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Eremophil-2-internal-ester diploymer having function of inhibiting tumor cell growth activity and use thereof

A technology of ester dimer and erimofantane, which is applied in the field of natural medicinal chemistry and pharmacology, can solve the problems that the biological activity research has not been reported yet

Inactive Publication Date: 2007-08-29
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the chemical constituents and biological activity of Ligularia black purple

Method used

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  • Eremophil-2-internal-ester diploymer having function of inhibiting tumor cell growth activity and use thereof
  • Eremophil-2-internal-ester diploymer having function of inhibiting tumor cell growth activity and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1: Compound of formula (1): 8α-[Erimofantane-3′, 7′(11′)-diene-12′, 8′α; 15′, 6′α-dilactone]-Erimophane Preparation of fenane 3,7(11)-diene-12,8α; 15,6α-dilactone

[0016] The underground part of the sample was sun-dried and pulverized (dry weight 5.0 kg), then heated twice under boiling with 95% industrial alcohol, the extracts were cooled and combined, and concentrated under reduced pressure to obtain 389 grams of tan viscous primary extract. Suspension was made with distilled water and sequentially distributed and extracted with petroleum ether, ethyl acetate and n-butanol. After the organic layers were evaporated to dryness under reduced pressure, 26 g, 127 g, and 89 g were obtained respectively, and the aqueous layer was 147 g.

[0017] Take 120 grams of ethyl acetate extraction extract, mix it with 150 grams of 200-300 mesh silica gel to evaporate the solvent, then go through silica gel column chromatography (2500 grams), and use chloroform-methanol syst...

Embodiment 2

[0029] Pharmacological embodiment 2: Cytotoxic activity of formula (1) compound on BEL-7404 cells

[0030] BEL-7404 (human liver cancer) cells were cultured with RPMI1640 medium containing 10% fetal bovine serum, 100 U / mL penicillin and 100 U / mL streptomycin. cells in 5×10 per well 3 concentration into a 96-well plate at 37 °C with 5% CO 2 Incubate for 24 hours in a humidified incubator.

[0031] Determination of cell viability by the modified MTT method, the specific method is as in Pharmacological Example 1. Wherein formula (1) compound is to BEL-7404 cell half inhibitory concentration (IC 50 ) obtained from the dose-response curve.

[0032] IC of the compound of formula (1) 50 For: 2.55×10 -4 M; while the IC of the positive control cisplatin on BEL-7404 cells 50 2.62×10 -5 M.

[0033] Experimental conclusion: This experiment shows that the arimorphine dilactone dimer has strong cytotoxicity to BEL-7404 cells, and it may be developed into a new drug with anti-live...

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PUM

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Abstract

The invention relates to a new structure of bilactone dimer and the producing method, and the natural product selecting to human HL-60, CNE, KB, A549, BEL-7404 and Hela. It could be used to produce anti-tumor medicine.

Description

technical field [0001] The invention belongs to the technical field of natural medicinal chemistry and pharmacology. Specifically, the present invention relates to the preparation of an erimorphine dilactone dimer and the effect of the natural product on six kinds of human tumor cell lines such as human myeloid leukemia cells (HL-60), nasopharyngeal carcinoma cells (CNE ), oral epithelial cancer cells (KB), human lung cancer cells (A549), human liver cancer cells (BEL-7404) and human cervical cancer cells (Hela) tumor cell growth inhibitory activity screening. The natural product is found to have a certain activity of inhibiting tumor cell growth, and can be expected to be used as an antitumor drug. technical background [0002] At present, due to environmental pollution and other problems brought about by industrial development, the quality of human living environment is continuously declining, and the incidence and mortality of tumor diseases are also increasing. However...

Claims

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Application Information

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IPC IPC(8): C07D519/00A61K31/365A61P35/00C07D493/06
Inventor 李校堃施树云杨雷香孙莲莉梁广约阿施·史托克希特赵昱
Owner WENZHOU MEDICAL UNIV
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