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Anti tumor application of 3-carbonyl-20alpha-hydroxy-24-en-dammarane compound

A technology of dammarane and compound, which is applied in the field of anti-tumor use of 3-carbonyl-20α-hydroxy-24-ene-dammarane compound to achieve the effect of promoting Bax up-regulation, sufficient raw materials and obvious effect

Inactive Publication Date: 2009-11-04
FUJIAN AGRI & FORESTRY UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, the reported literature on the antitumor activity of compounds isolated from Panax notoginseng has not found the antitumor activity and apoptosis induction of triterpenoids on gastric cancer cell line SGC-7901 and liver cancer cell line BEL-7404. reports of death reactions

Method used

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  • Anti tumor application of 3-carbonyl-20alpha-hydroxy-24-en-dammarane compound
  • Anti tumor application of 3-carbonyl-20alpha-hydroxy-24-en-dammarane compound
  • Anti tumor application of 3-carbonyl-20alpha-hydroxy-24-en-dammarane compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment one: the preparation of compound A

[0035] 1. Preparation method

[0036] Weigh 5 kg of Panax notoginseng tuber, crush it and extract it 3 times with 70% ethanol under reflux at 55°C, filter off the insoluble matter, combine the extracts, concentrate under reduced pressure at 38°C to obtain the extract, and disperse the extract suspension in In cold water, the extract is divided into two parts, water-soluble and fat-soluble. Take the fat-soluble extract and pass it through a 200-300-mesh silica gel column through the eluent petroleum ether-acetone (10:3); then, repeatedly separate it on silica gel (10-40 μm) with the eluent n-hexaneacetone (10:1), Finally, it was separated by HPLC to obtain compound A.

[0037] 2. Test results

[0038] Compound A is solid and powdery, and the test data are as follows:

[0039] [α] 24 +41.2°(CHCl 3 c 0.58); IR: 3100 (C-H), 1710 (C=O) 1610 (C=C), 1384 and 1359 cm -1 ;EI-MS m / z: 442[M] + (C 30 h 50 o 2 )(6), 427[M-C...

Embodiment 2

[0040] Embodiment 2: MTT method detects compound A antitumor activity test

[0041] 1. Materials

[0042] 1.1 Culture medium

[0043] RPMI 1640 (Gibco BRL), calf serum (Hangzhou Sijiqing), penicillin and streptomycin (Sigma), trypsin (Beijing Tianxiangren Laboratories).

[0044] 1.2 Solvents and solutions

[0045] MTT (Xiamen Lulong Biological Company), DMSO (domestic analytical grade).

[0046] 1.3 Cell lines: human gastric cancer cell line SGC-7901, human liver cancer cell line BEL-7404.

[0047] 2. Operation steps:

[0048] Digested single-cell suspension, after counting, cells were seeded in 96-well flat-bottom culture plates at 180 μL / well, at 37°C in CO 2 Cultivate overnight in an incubator, add 20 μL / well of compound A solution and standard solution after bacterial filter treatment according to different concentrations, and incubate for 3 days. Pour off the culture medium and wash with PBS. Add MTT (0.2mg / L) 200μL / well, put in CO 2 Incubate at 37°C for 4 hours i...

Embodiment 3

[0057] Example 3: Detection of compound A-induced apoptosis of liver cancer cells

[0058] 1 material

[0059] Apoptotic Cell DNA Extraction Kit (TaKaRa).

[0060] Cell lines: human gastric cancer cell line SGC-7901, human liver cancer cell line BEL-7404.

[0061] 2 operation steps

[0062] (1) Cell inoculation, after culturing for 24 hours, compound A was added to 50 μg / mL.

[0063] (2) After continuing to culture for 12h, 24h, and 48h, the cells were digested with trypsin solution, centrifuged at 1000rpm / min for 5min in a centrifuge, and the cells of the test group and the control group were collected.

[0064] (3) Extract cell DNA according to the instructions of the apoptotic cell DNA extraction kit, and dissolve it with TE.

[0065] (4) Take 20 μL of DNA and load it on 1% agarose gel for electrophoresis detection.

[0066] 3 test results

[0067] Such as figure 1 As shown, the DNA fragments of the normal liver cancer cell DNA in the left figure are complete after b...

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Abstract

The invention relates to an application of 3-carbonyl-20alpha-hydroxy-24-en-dammarane compound for inhibiting gastric cancer cell SGC-7901 and hepatoma cell BEL-7404. Experiments show that 3-carbonyl-20alpha-hydroxy-24-en-dammarane compound can inhibit the proliferation of gastric cancer cell SGC-7901 and hepatoma cell BEL-7404 with an obvious effect and can be used to prepare antineoplastics. Electrophoresis detection shows that by increasing the expression quantity of apoptosis-related gene Bax, the 3-carbonyl-20alpha-hydroxy-24-en-dammarane compound can improve the apoptosis of hepatoma cell BEL-7404.

Description

Technical field [0001] The invention relates to an anti-tumor application of triterpenoids, in particular to the application of 3-carbonyl-20α-hydroxy-24-ene-dammarane compound to inhibit gastric cancer cell SGC-7901 and liver cancer cell BEL-7404. Background technique [0002] The 3-carbonyl-20α-hydroxy-24-ene-dammarane compound used in the present invention is extracted from the medicinal plant Panax notoginseng, and its chemical structural formula is as follows: [0003] [0004] Panax notoginseng is a unique medicinal plant in China, and it is only produced in the southwest of my country. The local folks have a long history of excavation and use. Traditional Chinese medicine believes that notoginseng is warm in nature, sweet and slightly bitter, enters the liver, stomach, and large intestine meridians, and can treat various bleeding disorders. Panax notoginseng, a rising star known 1,000 years later than ginseng, enjoys the reputation of "the most precious Chinese me...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61P35/00A61P1/00A61P1/16
Inventor 欧阳明安沈硕吴祖建谢联辉
Owner FUJIAN AGRI & FORESTRY UNIV
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