Glaucocalyxin A derivative, preparation method and application thereof

A technology of cyanine A and its derivatives, which is applied in the direction of drug combinations, pharmaceutical formulas, medical preparations containing active ingredients, etc., and can solve the problems of unreported pharmacological effects

Inactive Publication Date: 2010-10-06
SUZHOU JINHAO MEDICINE DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Glaucocalyxin A derivative, preparation method and application thereof
  • Glaucocalyxin A derivative, preparation method and application thereof
  • Glaucocalyxin A derivative, preparation method and application thereof

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Effect test

Embodiment 1

[0066] The preparation of embodiment 1 cyanine A (GLA) derivative:

[0067] The chemical reagents used in the following preparation process are analytically pure unless otherwise specified.

[0068] Using fragrant tea herbs (aerial parts) as a raw material, purifying cyanine A (GLA), and modifying its structure with a polypeptide cNGQGEQc, to prepare a method for preparing cyanine A (GLA) derivatives, specifically comprising the following steps:

[0069] Step 1: Crush

[0070] Take fragrant tea and vegetable medicinal materials (aerial parts) and pulverize to 20 mesh to 50 mesh.

[0071] Step 2: Extract

[0072] Step 2.1: Mix the pulverized product obtained in step 1 with 95% ethanol (A.R.) at a volume ratio of 1:6 to 1:10, heat, reflux at 80°C to 90°C for 1 to 2 hours, extract and filter, An extract and a residue are obtained.

[0073] Step 2.2: Mix the residue obtained in step 2.1 with 95% ethanol (A.R.) at a volume ratio of 1:6 to 1:10, heat, reflux at 80°C to 90°C for ...

Embodiment 2

[0107] The preparation of embodiment two cyanine A (GLA) derivatives:

[0108] Adopt the following technical parameters to improve the preparation method of embodiment one:

[0109] In the step 2.1, the pulverized product is mixed with 95% ethanol (A.R.) in a volume ratio of 1:6.5, heated, refluxed at 82° C. for 1.8 hours, and then extracted and filtered.

[0110] In the step 2.2, the residue is mixed with 95% ethanol (A.R.) at a volume ratio of 1:9.5, heated, refluxed at 88° C. for 1.2 hours, extracted and filtered, and this step is repeated once.

[0111] In the step 3.1, the extract is heated and concentrated under reduced pressure at a temperature of 57°C.

[0112] In the step 3.2, the primary concentrate and water were mixed in a volume ratio of 1:8.5, stirred at room temperature and then left to stand for 11 hours before the supernatant and solid were separated.

[0113] In the step 3.3, the solid was mixed with ethyl acetate (A.R.) at a volume ratio of 1:5.5, stirred ...

Embodiment 3

[0130] Preparation of embodiment three cyanine calyxin (GLA) derivatives:

[0131] Adopt the following technical parameters to improve the preparation method of embodiment one:

[0132] In the step 2.1, the pulverized product is mixed with 95% ethanol (A.R.) at a volume ratio of 1:7.5, heated, refluxed at 84° C. for 1.6 hours, and then extracted and filtered.

[0133] In the step 2.2, the residue is mixed with 95% ethanol (A.R.) at a volume ratio of 1:8.5, heated, refluxed at 86° C. for 1.4 hours, extracted and filtered, and this step is repeated once.

[0134] In the step 3.1, the extract is heated and concentrated under reduced pressure at a temperature of 59°C.

[0135] In the step 3.2, the primary concentrate and water were mixed at a volume ratio of 1:8.5, stirred at room temperature and then allowed to stand for 10 hours to separate the supernatant and solid.

[0136] In the step 3.3, the solid was mixed with ethyl acetate (A.R.) at a volume ratio of 1:5.5, stirred and...

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Abstract

The invention discloses a glaucocalyxin A derivative, a preparation method and application thereof. The glaucocalyxin A (GLA) is used as a main body of the glaucocalyxin A (GLA) derivative which is a diterpenes substance and has an ent-kaurane structure, carbonyl, polypeptide cNGQGEQc and/ or hydroxyl. In the invention, rabdosia amethystoides medicinal material (part on the above-ground) is used as a raw material, and the preparation method of the derivative is as follows: crashing the raw material, extracting, treating solution, passing through a column, recrystallizing and carrying out other steps to obtain the glaucocalyxin A (GLA), and further carrying out acetylation on the glaucocalyxin A (GLA) and the polypeptide cNGQGEQc to obtain the glaucocalyxin A (GLA) derivative. The glaucocalyxin A (GLA) derivative has high anticancer activity, can significantly inhibit a plurality of tumor cells such as cells in lung cancer, liver cancer, nasopharyngeal carcinoma, lymphoma, melanoma and myelomatosis, especially has a targeting effect on the lung caner and can pertinently treat the lung caner.

Description

technical field [0001] The present invention relates to lamina (GLA) derivatives, in particular to lamina (GLA) derivatives containing polypeptides. [0002] The present invention also relates to the preparation method of the cyanine A (GLA) derivative containing the polypeptide and its application in treating cancer. Background technique [0003] Fragrant tea is a plant belonging to the family Lamiaceae, which is widely distributed in Henan, Hubei, Sichuan, Guizhou, Shaanxi, Shanxi, Hebei and other provinces. The whole herb has antibacterial and anti-inflammatory effects, and is used in the folk to treat acute jaundice hepatitis, acute cholecystitis, bruises, snake bites, impetigo, etc. Its pharmacological effects have not been reported. The pharmacological effect of the crude preparation of Hubei Xiangchacai was studied, and the results showed that it had obvious inhibitory effect on Ehrlich ascites carcinoma tumor cells in vivo and in vitro. [0004] Plants of the genu...

Claims

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Application Information

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IPC IPC(8): C07K7/06C07K7/08C07C49/743A61K38/08A61K38/10A61K31/122A61P35/00A61P35/02
Inventor 李云森陈子珺檀爱民程萍雷启福
Owner SUZHOU JINHAO MEDICINE DEV
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