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A new application of 2,6-disubstituted pyridine-4-thiocarboxamide

A technology of dithiocarboxamide and thiocarboxamide, applied in the field of medicine, can solve the problems such as the inhibitory effect that has not yet been reported

Active Publication Date: 2021-01-08
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the inhibitory effect of 2,6-disubstituted pyridine-4-carbothioamide on hTAS2R38 bitter taste receptor has not been reported yet

Method used

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  • A new application of 2,6-disubstituted pyridine-4-thiocarboxamide
  • A new application of 2,6-disubstituted pyridine-4-thiocarboxamide
  • A new application of 2,6-disubstituted pyridine-4-thiocarboxamide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1, Inhibition of the Function of Bitter Taste Receptor hTAS2R38 by 2-Propylpyridine-4-thiocarboxamide

[0025] PROP is an agonist of bitter taste receptor hTAS2R38, which can stimulate and activate bitter taste receptors, resulting in changes in calcium ion concentration in cells. Fluo4-AM is an acetyl methyl ester derivative of Fluo4, which can easily enter cells through culture. After AM enters the cell, it will be hydrolyzed by intracellular esterase, and the resulting Fluo4 will then react with calcium ions (Ca 2+ ) bind and fluoresce. In this study, HEK293T cells transfected and expressing bitter taste receptors were stimulated with PROP alone or PROP and 2-propylpyridine-4-carbothioamide (PROP+3), and the immediate fluorescence changes were obtained by fluorescence microscopy.

[0026] In this study, the expression vector of the bitter taste receptor hTAS2R38 was constructed, and the first 39 amino acid residues sequence of rhodopsin N-terminal and hTAS2...

Embodiment 2

[0032] Example 2, Sensory evaluation of 2-propylpyridine-4-carbothioamide for inhibiting bitterness

[0033] This study verified the inhibitory effect of bitter receptor inhibitors on bitter taste through the human body's sense of bitter taste. 20 healthy volunteers (10 males and 10 females) were selected from the research group as subjects. These people need to be interested in sensory evaluation experiments and be able to treat sensory evaluation experiments objectively and fairly. Language expression ability and basic sensory discrimination ability, signed an informed consent form before the experiment.

[0034] Prepare bitter substance and bitter inhibitor solution. Bitter substances and their concentrations: Potassium chloride, sodium saccharin, caffeine, quinine hydrochloride, artificial bezoar (commercialized product, not pure), refer to the amount specified in the food additives and the different bitterness intensity of the substance itself to set the above five kinds...

Embodiment 3

[0039] Example 3, Inhibition of the Function of Bitter Taste Receptor hTAS2R38 by 6-Methylpyridine-2,4-Dithiocarboxamide

[0040] In this study, HEK293T cells transfected and expressing bitter taste receptors were stimulated with PROP alone or with PROP and 6-picoline-2,4-dithiocarbamide (PROP+5).

[0041] The research method is similar to Example 1.

[0042] The difference from Example 1 is that 2-propylpyridine-4-carbothioamide is replaced by 6-methylpyridine-2,4-dithiocarboxamide.

[0043] Depend on Figure 4 with Figure 5 It can be known that 6-picoline-2,4-dithiocarboxamide inhibits the function of bitter taste receptor hTAS2R38. Figure 4 It can be seen that 6-picoline-2,4-dithiocarboxamide can significantly inhibit the change of intracellular calcium ion concentration caused by PROP, and its inhibition rate reaches 66.0%, indicating that 6-picoline-2,4 - Dithioformamide has a good inhibitory effect on bitter taste receptors. Figure 5 It can be seen that 6-methylp...

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Abstract

The invention belongs to the technical field of medicines and the field of foods and particularly relates to a novel application of 2,6-disubstituted pyridine-4-thioformamide to preparation of a bitterness inhibiting drug or food. The invention firstly discloses that 2,6-disubstituted pyridine-4-thioformamide has an effect on inhibiting a bitterness receptor hTAS2R38 and is obvious in inhibiting effect. 2,6-disubstituted pyridine-4-thioformamide disclosed by the invention can be applied to the preparation of the bitterness inhibiting drug alone, can also be used as a drug preparation additive to be compounded to form a composition for reducing the bitterness of a drug and can be prepared into any one of dosage forms including a tablet, powder, an oral solution or a spray and the like suitable for clinic use. Meanwhile, 2,6-disubstituted pyridine-4-thioformamide can also be used as a food additive for regulating the taste of the food.

Description

technical field [0001] The invention belongs to the technical field of medicine and food, and specifically relates to a new application of 2,6-disubstituted pyridine-4-carbothioamide in preparing bitter taste suppressing medicine or food. Background technique [0002] Bitterness is one of the basic tastes of the human body. In recent years, due to the improvement of consumers' health awareness, various foods and beverages with functional components have appeared. The so-called functional components that have useful effects on the human body usually have a bitter taste, which will inevitably cause taste preference. reduced, resulting in a less attractive product. Although bitterness can make some foods taste delicious, such as beer, coffee, dark chocolate, and red wine, in most cases, the bitterness of food is unacceptable, and if the bitterness is too strong, it will be accompanied by unpleasantness and even disgust. In the pharmaceutical industry, many drugs are subject t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/22A23L29/00
CPCA23V2002/00A61K47/22A23L29/045A23L29/055A23V2200/16
Inventor 刘忠马冬磊揭辉洋李满妹
Owner JINAN UNIVERSITY
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