DIC, and stir to obtain an activation solution, add the activation solution to the reactor, start the reaction with nitrogen blowing, add 15 ml of NMM after the reaction starts, and continue the reaction for 2 hour, suction filtered, washed with DMF, washed with DCM;
[0077] 3.2. Add 2.7 g of Boc-Dab(Fmoc)-OH to the reactor, add DCM to dissolve in an appropriate amount, blow nitrogen gas, add 0.5 g of pyridine, control the temperature of the reacti...
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Description
Claims
Application Information
- IPC
- C07K19/00; C07K1/04; C07K1/06; C07K1/14; C07K1/34; C07K1/36; A61K38/08; A61K38/06; A61P17/18; A61P17/00; A61P29/00; A61K8/64; A61Q19/08; A61Q19/02; A23L33/18
- CPC
- C07K7/06; C07K5/0821; A61P17/18; A61P17/00; A61P29/00; A61K8/64; A61Q19/08; A61Q19/02
- Inventors
- 王宇恩; 张凌云