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

A technology of carbazole alkaloids and Xanthomonas genus, which is used in the preparation of anti-tumor 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 The effect of good reproducibility, less sample loss and convenient operation

Inactive Publication Date: 2014-08-27
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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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] The preparation method and structure identification of carbazole alkaloids clausine D (1), 6-methoxyheptaphylline (2), mafaicheenamine C (3) and claulansine G (4) in the genus of yellow bark:

[0034] Take 27 kg of rhizome of yellow bark, dry and crush, extract 3 times with methanol reflux (100 L × 3 times) for 4 h, and concentrate the extract under reduced pressure to obtain 800 g of methanol extract; After suspending in water, fully extract with ethyl acetate and n-butanol successively, and extract three times with equal volume (30 L × 3 times). Recover the solvent to obtain 406 g ethyl acetate, 158 g n-butanol and 236 g 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 the following steps must be combined wi...

Embodiment 2

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

[0040] Experimental principle: The survival rate of tumor cells is detected after the drug and cells are co-cultured. Sulforhodamine B (Sulforhodamine B, SRB) is a water-soluble protein dye. The sulfonic acid anion in its molecule binds to the basic amino acid of the protein in the cell in a weakly acidic environment, and dissolves the cell with an alkaline solution. The SRB of SRB and its absorbance value are measured. From the content of SRB, the protein content in the cell can be known, and this represents the cell survival rate.

[0041] Experimental method: (1) Inoculation of cells: the above three types of tumor cells were made into a single cell suspension with a culture medium containing 10% fetal...

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

A pharmaceutical composition containing carbazole alkaloids clausine D (1), 6-methoxyheptaphylline (2), mafaicheenamine C (3) or claulansine G (4) as active ingredients. Their preparation methods, their application in the preparation of tumor cell growth inhibitors, and their application in the preparation of antitumor drugs.

Description

Technical field: [0001] The present invention belongs to the technical field of medicines, and in particular, relates to a pharmaceutical composition with carbazole alkaloids from a plant of the genus Huangpi as an active ingredient, a preparation method thereof, as a tumor cell growth inhibitor, and 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 is second only to cardiovascular diseases, which has become a major problem in the human medical field. According to a report recently published by the World Health Organization, in 28 industrialized countries, the death rate from cancer in men has increased by 55%, while that in women has increased by 40%. Gastric cancer ranks first, followed by esophageal cancer, liver cancer, cervical cancer, and bowel cancer. . With the development of molecular oncology, it has been found that the overexpression of pro-...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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