Thermosensitive cyclodextrin-based carbonic anhydrase inhibitor and preparation method thereof

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. ...

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Problems solved by technology

However, if the supramolecular interaction between the sulfonamide group and carbonic anhydrase is not destroyed, this inhibitory effect will always exist, and reversible activity regulation cannot be achieved.

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