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Antineoplastic compound of red pineapple flower alkali A, preparation method and application thereof

A technology of piroline and compounds, applied in the field of anti-tumor alkaloid compound rubypine A and its preparation

Inactive Publication Date: 2008-08-20
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are not many studies on the chemical constituents of Red Pond, so we conducted a systematic study on the chemical constituents of Red Pond, in order to isolate natural products with good anti-tumor activity.

Method used

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  • Antineoplastic compound of red pineapple flower alkali A, preparation method and application thereof
  • Antineoplastic compound of red pineapple flower alkali A, preparation method and application thereof
  • Antineoplastic compound of red pineapple flower alkali A, preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Red Polo flower (Incarvillea delavay) whole herb 3kg, reflux extraction with 20L of 80% ethanol for 3 times, each time for 2 hours, combined extracts, concentrated under reduced pressure to obtain 60g extract, diluted with water, adjusted pH to 2-3. Filtrate to obtain the filtrate and filter residue, add 20% NaOH to the filtrate to adjust the pH to 11, extract with chloroform to obtain the chloroform fraction; concentrate the extracted fraction under reduced pressure to obtain 25 g of the crude product. Mix the crude product with 50 g of silica gel, add to the top of the installed silica gel column, and elute with the gradient of chloroform-acetone (20:1 to 2:1 by volume) system, collect the fraction containing Delavatine A, and pass through C18 reverse-phase column chromatography, eluted with methanol-water (50%-70% by weight), and detected by thin layer chromatography, obtained 212 mg of pure Delavatine A.

Embodiment 2

[0020] Embodiment 2: Cytotoxic activity experiment of Delavatine A

[0021] 1. Experimental materials

[0022] 1.1. Test samples

[0023] After Delavatine A was dissolved in DMSO (Merck), PBS (-) was added to make a 1000 μg / ml solution or a homogeneous suspension, and then diluted with DMSO-containing PBS (-).

[0024] 1.2. Cell lines

[0025] A549 (human lung cancer cells)

[0026] LOVO (human intestinal cancer cells)

[0027] 6T-CEM (Human T cell leukemia cells)

[0028] HL-60 (human leukemia cells)

[0029] HepG-2 (human liver cancer cells)

[0030] 1.3. Culture medium

[0031] RPMI1640+15%NBS+double antibody

[0032] 1.4. Other materials

[0033] Fully automatic microplate reader: model: WellscanMK-2, manufacturer: Labsystems

[0034] Imported 96-well culture plates, etc.

[0035] 2. Test method

[0036] MTT method: 4-6×10 4 cells / ml cell suspension 100 μl, set at 37°C, 5% CO 2 Inside the incubator. After 24 hours, add the sample solution, 10 μl / well, set up...

Embodiment 3

[0039] Embodiment 3: The curative effect experiment of Delavatine A on mouse S180 sarcoma (solid type)

[0040] 1. Experimental materials

[0041] 1.1 Test sample

[0042] Delavatine A was dissolved with a small amount of Tween-80 and then made into a solution with 0.5% CMC.

[0043] 1.2 Animals

[0044] Strain: Kunming mouse

[0045] Source: Provided by the Experimental Animal Center of Second Military Medical University.

[0046] Certificate number: Shanghai Donghe Zhengzi No. 107

[0047] Weight: 18-20g

[0048] Gender: female.

[0049] 1.3 Transplanted tumors

[0050] The mouse S180 sarcoma was maintained by the Shanghai Institute of Pharmaceutical Industry.

[0051] 2. Experimental method

[0052] Get the well-growing mouse S180 sarcoma ascites, dilute it 1:4 with normal saline, inoculate 0.2ml under the skin of each mouse armpit, divide into random groups, be divided into control group, cyclophosphamide group (CTX group, 20mg / kg, ip ×7), LID-15-1 (5mg / kg) group...

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Abstract

The invention pertains to the medical technology, in particular to an anti-tumor compound of incarvillea delavayi base A. The compound is a new alkaloid compound, which is extracted from the Chinese herbal medicine incarvillea delavayi. The precise mass number of the compound is 278.1546 (M plus H) <plus>, the molecular formula is C19H19NO by calculation; and the ultraviolet spectrum has strong absorption at 273nm and 249nm. Experiments show that the compound has good activity for inhibiting various tumor cells and can be used for the preparation of anti-tumor drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a new anti-tumor alkaloid compound Delavatine A (Delavatine A) isolated from the plant Red Pomme, a preparation method and application thereof. Background technique [0002] Tumor is one of the main causes of human death. The Ministry of Health of China announced the main causes of death of urban and rural residents in 2006. Statistics show that malignant tumors have become the leading cause of death. It can be seen that the prevention and treatment of tumors is very urgent. Drug therapy is one of the main treatments for tumors. At present, although dozens of anti-tumor drugs have been developed, they can effectively prolong the life of patients or improve the quality of life of patients. Some of these anti-tumor drug treatments have very significant curative effects, such as drug treatment of acute leukemia in children. However, the research and development of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D221/04A61K31/44A61K36/185A61P35/00
Inventor 张卫东沈云亨苏娟柳润辉李慧梁徐希科卢涛
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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