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Application of cyclohexanediamine hypocrelline B in photodynamic anti-tumor medicaments

A technology of ethylenediamine-based bamboo rhododendron and antitumor drug, which is applied in the application field of ethylenediamine-based rhododendron chinensis B in photodynamic antitumor drugs, and achieves single and clear components, low dark toxicity, and anti-tumor effect. The effect of a broad spectrum of cancer

Inactive Publication Date: 2012-07-04
BEIJING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the application of ethylenediaminohypocretin as a photosensitizer in photodynamic antitumor drugs has not been reported in the literature at present.

Method used

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  • Application of cyclohexanediamine hypocrelline B in photodynamic anti-tumor medicaments
  • Application of cyclohexanediamine hypocrelline B in photodynamic anti-tumor medicaments
  • Application of cyclohexanediamine hypocrelline B in photodynamic anti-tumor medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Example 1: Preparation and purification of ethylenediamine hypocrellin

[0067] Prepared according to the method disclosed in CN1600771A. Weigh 200 grams of the raw material Hypocretin B, dissolve it in 200 ml of freshly steamed tetrahydrofuran; add 20 ml of ethylenediamine; stir at 55 degrees Celsius for 12 hours in the dark, distill off the solvent under reduced pressure; dissolve the precipitate with 200 ml of chloroform, and use 1% Adjust the pH value to neutral with dilute hydrochloric acid; distill off the chloroform; recrystallize with 200 g of ethyl acetate; then purify the residue by thin-layer chromatography to obtain ethylenediaminohypocretin with a yield of 55%. The purity of ethylenediaminohypocretin B was determined by high-performance liquid chromatography, and the purity was higher than 95%.

[0068] The ethylenediamine-hypocretin B obtained above is stored in a freeze-dried form, dissolved in DMSO to make a storage solution when in use, and diluted wit...

Embodiment 2

[0069] Embodiment 2: the preparation of injection

[0070] Take 1 g of the freeze-dried powder of ethylenediaminohypocretin B prepared in Example 1, encapsulate it in liposome, add a pH regulator and an osmotic pressure regulator, and prepare it into an injection.

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Abstract

The invention relates to an application of cyclohexanediamine hypocrelline B in photodynamic anti-tumor medicaments as a photosencitizer, and the photodynamic anti-tumor medicaments comprise the medicaments for treating cervical cancer, breast cancer, lung cancer, stomach cancer, skin cancer and other malignancies. The detection proves that the IC50 dark toxicity of the cyclohexanediamine hypocrelline B against HeLa, MCF7, MCF7 / Adr, A549, A549 / DDP, H1299, MGC803, A875 and other tumor cells when the cyclohexanediamine hypocrelline B is placed away from light is greater than 160 mu M; the IC50 phototoxicity of the cyclohexanediamine hypocrelline B against the detected tumor cells when the dose of red light is 12J / cm<2> for irradiation is less than 0.3 mu M; and a light enhancement factor (IC50 dark toxicity / IC50 phototoxicity) is greater than 500 and even greater than 1600. Mitochondria are further proven to be important action target points for photodynamic killing of the tumor cells through the cyclohexanediamine hypocrelline B, and the tumor cells mainly die in an apoptosis way.

Description

technical field [0001] The invention relates to the application of ethylenediaminohypocretin as a photosensitizer in photodynamic antitumor drugs. Background technique [0002] Photodynamic therapy (PDT) is an emerging therapy that combines light and photosensitizers to treat pathological tissues of the body. Photodynamic therapy has been approved and successfully used in the United States, Japan and other countries for the clinical treatment of esophageal cancer, lung cancer, oral cancer, liver cancer and other malignant tumors. A photosensitizer is a chemical substance that can be concentrated in a pathological site and can produce a photochemical reaction under the excitation of light of an appropriate wavelength to destroy pathological target cells (or tissues). At present, the development of new photosensitizers with excellent properties such as low dark toxicity and strong phototoxicity has always been the key to the field of photodynamic therapy. [0003] Photofrin ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/498A61P35/00
Inventor 周志祥张立娜李泽琳闫红钟儒刚曾毅
Owner BEIJING UNIV OF TECH
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