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Chlorambucil precursor compound with photo-responsive degradation effects and its preparation and application

A kind of precursor compound, the technology of leuconin, which is applied in the field of leuconin precursor compounds, can solve the problems of toxic and side effects, incomplete and burst release of leuconin preparations, unable to release at a fixed time and at a fixed point, etc., and achieves the drug load Large, small size, reducing the effect of toxic and side effects

Active Publication Date: 2018-02-09
MENGCHAO HEPATOBILIARY HOSPITAL OF FUJIAN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to provide a nano-precursor compound, preparation method and application of Licotonin with light-responsive release, so as to solve the incomplete release and burst release of Licotonin preparations in the prior art, which cannot be released at a fixed time and at a fixed point, so that The problem of severe toxic side effects caused by

Method used

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  • Chlorambucil precursor compound with photo-responsive degradation effects and its preparation and application
  • Chlorambucil precursor compound with photo-responsive degradation effects and its preparation and application
  • Chlorambucil precursor compound with photo-responsive degradation effects and its preparation and application

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Experimental program
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Effect test

Embodiment 1

[0030] Embodiment 1: the preparation of precursor compound molecule

[0031] Dissolve 180mg (0.6mmol) of Cyclonine in 10mL of anhydrous CH 2 Cl 2 After cooling in an ice bath, add 148mg (0.72mmol) of N,N'-dicyclohexylcarbodiimide, 13.8mg (0.072mmol) of 4-dimethylaminopyridine and 236mg (0.6mmol) of hexadecyl For nitrobenzyl derivatives, react at 0-5°C for 1 hour, then naturally rise to room temperature and keep reacting for 24 hours. After the reaction was finished, the white by-product (DCU) was filtered off, the filtrate was concentrated under reduced pressure, and the white solid product was obtained by silica gel column chromatography. The eluent was ethyl acetate:petroleum ether, and the yield was 75%.

[0032] The molecular structure of the precursor compound was characterized by H NMR and C NMR results. The results are as follows: figure 1 and figure 2 shown.

Embodiment 2

[0033] Example 2: Photodegradation Assay of Precursor Compound Molecules

[0034] Prepare 0.1mg / mL acetonitrile solution of precursor compound molecules, and irradiate with 365nm ultraviolet light (1mW / cm 2 ) irradiated for different times, using high-performance liquid chromatography to measure the behavior of precursor compound molecules transformed into Lianke Ning drug molecules by light, and the degradation efficiency was determined by comparing the integral areas of the two. The results are as follows image 3 shown. Experiments have shown that the precursor compound molecules are almost completely degraded after only 10 minutes of irradiation.

Embodiment 3

[0035] Embodiment 3: the preparation of nano drug

[0036] Precursor compound molecules (20 mg) and MSNs (18 mg) were dissolved in 3 mL of absolute ethanol, shaken at room temperature for 24 hours, centrifuged at 10,000 rpm for 10 minutes to collect nanoparticles, and washed twice with water to obtain nanomedicines. The morphology of the nanomedicine was characterized by transmission electron microscopy, and the results were as follows: Figure 4 shown.

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Abstract

The invention discloses a chlorambucil precursor compound with photo-responsive degradation effects and its preparation and application. The precursor compound has a structural formula (I). The chlorambucil precursor molecule contains a light-sensitive group and is connected to a strong hydrophobic group through the light-sensitive group. Mesoporous silica (MSNs) with good biocompatibility is usedas a carrier so that the hydrophobic light-responsive chlorambucil prodrug molecule is adsorbed in MSNs channels. Under illumination, the hydrophobic prodrug molecule can be degraded into hydrophilicchlorambucil molecules so that the hydrophilic chlorambucil molecules can escape from mesoporous silica and produce drug effects. The preparation method realizes light-controlled release of drugs andthe problem that the existing chlorambucil preparation cannot be fully released and largely released and cannot be regularly released at fixed points so that violent toxic and side effects are produced.

Description

(1) Technical field [0001] The invention relates to a photoresponsive degradable tumor cloningin precursor compound, a preparation method and an application thereof. (2) Background technology [0002] Chlorambucil (Chlorambucil) is an antineoplastic drug that acts on the structure of DNA. It is mainly used for chronic lymphocytic leukemia, and is also suitable for malignant lymphoma, multiple myeloma, macroglobulinemia, ovarian cancer. However, the small-molecule Liukonin lacks selectivity to tumor tissue and has strong bone marrow and nerve cell toxic side effects, so it generally cannot be used directly. In recent years, the development of a controlled release system for Liukonin is an effective way to improve efficacy and reduce side effects. [0003] Among many environment-sensitive drug controlled release strategies, the light-controlled drug controlled release system can actively and precisely regulate the target molecule to achieve "timed, fixed-point, and fixed-spe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C229/42C07C227/18A61K41/00A61K9/14A61K47/04A61K31/196A61P35/00
CPCA61K9/0009A61K9/143A61K31/196A61K41/0042C07C229/42
Inventor 吴名刘景丰刘小龙曾永毅
Owner MENGCHAO HEPATOBILIARY HOSPITAL OF FUJIAN MEDICAL UNIV
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