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Sesquiterpenoid compound from seaweed as well as preparation method and purpose thereof

A technology of sesquiterpenoids and compounds, which is applied in the field of preparation of drugs for the prevention and/or treatment of type II diabetes, can solve the problems of small side effects, threat to human health, inestimable personnel and economic losses, etc., and achieve the effect of easy preparation and acquisition

Inactive Publication Date: 2017-09-19
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a developing country active on the world stage with a large population, China currently has about 50 million diabetics, and there is an upward trend, which seriously threatens human health. The human and economic losses caused by diabetes in the future will be immeasurable In addition, there is no drug for treating diabetes with independent intellectual property rights in China. Therefore, it is still a research hotspot to find diabetes drugs with independent intellectual property rights in my country that have good activity and few side effects.

Method used

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  • Sesquiterpenoid compound from seaweed as well as preparation method and purpose thereof
  • Sesquiterpenoid compound from seaweed as well as preparation method and purpose thereof
  • Sesquiterpenoid compound from seaweed as well as preparation method and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Preparation of seaweed sesquiterpenoids:

[0035] (1) Cut the frozen marine red algae S. Okamura into pieces, soak and extract 4 times with acetone, combine the extracts and concentrate under reduced pressure, then extract with anhydrous ether until the supernatant is nearly colorless, and extract the extracts Concentrate to obtain anhydrous ether extract;

[0036] (2) The anhydrous ether extract in step (1) is subjected to silica gel column chromatography (200-300 mesh, Qingdao Ocean Chemical Co., Ltd.), and gradient elution is performed with an organic solvent, and the eluted components are collected;

[0037] (3) The collected eluted fractions were subjected to 1 gel column chromatography (GE-Healthcare company, ephadex LH-20, hydroxypropyl sephadex, 17-0090-02, 500 g) and 1 gel column chromatography respectively. Purify by silica gel column chromatography (500-600 mesh, Qingdao Ocean Chemical Co., Ltd.) once or twice to obtain compounds 1-5.

[0038]In step (2), c...

experiment example 2

[0050] Experimental example 2: Compound inhibits PTP1B activity test

[0051] 1) Material: PTP1B, obtained from laboratory purification, reference Biochim Biophys Acta, 2006, 1760, 1505-1512.

[0052] Substrate: pNPP (disodium p-nitrophenylphosphate)

[0053] 2) Process: the enzyme activity is detected in a 96-well or 384-well flat-bottomed transparent microwell plate by light absorption detection method. The free product obtained by the hydrolysis of the substrate pNPP by PTP1B has a strong light absorption at 405nm. The change of light absorption intensity at 405 nm was monitored by a microplate reader, and the initial reaction velocity was calculated. The control compound used in the experiment was oleanolic acid.

[0054] 3) Sample treatment: the sample was dissolved in DMSO, stored at low temperature, and the concentration of DMSO in the final system was controlled within the range that did not affect the detection activity.

[0055] 4) Data processing and result desc...

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Abstract

The invention relates to the technical field of medicines, and particularly speaking, discloses a sesquiterpenoid compound from seaweed as well as a preparation method and a purpose thereof. The sesquiterpenoid compound provided by the invention is of a structure as shown in the following general formula I. The preparation method of the sesquiterpenoid compound comprises the following steps of cleanly flushing marine laurencia okamurai through seawater, then freezing, cutting up, carrying out percolation extraction, and obtaining a monomeric compound through multiple separation means. Such a compound belongs to a natural organic small molecular compound, and is indicated through in-vitro detection to have more obvious activity of being resistant to protein tyrosine phosphatase 1B. The sesquiterpenoid compound can provide a lead compound for researching and preparing a novel medicine for being resistant to type-II diabetes, and has the important significance for developing and utilizing a Chinese marine biological resource.(The structural formula of the sesquiterpenoid compound is shown in the description).

Description

technical field [0001] The invention belongs to the technical field of medicine. Specifically, it relates to two compounds isolated from seaweed in the East China Sea, their preparation methods and new applications, especially their application in the preparation of drugs for preventing and / or treating type II diabetes. Background technique [0002] Diabetes is a common and frequently-occurring disease, and has become the second killer of modern diseases. Its harm to the human body is second only to cancer. The World Health Organization has listed diabetes as one of the three difficult diseases. Diabetes is a group of metabolic diseases characterized by hyperglycemia. Hyperglycemia is caused by defective insulin secretion or impaired biological action, or both. Diabetes is long-standing hyperglycemia, which leads to chronic damage and dysfunction of various tissues, especially the eyes, kidneys, heart, blood vessels, and nerves. Diabetes is divided into type I diabetes an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/93C07C39/42C07C37/70C07C37/82A61P3/10
CPCC07C37/685C07C37/70C07C37/82C07C39/42C07D307/93
Inventor 郭跃伟李佳李晓露盛丽龚景旭
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI