Micro-assisted solid-phase synthesis of analogue of MC-JJ0105 polypeptide isolated from Momordica charantia and application of the analogue
A MC-JJ0105, solid-phase synthesis technology, used in medical preparations, peptides, and drug combinations containing active ingredients, can solve the problems of inability to synthesize target polypeptides, loss of synthetic significance, and long synthesis cycle, achieving easy industrial The effect of automatic production, low production cost and short synthesis cycle
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Embodiment 1
[0023] Microwave-promoted solid-phase synthesis of Pro-Ala-Ala-Tyr-Ser-Ile-Ala-Ala-Ser (SEQ.ID NO: 2)
[0024] (1) Swelling of the resin
[0025]Weigh 50mg of Fmoc-rink amide-MBHA Resin (substitution amount 0.4mmol / g), swell with 7mL DCM for 30min, filter to remove DCM, then swell with 10mL NMP for 30min, and finally rinse with NMP, DCM, and NMP 7mL respectively.
[0026] (2) Microwave promotes removal of Fmoc protecting group
[0027] Put the swollen resin into the reactor, add 7mL of 25% piperidine / NMP (V / V) solution containing 0.1M HOBT, react in the microwave reactor for 1min, the microwave power is 15W, and the reaction temperature is controlled at 50°C Within the time period, use an air compressor to compress the air to cool, and filter the solution after the reaction; add 7 mL of 25% piperidine / NMP (V / V) solution containing 0.1M HOBT and react in a microwave reactor for another 4 minutes, and the microwave power is 25W , the reaction temperature was controlled at 50°C...
Embodiment 2~42
[0041] According to the method described in Example 1, the polypeptides of Examples 2-42 were synthesized according to the corresponding sequences, and their respective molecular weights were confirmed by electrospray mass spectrometry (ESI-MS).
Embodiment 2
[0043] Pro-(D-Ala)-Ala-Tyr-Ser-Ile-Ala-Ala-Ser (SEQ.ID NO: 3); Theoretical relative molecular mass is 849.9
[0044] ESI-MSm / z: found[M+3H] 3+ 284.3, [M+4H] 4+ 213.4, [M+5H] 5+ 171.0;calu[M+3H] 3+ 284.3, [M+4H] 4+ 213.5, [M+5H] 5+ 171.0
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