Chlorins e6-metal complex-lentinan ester and preparation method thereof

A technology of metal complexes and chlorphenes, which is applied in the directions of drug combinations, pharmaceutical formulations, medical preparations of inactive ingredients, etc., can solve problems such as no reports of metal complexes binding, and achieve good anti-tumor effects. effect of effect

Inactive Publication Date: 2018-10-16
桂林市兴达光电医疗器械有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] There is no report on the binding of lenti

Method used

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  • Chlorins e6-metal complex-lentinan ester and preparation method thereof
  • Chlorins e6-metal complex-lentinan ester and preparation method thereof
  • Chlorins e6-metal complex-lentinan ester and preparation method thereof

Examples

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Effect test

Embodiment 1

[0028] Under the condition of protective gas and light avoidance, the copper complex of chlorin e6 (Chlorin e6, Ce6) is dissolved in ultrapure water, which is A. Lentinan was dissolved in hot water at 50-80 degrees, then A was added, and the reaction was carried out under stirring at room temperature for 36 hours; the chlorin e6 (Chlorin e6, Ce6) metal complex and the lentinan were in equimolar amounts.

[0029] After centrifugation, the supernatant was dialyzed against deionized water and freeze-dried.

[0030] The dry matter is separated by silica gel column chromatography, and the eluent is a mixed solution of dichloromethane / methanol with a volume ratio of 3 / 7 to 7 / 3;

[0031] After dichloromethane / methanol is evaporated, dissolve with methanol or acetonitrile, refine and purify with reverse phase column chromatography, the eluent is methanol / water mixed solution or acetonitrile / water mixed solution; the filler used in the reversed phase column is C 18 ; The volume ratio ...

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PUM

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Abstract

The invention discloses chlorins e6-metal complex-lentinan ester which is prepared by esterification reaction of lentinan and a chlorins e6-metal complex. The lentinan serving as a polar end dissolvable in water enables the chlorins e6-metal complex-lentinan ester to be dissolvable in water, so that the problem of low water solubility of Ce6 is solved; the chlorins e6-metal complex-lentinan esterhas double anti-tumor effects of the chlorins e6 and the lentinan, belongs to a photoacoustic dynamic therapy drug, and can be used for preparing a drug for treating dermatosis, malignant tumors or carcinomatous pleural effusion, gastric ulcer and iron-deficiency anemia and preparing a liver-protecting drug.

Description

technical field [0001] The invention relates to light and sound dynamic therapy drugs, in particular to chlorin e6 metal complex-lentinan ester. Background technique [0002] Chlorin e6 (Chlorin e6, Ce6), dark green powder, very hygroscopic and easy to oxidize. Insoluble in water, soluble in acetone, tetrahydrofuran, ethanol. [0003] Chlorin e6 has certain photosensitivity and thermosensitivity, so chlorin e6 is not only a photosensitizer, but also a potential sound sensitizer. It has an absorption wavelength of 663nm, can generate more ROS (reactive oxygen species), and is non-toxic, has high selectivity for tumor tissue and high clearance rate for non-tumor tissue, and has less side effects on the skin, so it is suitable for use in tumors Light and sound dynamic therapy. However, Ce6 has poor water solubility, which limits its clinical development and application. [0004] The metal complex of chlorin e6 is a derivative of chlorin e6, which has the same characteristic...

Claims

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Application Information

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IPC IPC(8): C08B37/00A61K41/00A61K47/55A61P35/00A61P17/12A61P17/10A61P17/00A61K31/715
CPCA61K31/715A61K41/0071A61K47/55A61P17/00A61P17/10A61P17/12A61P35/00C08B37/0024A61K2300/00
Inventor 陈志强
Owner 桂林市兴达光电医疗器械有限公司
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