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Polyethylene glycol omega-interferon with long connection bridge and preparation process thereof

A technology of PEGylation and polyethylene glycol, applied in the field of biomedicine, can solve the problems such as omega-interferon PEG-modified products that have not yet appeared, and achieve the effect of being beneficial to separation and purification and high yield of single modification

Inactive Publication Date: 2014-04-02
INST OF PROCESS ENG CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of the interferon drugs currently on the market are based on α-interferon and β-interferon, and there is no PEG-modified product of ω-interferon

Method used

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  • Polyethylene glycol omega-interferon with long connection bridge and preparation process thereof
  • Polyethylene glycol omega-interferon with long connection bridge and preparation process thereof
  • Polyethylene glycol omega-interferon with long connection bridge and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1I

[0023] Determination of the preparation conditions of embodiment 1IFN-mal-P20K

[0024] Replace ω-interferon into 50mM NaAc-HAc buffer (pH5.5), and adjust the concentration of ω-interferon to 2.2mg / mL (ie 0.1mM). According to ω-interferon: 2-iminothiolane: PEG-maleimide (20kDa) molar ratio is 1:1:1, 1:1:2, 1:2:2, 1:2 :4 and 1:4:4 were reacted at 4°C overnight (~16 hours). The modified product was detected with a Superdex200 gel filtration column (1cm×30cm), and the eluent was 20mM phosphate buffer (pH7.4). 20kDa PEG-maleimide modified ω-interferon results as follows figure 2 As shown, the yield was measured by the ratio of the peak area (2 peaks) of IFN-mal-P20K to the total peak area. As the reaction ratio of 2-iminothiolane and 20kDa PEG-maleimide increased, the yield of IFN-mal-P20K also increased, while the peak area of ​​ω-interferon decreased (3 peaks ). However, polymodified ω-interferon (1 peak) appeared and increased with increasing response ratio. Although hig...

Embodiment 2I

[0025] Determination of the preparation conditions of embodiment 2IFN-mal-P40K

[0026] Replace ω-interferon into 50mM NaAc-HAc buffer (pH5.5), and adjust the concentration of ω-interferon to 2.2mg / mL (ie 0.1mM). According to ω-interferon: 2-iminothiolane: PEG-maleimide (40kDa) molar ratio is 1:1:1, 1:1:2, 1:2:2, 1:2 :4 and 1:4:4 were reacted at 4°C overnight (~16 hours). The modified product was detected with a Superdex200 gel filtration column (1cm×30cm), and the eluent was 20mM phosphate buffer (pH7.4). 40kDa PEG-maleimide modified ω-interferon results as follows image 3 As shown, the yield was measured by the ratio of the peak area (2 peaks) of IFN-mal-P40K to the total peak area. As the reaction ratio of 2-iminothiolane and 40kDa PEG-maleimide increased, the yield of IFN-mal-P40K also increased, while the peak area of ​​ω-interferon decreased (3 peaks ). However, polymodified ω-interferon (1 peak) appeared and increased with increasing response ratio. Although high...

Embodiment 3I

[0027] Example 3 Identification of IFN-mal-P20K and IFN-mal-P40K

[0028] IFN-mal-P20K and IFN-mal-P40K were identified by SDS-PAGE and gel filtration chromatography. Such as Figure 4 As shown, IFN-mal-P20K and IFN-mal-P40K both showed a band on the SDS-PAGE electropherogram, which indicated that the two PEG modified products had higher purity. The migration rate of IFN-mal-P40K electrophoresis band is slower than IFN-mal-P20K, and IFN-mal-P20K is slower than ω-interferon. This indicates that PEG modification can increase the molecular weight of ω-interferon, and the molecular weight of IFN-mal-P40K is higher than that of IFN-mal-P20K. Such as Figure 5 As shown, after being eluted with buffer, IFN-mal-P20K and IFN-mal-P40K had a single elution peak on Superdex200 gel filtration column (1.0cm×30cm). Among them, the peak time of IFN-mal-P20K is faster than that of IFN-mal-P40K, but slower than that of ω-interferon. This shows that IFN-mal-P20K and IFN-mal-P40K have higher...

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Abstract

The invention relates to the field of biological medicines and specifically relates to polyethylene glycol (PEG) omega-interferon with a long connection bridge and a preparation method thereof. The method comprises: (1) 2-imino thiacyclopentane reacts with a primary amine group of the omega-interferon, sulfydryl is introduced, the sulfydryl on the surface of the omega-interferon reacts with PEG-maleimide to realize PEG-modified omega-interferon; (2), a longer connection bridge exists between the PEG and the omega-interferon, so that space shielding effect of the PEG on the omega-interferon can be predicated to be lowered, and the biological activity of the omega-interferon can be improved; (3), compared with un-modified omega-interferon, the polyethylene glycol omega-interferon has a longer circulation half-life period in vivo, can be used for obviously reducing drug-use times and lowering the toxic and side effect, is especially suitable for treating a patient resistant to the alpha-interferon, and has wide application prospect in clinical.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular, the invention relates to a polyethylene glycol (PEG) ω-interferon with a long connecting bridge, and a preparation process thereof. Background technique [0002] Interferon (interferon, IFN) is a kind of glycoprotein produced by white blood cells through anti-viral immune response after the body is infected by virus, and has biological activities such as anti-virus, anti-tumor and immune regulation. Since 1986, interferon has become the first cytokine approved by the FDA for clinical use. Interferon was first divided into type Ⅰ and type Ⅱ. There are two components in Type I, which can be divided into α and β. The subsequently discovered ε, κ, ω, and δ-IFN all belong to type I interferon. Type II is defined as gamma interferon. ω-interferon is a type I interferon discovered by Austrian scientist Rudelf Hamptan et al. in 1985. Gunther R. Adolf found in 1987 that ω-interferon and α-in...

Claims

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Application Information

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IPC IPC(8): C07K14/555A61K38/21A61P31/12A61P35/00
CPCC07K14/555A61K38/00
Inventor 胡涛陈薇于长明房婷付玲张金龙于婷
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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