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Novel ghrelin-like peptide dimer and its application

A technology for releasing hormones and growth hormones, which is applied in the field of medicine and biology, and can solve problems such as reduced activity

Active Publication Date: 2019-07-12
深圳纳福生物医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Native hGHRH(1-44)OH has a half-life of 13 minutes, C-terminal PEGylation of GHRH analogues can increase molecular stability and prolong half-life, but the activity is also significantly reduced

Method used

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  • Novel ghrelin-like peptide dimer and its application
  • Novel ghrelin-like peptide dimer and its application
  • Novel ghrelin-like peptide dimer and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] 1. Synthesis of human growth hormone releasing hormone analogue peptide without side chain modification or 30-33 peptide with side chain modification:

[0039] (1) Monomer peptide synthesis process: Manual solid-phase peptide synthesis operation steps.

[0040] 1. Resin swelling: put Dawang resin (wang resin, purchased from Tianjin Nankai Synthetic Technology Co., Ltd.) into a reaction pot, add dichloromethane (DCM, Dikma Technologies Inc.) 15ml / g resin, and shake for 30min. SYMPHONY 12-channel polypeptide synthesizer (SYMPHONY model, software Version.201, Protein Technologies Inc.).

[0041] 2. Connect the first amino acid: Remove the solvent through sand core suction filtration, add 3 times the mole of the first Fmoc-AA amino acid at the C-terminal (all Fmoc-amino acids are provided by Suzhou Tianma Pharmaceutical Group Fine Chemicals Co., Ltd.), and then Add 10-fold molar amounts of 4-dimethylaminopyridine (DMAP) and N,N'-dicyclohexylcarbodiimide (DCC), and finally ...

Embodiment 2

[0094] Example 2: Pituitary growth hormone releasing activity

[0095] 1. Growth hormone releasing activity in vitro: S-D female mice (body weight 200±20 g) were purchased from the Experimental Animal Center of Guangzhou University of Traditional Chinese Medicine. The regime of care and use of all experimental animals was consistent with animal husbandry guidelines. During feeding, the rats were reared alternately between light and dark for 12:12 hours, and the feeding temperature was 26±1°C. Rats died suddenly by dislocation, and the pituitary gland was removed within 30 minutes. After washing with sterilized lactated Ringer's buffer (LRB), the pituitary gland was immediately placed in a 1×10cm glass tube with 1ml of LRB, and kept at 37°C. All glass tubes are kept warm for 5h (P 1 ,P 2 , I 3 , I 4 and I 5, representing different periods of 5 hours of heat preservation, each period represents 1 hour), while shaking gently every 5 minutes. After every 1 hour, the buffer...

Embodiment 4

[0109] Example 4: Treatment of Dimeric Peptides to Infertility Models (Represented by No. 29, 38, 41 and No. 50 Peptides in Table 1)

[0110] 1. Infertility model test method: Take 50 Chinese hamster males and 50 Chinese hamster females (five-week-old, provided by the Experimental Animal Center of Sichuan Province), and group them according to the indifferent body weight [dimer Peptide dosage groups (peptide dosage groups No. 29, 38, 41 and 50 in Table 1), human gonadotropin hMG group, cyclophosphamide control group and normal saline group]. Each group initially set n=10, intraperitoneally injected cyclophosphamide (Jiangsu Hengrui Medicine Co., Ltd., H32020857, batch number 12032925) at 20 mg / kg, once a week, five times in total. After the injection of cyclophosphamide in the fourth week, the mice were grouped and labeled according to their body weight, and the dosage was calculated according to their body weight before each administration. Others used physiological saline a...

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Abstract

The invention discloses a novel growth hormone releasing hormone analogue peptide dimer and an application thereof. The amino acid sequence of the novel growth hormone releasing hormone analogue peptide dimer is as follows: (NH2)X1-ADAIFTNSYR-X12-VLGQLSAR-X21-LLQDIMS--C32-C32-theta-SMIDQLL-X21-RASLQGLV-X12-RYSNTFIADA-X1(NH2), wherein formula is R, RG or RGG; theta is GGR or GR and R or (NH2)X1-ADAIFTNSYR-X12-VLGQLSAR-X21-LLQDIMSRQQGESNQERGARAR--C46-C46-omega-RARAGREQNSEGQQRSMIDQLL-X21-RASLQGLV-X12-RYSNTFIADA-X1(NH2), wherein formula is L, LG or LGG and omega is GGL or GL and L. The growth hormone releasing hormone analogue peptide dimer can improve in vivo or in vitro growth hormone releasing activity and has a longer half life, so that the dimer has wide pharmacological activity, for example, promoting wound healing, promoting cardiac muscle cell reconstruction, improving sleeping quality, promoting proliferation and differentiation of generative cells so as to treat infertility, adjust immunity, reduce weight and treat diabetes.

Description

[0001] Technical field: [0002] The invention belongs to the field of medicine and biology, and specifically relates to the preparation of various human new growth hormone releasing hormone analogue peptide dimers and their application in treatment. [0003] Background technique: [0004] Central growth hormone releasing hormone (GHRH) is a neuropeptide hormone released by the hypothalamus, which can specifically stimulate the pituitary gland to synthesize and release growth hormone (GH), and growth hormone stimulates the liver and other organs to produce insulin-like growth factors (IGFs ), regulate the growth of body cells. hGHRH exists in three forms in the human hypothalamus: hGHRH(1-44)NH 2 , hGHRH(1-40)OH and hGHRH(1-37)OH. Among the hGHRH molecules, the short sequence hGHRH(1–29) with 51% biological activity was the core peptide. According to the mechanism of hGHRH molecules specifically acting on the pituitary gland to produce GH, we designed to determine the in vit...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/60A61K38/25A61P15/08A61P17/02A61P3/10A61P9/00A61P25/20A61P37/02
CPCA61K38/00A61P3/10A61P9/00A61P15/08A61P17/02A61P25/20A61P37/02C07K14/60
Inventor 唐松山张旭东谭宏梅唐婧晅罗群
Owner 深圳纳福生物医药有限公司
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