Thermosensitive cyclodextrin-based carbonic anhydrase inhibitor and preparation method thereof

A technology of carbonic anhydrase and cyclodextrin, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas. It can solve problems such as inability to achieve activity regulation, and achieve low toxicity and good application. Prospects, low-cost effects

Active Publication Date: 2017-06-13
SHANGHAI UNIV
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

However, if the supramolecular interaction between the sulfonamide group and carbonic anhydrase is not...

Method used

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  • Thermosensitive cyclodextrin-based carbonic anhydrase inhibitor and preparation method thereof
  • Thermosensitive cyclodextrin-based carbonic anhydrase inhibitor and preparation method thereof
  • Thermosensitive cyclodextrin-based carbonic anhydrase inhibitor and preparation method thereof

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Embodiment Construction

[0041] Preferred embodiments of the present invention are described in detail as follows:

[0042] 1. Test of compound phase transition temperature

[0043] The temperature-sensitive cyclodextrin inhibitor is dissolved in water. Since the alkoxy ether has temperature-sensitive behavior, once heated to a certain temperature, its aqueous solution will become turbid, and the solution will return to a clear state after cooling down. The phase transition process in neutral aqueous solution was tracked by temperature-variable UV / vis. The turbidity phase transition curves of different concentrations of thermosensitive cyclodextrin inhibitors were measured as follows: figure 1 shown. When the concentration is 100μM, the phase transition temperature of the thermosensitive cyclodextrin inhibitor is 32℃.

[0044] 2. Testing of Enzyme Activity

[0045] Carbonic anhydrase can catalyze the hydrolysis reaction of esters, so it can be used to indirectly react the enzyme activity. With p-ni...

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Abstract

The invention discloses a thermosensitive cyclodextrin-based carbonic anhydrase inhibitor and a preparation method thereof. In the inhibitor, a natural small-molecule inhibitor with a sulfonamide group is modified onto thermosensitive cyclodextrin with temperature response, an inhibitory effect on carbonic anhydrase is achieved through the sulfonamide group, and the reversible regulation of the activity of carbonic anhydrase is achieved through the thermosensitive effect of an alkoxy ether chain. When temperature is below a phase-transition temperature, the alkoxy ether chain stretches, the sulfonamide group can have good supramolecular interaction with carbonic anhydrase, and thereby the activity of carbonic anhydrase is inhibited. When temperature is above the phase-transition temperature, because the alkoxy ether chain is dehydrated to collapse to generate powerful steric resistance, destroying the supramolecular interaction between the sulfonamide group and carbonic anhydrase, and thereby the activity of the enzyme recovers again. Moreover, compared with other carbonic anhydrase inhibitors, the thermosensitive cyclodextrin-based carbonic anhydrase inhibitor is lower in toxicity and wider in resource, thus having high application value in the field of biomedical materials.

Description

technical field [0001] The invention relates to a carbonic anhydrase inhibitor based on a thermosensitive cyclodextrin and its preparation method and application. Background technique [0002] In recent years, carbonic anhydrase inhibitors have received extensive attention. Carbonic anhydrase is a ubiquitous metalloenzyme that can be found in almost all organisms. Some studies have shown that carbonic anhydrase plays an important physiological role in the human body, participates in biochemical reactions in the body's gas transport, acid-base regulation, and tissue secretion, and plays an important role in maintaining the stability of the internal environment. The most important physiological role is to catalyze the reversible hydration of carbon dioxide: H 2 O + CO 2 ←→ H 2 CO 3 ←→ HCO 3 - +H + . However, in some cases, excessive carbonic anhydrase activity has also brought some diseases to people, such as glaucoma, macular degeneration, osteoporosis and so on. ...

Claims

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Application Information

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IPC IPC(8): A61K31/724A61K47/61C08B37/16A61P19/10A61P27/02A61P27/06
Inventor 张阿方史晃祝润朗徐刚董庆豪闫家涛刘坤
Owner SHANGHAI UNIV
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