Elastic targeting polypeptide-based medicine-carrying nanoparticle as well as preparation method and application thereof
A technology targeting peptides and drug-loaded nanometers, which is applied in the field of medicine, can solve the problems of large side effects and poor targeting selectivity of anticancer drugs, and achieve the effects of high drug loading rate, expansion and efficacy, and small dispersion
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Embodiment 1
[0018] Example 1: Preparation of Elastic Targeting Polypeptide ABD-iTEP70-(GGGGC)8
[0019] First design the amino acid sequence ABD and iTEP, and then use the existing peptide synthesis method to prepare
[0020] ABD-(iTEP)70-(GGGGC)8, where
[0021] ABD amino acid sequence: LAEAKVLANRELDKYGVSDFYKRLINKAKTVEGVEALKLHILAALP
[0022] Amino acid sequence of iTEP: GAGVPG
[0023] After the gene encoding the elastic targeting polypeptide ABD-(iTEP)70-(GGGGC)8 was synthesized, it was digested and inserted into the modified pET25b(+) vector to construct a recombinant expression plasmid; the gene sequence was successfully prepared after sequencing.
Embodiment 2
[0024] Example 2: Preparation of Elastic Targeting Polypeptide ABD-(iTEP)70-(GGGGGGC)8
[0025] First design the amino acid sequences ABD and iTEP, and then prepare ABD-(iTEP)70-(GGGGGGC)8 using the existing peptide synthesis method, wherein
[0026] ABD amino acid sequence: LAEAKVLANRELDKYGVSDFYKRLINKAKTVEGVEALKLHILAALP
[0027] Amino acid sequence of iTEP: GAGVPG
[0028] After the gene encoding the elastic targeting polypeptide ABD-(iTEP)70-(GGGGGGC)8 was synthesized, it was digested and inserted into the modified pET25b(+) vector to construct a recombinant expression plasmid; its gene sequence was successfully prepared after sequencing.
Embodiment 3
[0029] Example three: Synthesis of modified paclitaxel PTX-LEV-MECH
[0030]
[0031] Synthesis of Compound 1: Dissolve hydrazine hydrate (20.0 g, 0.40 mmol) in 80 mL of isopropanol at 0° C., then add di-tert-butyl dicarbonate (43.6 g, 0.20 mmol) to the solution, and dissolve the reaction solution The temperature was raised to room temperature, stirred for 1 hour, the solvent was removed, the residue was dissolved in dichloromethane, the insoluble matter was removed by filtration, and the organic phase was concentrated to obtain compound 1 (19.4 g, 74% yield) as a white solid. 1 H NMR (400MHz, CDCl 3 )δ1.46(s, 9H)
[0032] Synthesis of Compound 2: Maleic anhydride (5.00 g, 51.0 mmol) was dissolved in 100 mL of acetic acid at 0° C., and then 6-aminocaproic acid (6.69 g, 51.0 mmol) was slowly added to the above solution. The reaction solution was warmed up to room temperature and stirred for 4 hours. Subsequently, the reaction solution was heated to reflux overnight. Unde...
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