Medicine composition with carbazole alkaloid in clausena plants as antineoplastic activity ingredient and preparation method and application thereof

A technology for carbazole alkaloids and compositions, which is applied in the preparation of antitumor drugs, the field of tumor cell growth inhibitors, can solve the problems of easy adsorption of samples, insufficient sensitivity, easy loss of samples, etc., and achieves controllability and reproducibility. The effect of good performance, less sample loss and convenient operation

Inactive Publication Date: 2013-03-27
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The disadvantage of this method is that the thin-layer preparation plate is only suitable for trace components, and it is easy to adsorb samples
[0007] The above methods focus on the use of normal-phase silica gel, and almost no reverse-phase silica gel is used, which is easy to lose samples; the single TLC detection method is not sensitive enough, it is not easy to detect trace components, and does not make full use of the strong ultraviolet absorption characteristics of carbazole alkaloids

Method used

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  • Medicine composition with carbazole alkaloid in clausena plants as antineoplastic activity ingredient and preparation method and application thereof
  • Medicine composition with carbazole alkaloid in clausena plants as antineoplastic activity ingredient and preparation method and application thereof
  • Medicine composition with carbazole alkaloid in clausena plants as antineoplastic activity ingredient and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Preparation and structural identification of carbazole alkaloids clausine D (1), 6-methoxyheptaphylline (2), mafaicheenamine C (3) and claulansine G (4) from plants of the genus Pampas:

[0034]Take 27 kg of rhizomes of Wampucum japonica, after drying and crushing, reflux extraction with methanol for 3 times (100 L × 3 times) for 4 h, and concentrate the extract under reduced pressure to obtain 800 g of methanol extract; After adding water to suspend, extract fully with ethyl acetate and n-butanol successively, and extract three times with equal volumes (30 L × 3 times), recover the solvent to obtain 406 g of ethyl acetate, 158 g of n-butanol and 236 g of water . The ethyl acetate part was subjected to silica gel column chromatography, eluted with 100:0, 95:5, 90:10 chloroform / methanol gradient, thin layer chromatography, combined with TLC detection method, according to the different polarity of carbazole alkaloids Combined into seven components Fr.1 - Fr.7; each of th...

Embodiment 2

[0039] Cytotoxicity test results of clausine D (1), 6-methoxyheptaphylline (2), mafaicheenamine C (3) and claulansine G (4) of the present invention on tumor cells BGC-823, HeLa and A549. The experimental principles, methods and results are as follows:

[0040] Experimental principle: After the co-culture of drugs and cells, the survival rate of tumor cells is detected. Sulforhodamine B (SRB) is a water-soluble protein dye. The sulfonate anion in its molecule binds to the basic amino acid of intracellular protein in a weakly acidic environment, and dissolves the intracellular substance with alkaline solution. SRB and measure its absorbance value, the protein content in the cell can be known from the content of SRB, and this represents the cell survival rate.

[0041] Experimental method: (1) Cell inoculation: The above three tumor cells were prepared into a single cell suspension with a culture medium containing 10% fetal bovine serum, and 5×10 cells were used for each well. ...

Embodiment 3

[0047] Compound 1-4 obtained in Example 1 was added with 4% sulfuric acid ethanol solution, pH = 4, filtered, and dried to prepare sulfate compound 1-4.

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Abstract

Provided is a medicine composition with carbazole alkaloid clausine D(1), 6-methoxyheptaphylline (2) and mafaicheenamine C (3) or claulansine G (4) as active ingredients. The invention further provides a preparation method of the medicine composition, application of the composition in preparation of tumor cell growth inhibitor and application of the composition in preparation of antineoplastic medicine.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, in particular, it relates to a pharmaceutical composition using carbazole alkaloids in plants of the genus Pseudomonas as an active ingredient, its preparation method, its use as a tumor cell growth inhibitor, and its application in the preparation of antitumor drugs . Background technique: [0002] In today's world, tumors are a serious threat to human health and life, and its mortality rate ranks second only to cardiovascular diseases, which has become a major problem in today's human medical field. According to a report recently published by the World Health Organization, in 28 industrialized countries, the cancer mortality rate of men has increased by 55%, and that of women has increased by 40%. Among them, gastric cancer ranks first, followed by esophageal cancer, liver cancer, cervical cancer and intestinal cancer. . With the development of molecular oncology, it has been found that th...

Claims

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Application Information

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IPC IPC(8): A61K31/403A61P35/00A61P1/00A61P15/00A61P11/00C07D209/88C07D209/94
Inventor 谭宁华宋卫武曾广智彭文文
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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