Anti-tumor tree-shaped polypeptide macromolecule medicament carrier system

A macromolecular carrier and anti-tumor drug technology, applied in the field of dendritic polypeptide macromolecular drug carrier system, can solve the problems of limited use, non-specific toxicity, poor water solubility, and no treatment options for cancer with chemotherapy drugs

Inactive Publication Date: 2009-06-24
刘湖
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently used anticancer drugs have severe side effects that often limit the use of chemotherapy drugs and leave many cancers without treatment options
For example, many anti-tumor drug molecules and platinum-containing substances have non-specific toxicity and poor water solubility, and the use of carboplatin and cisplatin has been limited accordingly.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 Synthesis of second-generation glutamic acid dendrimer-camptothecin (1a)

[0021] A suspension of the second-generation glutamic acid dendrimer (300mg, 2.9mmol) and (S)-10-tert-butoxycarbonylcamptothecin (200mg, 0.46mmol) in dimethylformamide (40mL), Dissolution was carried out with gentle heating. When the obtained solution was cooled to room temperature, a solution of chloromethylpyridinium iodide (150 mg, 0.7 mmol) in dimethylformamide (2.5 mL) and 4-dimethylaminopyridine (100 mg, 0.9 mmol) were added sequentially. ) in dimethylformamide (2.5 mL). After stirring for 100 h, the mixture was cooled in an ice bath, then 10% aqueous sodium chloride solution (100 mL) was added within 30 min under vigorous stirring. After acidification to pH = 2 by slowly adding 0.5M hydrochloric acid, it was stirred at room temperature for another 30 min. The solid was collected by centrifugation and the supernatant removed. The solid was suspended in water (200 mL) and isolat...

Embodiment 2

[0023] Example 2 Synthesis of second-generation glutamic acid dendrimer-alanine-camptothecin (2a)

[0024] In the To a suspension in anhydrous dimethylformamide (15 mL), a solution of 1,3-diisopropylcarbodiimide (70 mg, 0.5 mmol) in dimethylformamide (1 mL) was added within 20 min . The mixture was stirred under nitrogen for 2 days. After cooling in an ice bath, 10% aqueous sodium chloride (40 mL) was added within 30 min. After stirring for 1 h, the mixture was adjusted to pH=2.5 by adding 1N hydrochloric acid. The solid was filtered off, washed with water (5 x 25 mL), and dried under vacuum. The solid was washed with 2% methanol-dichloromethane (4 x 50 mL) and dried under vacuum to yield the second-generation glutamic acid dendrimer-alanine-camptothecin (2a) (630 mg, Yield 75%), H-NMR (300MHz, TFA-d): δ 9.45 (s), 7.85-8.6 (m, aromatic hydrocarbon proton), 5.92 (d, J=18.3Hz, lactone proton), 5.70 (s ), 5.62 (d, J=18.3Hz, lactone proton), 4.8 0-6.05 (m), 3.80-4.50 (m), 1....

Embodiment 3

[0026] Example 3 Synthesis of second-generation glutamic acid dendrimer-Gln-Ser-camptothecin (3a)

[0027] The second-generation glutamic acid dendrimer-Gln-Ser-camptothecin (3a) was synthesized from the third-generation glutamic acid dendrimer and O-(N-tert-butoxycarbonyl)Gln-Ser-camptothecin The preparation process is the same as that of 2a.

[0028] Synthesis of three generations of glutamic acid dendrimers-Gln-Ser-camptothecin (3b) and 3a.

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PUM

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Abstract

The invention relates to an anti-tumor dendric polypeptide macromolecule medicine vector system and application thereof in pharmacy. The dendric polypeptide macromolecule can be prepared by the solid phase, liquid phase or solid-liquid combination method of single or different natural amino acids, and can be used for preparing a vector release system which is loaded with malignant tumor resisting treatment medicines. The dendric polypeptide macromolecule medicine vector system is a covalent bond vector medicine system in which anti-tumor activity micromolecule medicines are sealed in dendric polypeptide macromolecule polymers, or the anti-tumor activity micromolecules are combined with functional groups on the surfaces of the anti-tumor dendric polypeptide macromolecules. The dendric polypeptide macromolecule medicine vector system can correspondingly inhibit growth of the malignant tumor and is applied to a patient suffered from the malignant tumor in the modes of venous, oral-taking, endermic and arterial administration or local administration. The anti-tumor dendric polypeptide macromolecule medicine vector system has the advantages of high targeting property, high medicine carrying capability, good waster solubility and stability and lower toxicity.

Description

technical field [0001] The invention relates to an anti-tumor dendritic polypeptide macromolecule drug carrier system and its application in pharmacy. Dendritic polypeptide macromolecules can be synthesized from single or different natural amino acids through solid phase, liquid phase or solid-liquid combination methods, and can be used to prepare carrier release systems loaded with anti-malignant tumor therapeutic drugs. The dendritic polypeptide macromolecule carrier drug system can be in two structural forms: the anti-tumor active small molecule drug is encapsulated in the dendritic polypeptide macromolecular polymer, and the anti-tumor drug interacts with the anionic functional groups on the surface of the dendritic polypeptide macromolecule , so that the dendrimers can take up anti-tumor active small molecules, and may combine with functional groups inside the dendritic polypeptide macromolecule; anti-tumor active drug small molecules and functional groups on the surface ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61P35/00A61K47/64
Inventor 刘湖
Owner 刘湖
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