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Application of mother-nucleus conjugated iridoid in preparing anti-tumor medicine

A technology of iridoids and anti-tumor drugs, which is applied in the field of medicine and can solve the problems of insufficient research on iridoid components and insufficient comprehensive and systematic research on chemical components.

Inactive Publication Date: 2009-06-03
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

[0004] Although the research on spider incense has reached a certain scale, the research on its chemical components is still not comprehensive and systematic, especially the research on the iridoids in it is not thorough enough.

Method used

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  • Application of mother-nucleus conjugated iridoid in preparing anti-tumor medicine
  • Application of mother-nucleus conjugated iridoid in preparing anti-tumor medicine
  • Application of mother-nucleus conjugated iridoid in preparing anti-tumor medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Preparation of iridoids conjugated to the mother nucleus

[0020] 25kg of dried spider incense medicinal material, crushed and extracted by percolation with 95% ethanol, the extract was decompressed to recover ethanol to a volume of 20L, filtered, the filtrate was extracted with petroleum ether, chloroform, ethyl acetate and n-butanol in sequence, and the extracted parts were collected And concentrated into an extract, wherein 120g of the extract is extracted with chloroform, and 180g of the extract is extracted with ethyl acetate. The obtained chloroform extraction fraction and ethyl acetate extraction fraction were subjected to silica gel column chromatography, gradient elution was carried out with different proportions of chloroform-methanol, and thin-layer chromatography was used for detection, and combined with Sephadex LH-20 and preparative liquid chromatography, the compounds were analyzed. Purified to obtain 42 compounds, using UV, MS, 1 H NMR, 13 C...

Embodiment 2

[0024] Embodiment 2: Cytotoxic activity experiment of the iridoid compound conjugated to the mother nucleus

[0025] 1. Experimental materials

[0026] 1.1. Test samples

[0027] After the nine iridoids described in Table 1 were dissolved in DMSO (Merck), add PBS (-)

[0028] Prepare 1000μg / ml solution or uniform suspension, and then dilute with DMSO-containing PBS(-).

[0029] 1.2. Cell lines

[0030] A549 (human lung cancer cells)

[0031] PC3 (human prostate cancer cells)

[0032] HCT-8 (human colon adenocarcinoma cells)

[0033] Bel 7402 (human liver cancer cells)

[0034] 1.3. Culture medium

[0035] RPMI1640+15%NBS+double antibody

[0036] 1.4. Other materials

[0037] Fully automatic microplate reader: model: WellscanMK-2, manufacturer: Labsystems

[0038] Imported 96-well culture plates, etc.

[0039] 2. Test method

[0040] MTT method: 4-6×10 4 cells / ml cell suspension 100μl, set at 37°C, 5% CO 2 Inside the incubator. After 24 hours, add the sample solu...

Embodiment 3

[0043] Example 3 Curative effect experiment of mother nucleus conjugated iridoid compound on mouse S180 sarcoma (solid type)

[0044] 1. Experimental materials

[0045] 1.1 Test sample

[0046] The nine iridoid compounds described in Table 1 were respectively dissolved with a small amount of Tween-80 and then formulated into solutions with 0.5% CMC.

[0047] 1.2 Animals

[0048] Strain: Kunming mouse

[0049] Source: Provided by the Experimental Animal Center of Second Military Medical University.

[0050] Certificate number: Shanghai Donghe Zhengzi No. 107

[0051] Weight: 18-20g

[0052] Gender: female.

[0053] 1.3 Transplanted tumors

[0054] The mouse S180 sarcoma was maintained by the Shanghai Institute of Pharmaceutical Industry.

[0055] 2. Experimental method

[0056]Take the well-growing mouse S180 sarcoma ascites, dilute it with normal saline at 1:4, inoculate 0.2ml under the skin of each mouse armpit, divide into random groups, and divide them into control...

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Abstract

The invention belongs to the medication technical field, in particular relates to application of a mother-nucleus conjugated iridoid in preparing anti-tumor medicine. Animal experiments proves the compound has obvious inhibiting effect to various cancer cells without toxic or side effect, so that the compound can be used for preparing the anti-tumor medicine. The invention further provides a medicine composition using the mother-nucleus conjugated iridoid as an active composition for treating tumor. The compound can either be extracted from plants, or obtained by a chemical synthesizing method.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of iridoid compounds conjugated with mother cores in the preparation of antitumor drugs. 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 tumor drugs is still facing great chall...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P35/00
Inventor 张卫东林生单磊苏娟柳润辉李慧梁沈云亨徐希科
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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