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Eremophil dilactone natural product with tumour cell growth inhibiting activity

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

Inactive Publication Date: 2006-10-25
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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 dilactone natural product with tumour cell growth inhibiting activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: the preparation of formula (1) compound

[0021] Obtain 89.0 grams of ethyl acetate extract from 5.0 kilograms of dried Lignus sinensis. The extract was chromatographed on 800 g of 100-200 mesh silica gel column, and chloroform-methanol (50:0-0:1) gradient eluted. Thin-layer chromatography detects that the same fractions are combined, and the partial extract containing the compound of formula (1) is purified through 16 grams of silica gel H (60-90° petroleum ether-ethyl acetate 4: 1-2: 1), followed by Purified by Sephadex LH-20 column chromatography (eluted with methanol) to finally obtain the compound of formula (1) (19 mg). Colorless needle crystal, melting point: 233-235℃; [α] D 20 : +29.0°(chloroform; c0.30,); UVλ max (CHCl 3 ) nm: 223; 1772, 1756, 1681; Electrospray mass spectrometry ESI-MS (m / z): 259 [M+H] + ; High-resolution electrospray mass spectrometry HR-ESI-MS (m / z): 259.0936 (Calc.for [C 15 h 16 o 4 +H] + 259.0926); 13 C and 1 HN...

Embodiment 2

[0032] Pharmacological Example 2: Cytotoxic Activity of Formula (1) Compounds on BEL-7404 Cells

[0033] BEL-7404 (human liver cancer) cells were cultured with RPMI 1640 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.

[0034] Cell viability was measured by the improved MTT method, and the specific method was 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.

[0035] IC of the compound of formula (1) 50 For: 1.44×10 -4 M; while the IC of the positive control cisplatin on BEL-7404 cells 50 1.50×10 -5 M.

[0036] Experimental conclusion: This experiment shows that the arimorphine dilactone compound has strong cytotoxicity to BEL-7404 cells, and it may be developed into a new drug with anti-liv...

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Abstract

This invention relates to Ailinofen bi lactone and its medical used salt or solvate. This invention also relates its preparation method and its medical combination and medical application. The compound in this invention can in vitro prevent two kinds of human body tumor cells activity as oral epithelium cancer cell (KB) and human hepatic carcinoma cell (BEL-7404). It can be developed as anti tumor medicine application.

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 natural product and the inhibition of the natural product on the growth of two human tumor cell lines oral epithelial carcinoma cells (KB) and human liver cancer cells (BEL-7404) active 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, the selectivity of cytotoxic antineoplastic drugs currently used in clinical practice is not high, resulting in malignant killing of normal cells, which limits ...

Claims

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Application Information

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IPC IPC(8): C07D493/06A61K9/00A61K31/365A61P35/00
Inventor 赵昱黄可新施树云王晓雨杨柳青汤淙淙杨雷香
Owner WENZHOU MEDICAL UNIV
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