Transglutaminase inhibitor comprising chlorogenic acid and a method for producing thereof
A technology of transglutaminase and chlorogenic acid, which is applied to medical preparations containing active ingredients, pharmaceutical formulations, active ingredients of hydroxyl compounds, etc., can solve the problem of not mentioning the inhibitory activity of transglutaminase and the like
Inactive Publication Date: 2010-06-16
NAT CANCER CENT
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However, in the prior art, there is no mention of its inhibitory activity against transglutaminase
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Embodiment 1
[0045] Example 1: In vitro analysis of inhibition of transglutaminase activity
[0046] To measure the inhibitory activity of chlorogenic acid that competes with putrescine, the observation [1,4,- 14 C] Transglutaminase-catalyzed reaction between putrescine and succinyl casein.
[0047] Succinylated casein was purchased from Calbiochem (catalogue number 573464), 1 g of powder was dissolved in a solution containing 5 mM DTT (0.1 M Tris-acetate (pH 8.0), 10 mM CaCl 2 , 0.15M NaCl, 1.0mM EDTA) in 50ml of reaction buffer solution. This solution was stored in a deep freezer for future use. [1, 4- 14 C] 1,4-Butanediamine dihydrochloride (putrescine dihydrochloride) was purchased from GE Healthcare (catalogue number CFA301), and the stock solution was diluted with distilled water to yield a radiological dose of 5 μCi / ml. Transglutaminase 2 was purchased from Sigma-Aldrich (cat# T5398) and diluted with distilled water to give a final concentration of 1 unit / ml. Chlorogenic acid (...
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The present invention relates to a transglutaminase inhibitor comprising chlorogenic acid, a pharmaceutically acceptable salt thereof, or a derivative thereof. More particularly, the present invention relates to a transglutaminase inhibitor comprising chlorogenic acid, a pharmaceutically acceptable salt thereof, or a derivative thereof which effectively inhibits the activity of transglutaminase, the overexpression of which is responsible for the etiology of various diseases, and to novel uses thereof. The present invention provides a transglutaminase inhibitor and a method of inhibiting transglutaminase, both of which are based on using chlorogenic acid, a pharmaceutically acceptable salt thereof, or a derivative thereof as an active ingredient. Featuring the use of chlorogenic acid, a pharmaceutically acceptable salt thereof, or a derivative thereof, the novel method of inhibiting transglutaminase according to the present invention is safely applied to patients who suffer from the diseases caused by the overexpression of transglutaminase, thereby obtaining an inhibitory effect against transglutaminase without causing side-effects.
Description
technical field [0001] The present invention relates to a transglutaminase inhibitor comprising chlorogenic acid, a pharmaceutically acceptable salt thereof or a derivative thereof. More specifically, the present invention relates to a transglutaminase inhibitor comprising chlorogenic acid, a pharmaceutically acceptable salt thereof or a derivative thereof, which effectively inhibits the activity of transglutaminase, said transglutaminase The overexpression of is the etiological cause of various diseases, and the present invention relates to its novel use. Background technique [0002] Transglutaminase is a protective enzyme that is normally responsible for blood clotting in response to tissue damage. However, these enzymes have also been reported to play important roles in the pathophysiology of various diseases in which the expression levels of these enzymes lack regulation-control (review paper: Soo-Youl Kim: New Target Against Inflammatory Diseases: Transglutaminase 2.A...
Claims
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IPC IPC(8): A61K31/216
CPCA61K31/216A61P25/00A61P25/14A61P25/16A61P25/28A61P35/00A61P35/02A61P43/00A61K31/045
Inventor 金铢烈郑炅采
Owner NAT CANCER CENT