A method for rapid screening of topoisomerase I inhibitors in natural products

A technology for topoisomerase and natural products, applied in the field of natural product analysis, can solve the problems of inability to provide detailed characteristics of protein-ligand interactions, false negatives, etc., and achieve fast sample analysis, strong specificity, and spectral information. large amount of effect

Active Publication Date: 2017-04-19
WUHAN BOTANICAL GARDEN CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, spectroscopic methods are prone to false negative and false positive results due to background interference; NMR detection process cannot provide detailed features of protein-ligand interactions in rapid exchange reactions, etc.

Method used

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  • A method for rapid screening of topoisomerase I inhibitors in natural products
  • A method for rapid screening of topoisomerase I inhibitors in natural products
  • A method for rapid screening of topoisomerase I inhibitors in natural products

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Experimental program
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Effect test

Embodiment 2

[0143] The topoisomerase I inhibitor is a natural product extract or its monomer compound; the natural product Lycoris alkaloid extract of the present invention comprises the following steps:

[0144] ① Preparation of samples to be tested

[0145] Accurately weigh an appropriate amount of the sample to be tested, use the buffer solution prepared in Example 1 to fully dissolve, and the final concentration of the solution to be tested is 2.0 mg / ml;

[0146] Described sample to be tested is Lycoris alkaloid extract;

[0147] ② Preparation of standard solution

[0148] The internal standard sample was prepared into a standard stock solution with a concentration of 100 μg / ml with acetonitrile, and added to the sample solution to be tested before mass spectrometry detection, with a final concentration of 5 μg / ml;

[0149] Described internal standard sample is lotus leaf base;

[0150] ③ Binding reaction of the sample to be tested with normal and inactive topoisomerase I

[0151]...

Embodiment 3

[0174] "Chinese Pharmacopoeia", 2015 edition, stipulates that the total amount of diosgenin compounds diosgenin I and II and peninoside compounds diosgenin VI and VII in Chonglou medicinal materials shall not be less than 0.6% as a measure of its medicinal value. index. Zhongzhonglou in traditional Chinese medicine is often composed of prescriptions for the treatment of tumors, such as esophageal cancer, laryngeal cancer, rectal cancer, lung cancer, cervical cancer, leukemia, etc. However, there are few studies on the anti-tumor targets of Chonglou and its main medicinal components.

[0175] The topoisomerase I inhibitor is a natural product extract or its monomeric compound; the topoisomerase I inhibitor described in this embodiment is the monomeric compound trilobites I, II, VI and VII;

[0176] ① Preparation of samples to be tested

[0177]Accurately weigh an appropriate amount of the sample to be tested, first dissolve it with a small amount of dimethyl sulfoxide, and th...

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Abstract

The invention discloses a method for fast screening a topoisomerase I inhibitor from a natural product, and relates to the analysis field of natural products. The method comprises the following steps of: (1) preparation of an enzyme binding reaction buffer solution; (2) preparation of a to be detected sample; (3) preparation of a standard solution; (4) binding reaction of the to-be-detected sample and normal and inactive topoisomerase I; (5) chromatography-mass spectrometry detection analysis of reaction sample; and (6) enrichment ratio of the topoisomerase I to the inhibitor. The ultrafiltration membrane technology and the chromatography-mass spectrometry united technology united method are applied to the screening of the topoisomerase I inhibitor, the sample analysis speed is fast and the specificity is strong so as to conveniently recognize a medicine ligand combined with a biological target molecule; meanwhile, the sample analysis dosage is less, and the spectrogram information quantity is large so as to realize the fast screening of the lead compound, the method has great advantage on the aspect of researching mutual effect of medicine small molecule ligand and biological macromolecule receptor; the method is suitable for analyzing in-vitro enrichment ratio of the natural product extract or monomer compound to the topoisomerase I inhibitor.

Description

[0001] Field of Invention [0002] The invention relates to the field of natural product analysis, in particular to a method for rapidly screening topoisomerase I inhibitors in natural products; A method for rapid screening of topoisomerase I inhibitors in compounds or their monomeric compounds. Background technique [0003] DNA topoisomerase I is an essential enzyme widely present in prokaryotic and eukaryotic organisms. The tyrosyl residue in its catalytic site attacks the DNA single strand, making the enzyme and DNA 3'-phosphodiester bond to form a covalent bond. Valence connection, resulting in DNA single-strand breaks, thereby affecting DNA topology by regulating supercoiling, linkage, unlinking, and nucleic acid unbinding. Targeted drugs are the most advanced drugs currently used in cancer treatment, which prevent the growth of tumor cells by interacting with specific targets necessary for tumorigenesis and growth. Studies have found that topoisomerase expresses a high...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): G01N30/88
CPCG01N30/88G01N2030/027G01N2030/884
Inventor 郭明全陈桂林田永强张春云
Owner WUHAN BOTANICAL GARDEN CHINESE ACAD OF SCI
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