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Xanthenone dimer compound IUE-1799a use

A technology of xanthone dimer and iue-1799a, which can be applied to medical preparations containing active ingredients, antibacterial drugs, organic active ingredients, etc., and can solve problems such as penicillin resistance

Active Publication Date: 2016-04-20
INST OF URBAN ENVIRONMENT CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the widespread use of penicillin, some Staphylococcus aureus can produce penicillinase and hydrolyze the β-lactam ring, showing resistance to penicillin

Method used

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  • Xanthenone dimer compound IUE-1799a use
  • Xanthenone dimer compound IUE-1799a use
  • Xanthenone dimer compound IUE-1799a use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: Preparation and identification of compound xanthone dimer compound IUE-1799a

[0027] Take 2 kg of the bark part of Bamboo basilica, dry it, soak it in 10L ethyl acetate overnight, repeat it three times, combine the ethyl acetate extracts, filter, and concentrate under reduced pressure to obtain 210 g of the total crude extract extract. The obtained extract was mixed with silica gel (100 mesh) and subjected to normal pressure silica gel (200-300 mesh) column chromatography, using chloroform-methanol as the eluting solvent, and performing gradient elution from 90:10 to 40:60, wherein Gradient elution components that can be developed in thin layer chromatography with a chloroform-methanol-0.1% formic acid aqueous solution system with a volume ratio of 100:20:2 are purified by a medium-pressure reversed-phase column (60 μm), and then passed through SephadexLH -20 column purification, eluting with methanol, 10ml of eluent as a tube, collecting 15 tubes, picking t...

Embodiment 2

[0029] Embodiment 2: antibacterial activity experiment

[0030] The resazurin chromogenic method was used as the method for detecting the activity. The principle of the resazurin chromogenic method is that lactate dehydrogenase in living cells can convert resazurin (blue) into the fluorescent substance resorufin (pink red) to generate a fluorescent signal. Resorufin will continue to be reduced by the cells to the non-fluorescent substance dihydroresazurin (white), which will decrease the fluorescent signal, and inactive or dead cells will lose their metabolic capacity and cannot restore resazurin, so they will not be able to produce fluorescence Signal, so this method can specifically detect active cells.

[0031] The antibacterial experiment was performed in a 96-well plate, and the color in the 96 wells was blue, indicating that the sample had inhibitory activity against the target strain; the color in the 96 wells was pink or red, indicating that the sample had no inhibito...

Embodiment 3

[0067] Embodiment 3: Cytotoxicity experiment

[0068] In this embodiment, an in vitro cytotoxicity test is used to determine the survival rate of human or mouse cancer cells cultured in vitro after adding IUE-1799a.

[0069] The selected cell lines are: human non-small cell lung cancer H1299, A549, human large cell lung cancer H460, human small cell lung cancer H446, mouse melanoma B16, B16-F10, human breast cancer MD-MBA-231, MCF7, human gastric cancer MGC803 , human pancreatic cancer PANC-1, human cervical cancer HeLa, human osteosarcoma U2OS, human liver cancer HepG2, human colon cancer HCT116, and human laryngeal cancer HEP2. Use the MTT method to determine the half-inhibitory concentration IC when the survival rate (or death rate) of each tumor cell is 50%. 50 (The above cells can be purchased from ATCC). MIC is the minimum inhibitory concentration.

[0070] The test results are shown in Table 2.

[0071]

[0072] It can be seen from Table 2 that IUE-1799a h...

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Abstract

The present invention discloses xanthone dimer compouns IUE-1799a use, specifically antibacterial use such as use to inhibit growth of methicillin-resistant staphylococcus aureus, and xanthone dimer compouns IUE-1799a has no significant cytotoxicity to a variety of cell lines, and can be used for the preparation of antibacterial agents.

Description

technical field [0001] The invention relates to the antibacterial field of compounds, in particular to the antibacterial use of the xanthone dimer compound IUE-1799a. Background technique [0002] Herbal medicines have been used for quite a long time in human history. With the development of human civilization and science and technology, chemical medicine once squeezed herbal medicine into the edge of market application. Nowadays, when people are weighing and choosing the quick-acting effects of chemical drugs and the pain caused by serious side effects, plant medicine once again comes to pharmacologists and patients with its concept of returning to nature. Finding exotic antibacterial drugs from plants has a broad space for development and application. [0003] Staphylococcus aureus is a clinically common and highly toxic bacterium. Since the advent of penicillin in the 1940s, infectious diseases caused by Staphylococcus aureus have been largely controlled. However, with...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P31/04
Inventor 王伟毅蔡澎廖艳艳
Owner INST OF URBAN ENVIRONMENT CHINESE ACAD OF SCI
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