A photoresponsive degradable tumor koningine precursor compound and its preparation and application

A technology of precursor compound and tumorikinin, which is applied in the field of tumorikinin precursor compounds, can solve the problems of inability to release timed and fixed-point, incomplete and burst release of tumoricornin preparations, toxic and side effects, etc. The effect of large drug load and reduction of toxic and side effects
CN107673983BActive Publication Date: 2020-03-10MENGCHAO HEPATOBILIARY HOSPITAL OF FUJIAN MEDICAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
MENGCHAO HEPATOBILIARY HOSPITAL OF FUJIAN MEDICAL UNIV
Publication Date
2020-03-10

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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.
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Description

[0001] (1) Technical field

[0002] The invention relates to a photoresponsive degradable tumor cloningin precursor compound, a preparation method and an application thereof.

[0003] (2) Background technology

[0004] 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.

[0005] 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...

Claims

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