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Medicines for targeted diagnosis and photosensitive therapy for cancer and application for same

A technology of photosensitizing drugs and photosensitizing compounds, which is used in cancer targeted diagnosis and photosensitizing therapeutic drugs and its application fields, and can solve the problem that photosensitizers can only reach the intercellular space, sample preparation of macromolecular carrier systems, chemical and biological stability and sample preparation. Storage issues, limited tumor uptake, etc.

Active Publication Date: 2012-06-27
武汉科信达致力科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, biomacromolecules have serious problems in the tumor-specific therapy of PS drugs, including: Because various physiological barriers (for example, temporally and spatially heterogeneous blood flow and vascular permeability) are difficult for drug molecules to reach effectively Obstruction of target tissue and target cells; problems with sample preparation, chemical and biological stability, and sample storage in macromolecule carrier systems; limited tumor uptake due to photosensitizers only reaching the intercellular space, etc.

Method used

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  • Medicines for targeted diagnosis and photosensitive therapy for cancer and application for same
  • Medicines for targeted diagnosis and photosensitive therapy for cancer and application for same
  • Medicines for targeted diagnosis and photosensitive therapy for cancer and application for same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1, PZ-001-Ce6 and PZ-001-Ce6 / 64 Preparation of Cu

[0055] Photosensitizer-carrier copolymer PZ-001-Ce6 and PZ-001-Ce6 / 64 The chemical synthesis route of Cu is shown below (Scheme 1):

[0056]

[0057] Chemical synthesis route (Scheme 1)

[0058] N-a-(tert-butoxycarbonyl)-lysine was purchased from Sigma-Aldrich Chemicals.

[0059] N,N'-dicyclohexylcarbodiimide (DCC), N-hydroxysuccinimide, 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) and sodium tetraborate buffer solution were purchased from Arcos Chemicals.

[0060] Chlorin e6 (Ce6) was a gift from Medkoo Biosciences.

[0061] MHI-148 was synthesized according to literature procedures.

[0062] [64Cu]copper chloride was purchased from Washington University in St. Louis.

[0063] (1) Synthesis of MHI-148-lysine 2:

[0064] MHI-148 (200 mg, 0.28 mmol) and N-hydroxysuccinimide (32 mg, 0.28 mmol) were dissolved in 140 mL of dichloromethane, then 57.3 mg (0.28 mmol) of DCC were added. The mixt...

Embodiment 2

[0068] Example 2: PZ-001-Ce6 / 64 Synthesis of Cu 4b (or 4a)

[0069] Continuously add 100 µg of PZ-001-Ce63 in 1.5 ml eppendorf vials, 200 UL to achieve 0.1 N ammonium acetate buffer (pH 5.5) and 2 mCi [ 64 Cu]CuCl 2 . The reaction mixture was shaken at room temperature for 15 minutes. Purified by high performance liquid chromatography to obtain 1.8 mCi PZ-001-CE6 / 64 Cu4b (radiolabeling 90 to 96%). By a similar method, the corresponding non-radioactive compound 4a can be obtained. The mass spectrum (MALDI-TOF) of 4a is m / z 1451 (M+H).

Embodiment 3

[0070] Embodiment 3: Determination of singlet oxygen quantum yield (Δφs)

[0071] The determination of singlet oxygen quantum yield (Δφs) was performed according to the method of reference [13]. Briefly, 9,10-diphenyl was added to a tetrahydrofuran solution of PZ-001-Ce6, and oxygen was bubbled for 5-10 minutes. The prepared solution was then illuminated with a 655 nm laser beam (20 mW) (5 minutes). Measure the absorbance of the solution at 375 nm before and after illumination, and record the readings. The quantum yield of singlet oxygen can be determined by the difference in absorbance value, the formula is as follows: Δφs=ΔAS / ΔAR×ΔφR×100%. The results showed that the singlet oxygen quantum yield (PSC) of PZ-001-CE6 was 0.26%.

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Abstract

The invention relates to a series of brand-new micromolecular targeted diagnosis reagents and photodynamic therapy (PDT) medicines for tumour. In the brand-new micromolecular targeted diagnosis reagents for tumour and the PDT medicines disclosed by the invention, tumour-targeting carrier molecules are connected with a photosensitizer via connection chemical bonds, thereby achieving a purpose of directionally conveying photosensitive medicines to cancer pathological cells and tissues. The compounds can be used for cancer diagnosis and location, observation pharmacokinetic and early evaluation for the effect of PDT after being combined with imaging isotope by the characteristic that Ce6 can be in complexation with metal ions.

Description

technical field [0001] This patent involves a series of diagnostic and therapeutic drugs with cancer cell targeting functions. This type of small molecule drug is composed of cancer targeting carrier compounds, photosensitive drugs and imaging isotopes, and integrates photosensitive therapy and nuclear imaging diagnostic functions ( figure 1 ), which can be applied to clinical photodynamic therapy and diagnostic positioning of cancer. The invention also relates to the synthesis and preparation of the series of compounds, and its use and effect have been verified in cancer animal models. Background technique [0002] Cancer remains by far the most difficult disease to treat due to its significant morbidity and mortality. There are more than 100,000 new cases worldwide each year [1]. Traditional cancer treatment methods such as surgery, chemotherapy, and radiotherapy lack target selectivity. While killing tumor cells, they will also cause great damage to the normal body and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/22A61K31/409A61K47/22A61K47/34A61K41/00A61K51/04A61K51/06A61P35/00
Inventor 潘东风
Owner 武汉科信达致力科技有限公司
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